Identification

Name
Bioallethrin
Accession Number
DB13746
Type
Small Molecule
Groups
Approved, Experimental
Description

Bioallethrin refers to a mixture of two of the allethrin isomers (1R,trans;1R and 1R,trans;1S) in an approximate ratio of 1:1, where both isomers are active ingredients. A mixture of the two same stereoisomers, but in an approximate ratio of R:S in 1:3, is called esbiothrin. A mixture containing only S-forms of allethrin is referred to as esbioallethrin or S-bioallethrin. Bioallethrin is a synthetic pyrethroid used as a pesticide against household pest insects such as mosquitoes, houseflies and cockroaches. It is claimed to have low mammalian toxicity.

Synonyms
  • Depall├ęthrine
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Para Special Shampoo for Lice & NitsBioallethrin (1.1 %) + Piperonyl butoxide (4.4 %)ShampooTopicalMedican Technologies Inc.1989-12-312005-09-15Canada
ScabeneBioallethrin (0.63 %) + Piperonyl butoxide (5.04 %)AerosolTopicalMedican Technologies Inc.1997-06-102005-09-15Canada
Scabene AerosolBioallethrin (.63 %) + Piperonyl butoxide (5.04 %)AerosolTopicalStiefel Laboratories, Inc.1991-12-311997-11-19Canada
Categories
UNII
G79DM7O471
CAS number
584-79-2
Weight
Not Available
Chemical Formula
C19H26O3
InChI Key
ZCVAOQKBXKSDMS-AQYZNVCMSA-N
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Bioallethrin was used for lice and scabies infestation. Other pyrethroids are now used in place of bioallethrin.

Pharmacodynamics

Bioallethrin causes respiratory paralysis in lice and scabies parasites resulting in death [1].

Mechanism of action

Bioallethrin, like other pyrethroids, binds to voltage gated sodium channels in their closed state and modifies the gating kinetics [1]. Channel opening appears to increase affinity of the channel for pyrethroids like bioallethrin. Once bound pyrethroids slow both the opening and closing of the sodium channel resulting in a need for stronger excitatory potentials to produce an action potential and a delay in repolarization. The these changes make the neuron more susceptible to large action potentials and repeated firing by both increasing the initial threshold and reducing the input needed for after-potentials. When repeated firing does occur, the nerve terminal will release more neurotransmitter which can produce muscle paralysis through tetanus. This paralysis stops the breathing of lice and scabies parasites resulting in death.

Some pyrethroids act on calcium channels to increase intracelllular calcium [2]. Bioallethrin produces a very small increase in intracellular calcium in mouse neocortical neurons by acting on N-type calcium channels but the effect returns to baseline within 2 min. In contrast bioallethrin has been found to block L T, and P/Q-types of voltage gated calcium channels in human embryonic kidney cell cultures [6]. Bioallethrin has been found to inhibit both sodium-calcium dependent and magnesium-calcium ATP hydrolysis in insects although it, along with other type I pyrethroids, has a greater effect on sodium-calcium dependent hydrolysis [3]. Bioallethrin may stimulate phosphoinositol breakdown in synaptoneuromes as other type I pyrethroids have been observed to do so [4]. Other type I pyrethoids have also been found to bind to kainate receptors [5].

TargetActionsOrganism
UVoltage gated sodium channel
modulator
human
ASodium channel protein
modulator
Pediculus humanus
UVoltage-dependent N-type calcium channel
agonist
Human
UVoltage-dependent T-type calcium channel
blocker
Homo sapiens
UVoltage-dependent P/Q-type calcium channel
blocker
Homo sapiens
UVoltage dependent L type calcium channel
blocker
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Metabolism of bioallethrin in both rats and humans is considered to be virtually 100% oxidative [7, 8]. This is because bioallethrin is very resistant to hydrolysis of its ester group although a negligible amount of hydrolysis may occur.

In humans bioallethrin is metabolized primarily by CYP2C19 with some metabolism by CYP2C8, CYP3A4, and CYP2C9*2 [7]. The metabolites produced include primary alcohols via allylic oxidation near the cyclopropane group and subsequent oxidation to carboxylic acid, formation of a primary alcohol via oxidation of a methyl group to located on the cyclopropane portion of the molecule, formation of a primary alcohol via allylic oxidation near the 5-membered ring or formation of an epoxide at this location and subsequent hydrolysis to a diol.

In rats bioallethrin has been found to be metabolized mainly by CYP2C6, CYP2C11, and CYP3A1 with some contribution from CYP1A1, CYP2A1 and CYP3A2 [7]. Rats appear to metabolize bioallethrin at about 15 times the rate of humans.

Route of elimination

Pyrethroids are excreted in both the feces and urine but values specific to bioallethrin are not available [8].

Half life
Not Available
Clearance
Not Available
Toxicity

Bioallethrin can produce hypersensitivity reactions in patients sensitive to ragweed or chrysanthemum [10]. Ingestion of bioallethrin can produce life-threatening convulsions or coma. Less serious toxic effects include sore throat, nausea, vomiting, abdominal pain, mouth ulceration, increased secretions and/or dysphagia. Systemic effects include dizziness, headache and fatigue are common, and palpitations, chest tightness and blurred vision and occur 4-48 h after exposure.

Bioallethrin is not carcinogenic or mutagenic [9]. In rats doses over 58.7 mg/kg/day produce reproductive effects and doses over 125 mg/kg/day are embryotoxic.

Observed LD50 for various routes in animal studies [9]:

Rat

  • Male Oral - 709 mg/kg
  • Female Oral - 1040 mg/kg
  • Inhalation - 2.51 mg/L

Rabbit

  • Dermal - >3000 mg/kg
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe therapeutic efficacy of 2-HYDROXY-1,4-NAPHTHOQUINONE can be increased when used in combination with Bioallethrin.Experimental
2-mercaptobenzothiazoleThe therapeutic efficacy of 2-mercaptobenzothiazole can be increased when used in combination with Bioallethrin.Vet Approved
AbirateroneThe serum concentration of Bioallethrin can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of hypotension can be increased when Acepromazine is combined with Bioallethrin.Approved, Vet Approved
Acetyl sulfisoxazoleThe metabolism of Bioallethrin can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AlfuzosinThe risk or severity of hypotension can be increased when Alfuzosin is combined with Bioallethrin.Approved, Investigational
AmiodaroneThe metabolism of Bioallethrin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe risk or severity of hypotension can be increased when Amitriptyline is combined with Bioallethrin.Approved
AmobarbitalThe metabolism of Bioallethrin can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe therapeutic efficacy of Amorolfine can be increased when used in combination with Bioallethrin.Approved, Investigational
AmoxapineThe risk or severity of hypotension can be increased when Amoxapine is combined with Bioallethrin.Approved
Amphotericin BThe therapeutic efficacy of Amphotericin B can be increased when used in combination with Bioallethrin.Approved, Investigational
AnidulafunginThe therapeutic efficacy of Anidulafungin can be increased when used in combination with Bioallethrin.Approved, Investigational
ApalutamideThe serum concentration of Bioallethrin can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Bioallethrin can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe risk or severity of hypotension can be increased when Aripiprazole is combined with Bioallethrin.Approved, Investigational
ArmodafinilThe metabolism of Bioallethrin can be decreased when combined with Armodafinil.Approved, Investigational
ArotinololThe risk or severity of hypotension, conduction block, and bradycardia can be increased when Arotinolol is combined with Bioallethrin.Investigational
ArtemetherThe therapeutic efficacy of Artemether can be increased when used in combination with Bioallethrin.Approved
AsenapineThe risk or severity of hypotension can be increased when Asenapine is combined with Bioallethrin.Approved
AtazanavirThe metabolism of Bioallethrin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Bioallethrin can be decreased when combined with Atomoxetine.Approved
Bafilomycin A1The therapeutic efficacy of Bafilomycin A1 can be increased when used in combination with Bioallethrin.Experimental
BarbexacloneThe metabolism of Bioallethrin can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Bioallethrin can be increased when combined with Barbital.Illicit
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be increased when used in combination with Bioallethrin.Approved, Investigational
BevantololThe risk or severity of hypotension can be increased when Bevantolol is combined with Bioallethrin.Approved
BifonazoleThe therapeutic efficacy of Bifonazole can be increased when used in combination with Bioallethrin.Approved, Investigational
BoceprevirThe metabolism of Bioallethrin can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Bioallethrin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Bioallethrin can be decreased when it is combined with Bosentan.Approved, Investigational
Brefeldin AThe therapeutic efficacy of Brefeldin A can be increased when used in combination with Bioallethrin.Experimental
BrexpiprazoleThe risk or severity of hypotension can be increased when Brexpiprazole is combined with Bioallethrin.Approved, Investigational
BucindololThe risk or severity of hypotension can be increased when Bucindolol is combined with Bioallethrin.Investigational
BunazosinThe risk or severity of hypotension can be increased when Bunazosin is combined with Bioallethrin.Investigational
ButenafineThe therapeutic efficacy of Butenafine can be increased when used in combination with Bioallethrin.Approved
ButoconazoleThe therapeutic efficacy of Butoconazole can be increased when used in combination with Bioallethrin.Approved
Calcium AcetateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Acetate.Approved, Investigational
Calcium CarbonateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Carbonate.Approved, Investigational
Calcium ChlorideThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Chloride.Approved
Calcium CitrateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium lactate.Approved, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium levulinateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium levulinate.Approved, Experimental
Calcium pangamateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Calcium Phosphate.Approved
CandicidinThe therapeutic efficacy of Candicidin can be increased when used in combination with Bioallethrin.Withdrawn
CapecitabineThe metabolism of Bioallethrin can be decreased when combined with Capecitabine.Approved, Investigational
Capric acidThe therapeutic efficacy of Capric acid can be increased when used in combination with Bioallethrin.Experimental
CarbamazepineThe metabolism of Bioallethrin can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe risk or severity of hypotension can be increased when Carvedilol is combined with Bioallethrin.Approved, Investigational
CaseinThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Casein.Approved
CaspofunginThe therapeutic efficacy of Caspofungin can be increased when used in combination with Bioallethrin.Approved
CelecoxibThe metabolism of Bioallethrin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Bioallethrin can be increased when it is combined with Ceritinib.Approved
CeruleninThe therapeutic efficacy of Cerulenin can be increased when used in combination with Bioallethrin.Approved
ChloramphenicolThe metabolism of Bioallethrin can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroxineThe therapeutic efficacy of Chloroxine can be increased when used in combination with Bioallethrin.Approved
ChlorpromazineThe risk or severity of hypotension can be increased when Chlorpromazine is combined with Bioallethrin.Approved, Investigational, Vet Approved
CholecalciferolThe metabolism of Bioallethrin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiclopiroxThe therapeutic efficacy of Ciclopirox can be increased when used in combination with Bioallethrin.Approved, Investigational
CimetidineThe serum concentration of Bioallethrin can be increased when it is combined with Cimetidine.Approved, Investigational
CitalopramThe metabolism of Bioallethrin can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Bioallethrin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Bioallethrin can be decreased when combined with Clemastine.Approved, Investigational
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Bioallethrin.Approved
ClotrimazoleThe metabolism of Bioallethrin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of hypotension can be increased when Clozapine is combined with Bioallethrin.Approved
CobicistatThe metabolism of Bioallethrin can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Bioallethrin.Approved, Investigational
CordycepinThe therapeutic efficacy of Cordycepin can be increased when used in combination with Bioallethrin.Investigational
CrisaboroleThe metabolism of Bioallethrin can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Bioallethrin can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Bioallethrin can be decreased when combined with Curcumin.Approved, Investigational
CyclosporineThe metabolism of Bioallethrin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Bioallethrin can be decreased when it is combined with Dabrafenib.Approved, Investigational
DapiprazoleThe risk or severity of hypotension can be increased when Dapiprazole is combined with Bioallethrin.Approved
DarunavirThe metabolism of Bioallethrin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Bioallethrin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Bioallethrin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Bioallethrin can be decreased when combined with Delavirdine.Approved
DextroamphetamineThe risk or severity of hypotension can be increased when Dextroamphetamine is combined with Bioallethrin.Approved, Illicit
DichloropheneThe therapeutic efficacy of Dichlorophene can be increased when used in combination with Bioallethrin.Vet Approved
DihydroergotamineThe metabolism of Bioallethrin can be decreased when combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe metabolism of Bioallethrin can be decreased when combined with Diltiazem.Approved, Investigational
DosulepinThe metabolism of Bioallethrin can be decreased when combined with Dosulepin.Approved
DoxazosinThe risk or severity of hypotension can be increased when Doxazosin is combined with Bioallethrin.Approved
DoxepinThe risk or severity of hypotension can be increased when Doxepin is combined with Bioallethrin.Approved, Investigational
DoxycyclineThe metabolism of Bioallethrin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Bioallethrin can be decreased when combined with Dronedarone.Approved
DroperidolThe risk or severity of hypotension can be increased when Droperidol is combined with Bioallethrin.Approved, Vet Approved
EconazoleThe therapeutic efficacy of Econazole can be increased when used in combination with Bioallethrin.Approved
EfavirenzThe serum concentration of Bioallethrin can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe therapeutic efficacy of Efinaconazole can be increased when used in combination with Bioallethrin.Approved
EnzalutamideThe serum concentration of Bioallethrin can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe risk or severity of hypotension can be increased when Epinephrine is combined with Bioallethrin.Approved, Vet Approved
ErythromycinThe metabolism of Bioallethrin can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe risk or severity of hypotension can be increased when Escitalopram is combined with Bioallethrin.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Bioallethrin can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Bioallethrin can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe metabolism of Bioallethrin can be decreased when combined with Etravirine.Approved
FelodipineThe metabolism of Bioallethrin can be decreased when combined with Felodipine.Approved, Investigational
FenticonazoleThe therapeutic efficacy of Fenticonazole can be increased when used in combination with Bioallethrin.Experimental
FloxuridineThe metabolism of Bioallethrin can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Bioallethrin can be decreased when combined with Fluconazole.Approved, Investigational
FlucytosineThe therapeutic efficacy of Flucytosine can be increased when used in combination with Bioallethrin.Approved, Investigational
FluorouracilThe metabolism of Bioallethrin can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Bioallethrin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of hypotension can be increased when Flupentixol is combined with Bioallethrin.Approved, Investigational, Withdrawn
FlutrimazoleThe therapeutic efficacy of Flutrimazole can be increased when used in combination with Bioallethrin.Experimental
FluvastatinThe metabolism of Bioallethrin can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Bioallethrin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Bioallethrin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Bioallethrin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Bioallethrin can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Bioallethrin can be increased when it is combined with Fusidic Acid.Approved, Investigational
GemfibrozilThe metabolism of Bioallethrin can be decreased when combined with Gemfibrozil.Approved
GlyphosateThe therapeutic efficacy of Glyphosate can be increased when used in combination with Bioallethrin.Experimental
GriseofulvinThe therapeutic efficacy of Griseofulvin can be increased when used in combination with Bioallethrin.Approved, Investigational, Vet Approved
HachimycinThe therapeutic efficacy of Hachimycin can be increased when used in combination with Bioallethrin.Experimental
HaloproginThe therapeutic efficacy of Haloprogin can be increased when used in combination with Bioallethrin.Approved, Withdrawn
HexetidineThe therapeutic efficacy of Hexetidine can be increased when used in combination with Bioallethrin.Approved, Investigational
HexobarbitalThe metabolism of Bioallethrin can be increased when combined with Hexobarbital.Approved
IdelalisibThe metabolism of Bioallethrin can be decreased when combined with Idelalisib.Approved
IloperidoneThe risk or severity of hypotension can be increased when Iloperidone is combined with Bioallethrin.Approved
ImatinibThe metabolism of Bioallethrin can be decreased when combined with Imatinib.Approved
ImipramineThe risk or severity of hypotension can be increased when Imipramine is combined with Bioallethrin.Approved
IndinavirThe metabolism of Bioallethrin can be decreased when combined with Indinavir.Approved
IndoraminThe risk or severity of hypotension can be increased when Indoramin is combined with Bioallethrin.Withdrawn
IrbesartanThe metabolism of Bioallethrin can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoleThe serum concentration of Bioallethrin can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Bioallethrin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe therapeutic efficacy of Isoconazole can be increased when used in combination with Bioallethrin.Approved
IsoniazidThe metabolism of Bioallethrin can be decreased when combined with Isoniazid.Approved, Investigational
IsradipineThe metabolism of Bioallethrin can be decreased when combined with Isradipine.Approved, Investigational
ItraconazoleThe metabolism of Bioallethrin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Bioallethrin can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Bioallethrin can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolThe risk or severity of hypotension can be increased when Labetalol is combined with Bioallethrin.Approved
LapatinibThe metabolism of Bioallethrin can be decreased when combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Bioallethrin can be decreased when combined with Leflunomide.Approved, Investigational
LisdexamfetamineThe risk or severity of hypotension can be increased when Lisdexamfetamine is combined with Bioallethrin.Approved, Investigational
LobeglitazoneThe metabolism of Bioallethrin can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Bioallethrin can be decreased when combined with Lopinavir.Approved
LorpiprazoleThe serum concentration of Bioallethrin can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Bioallethrin can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Bioallethrin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Bioallethrin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Bioallethrin can be increased when it is combined with Lumacaftor.Approved
Magnesium hydroxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Bioallethrin is combined with Magnesium hydroxide.Approved, Investigational
Magnesium oxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Bioallethrin is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of hypotension and neuromuscular blockade can be increased when Bioallethrin is combined with Magnesium salicylate.Approved
Magnesium sulfateThe risk or severity of hypotension and neuromuscular blockade can be increased when Bioallethrin is combined with Magnesium sulfate.Approved, Investigational, Vet Approved
ManidipineThe metabolism of Bioallethrin can be decreased when combined with Manidipine.Approved, Investigational
MepartricinThe therapeutic efficacy of Mepartricin can be increased when used in combination with Bioallethrin.Experimental
MethohexitalThe metabolism of Bioallethrin can be increased when combined with Methohexital.Approved
MethotrimeprazineThe risk or severity of hypotension can be increased when Methotrimeprazine is combined with Bioallethrin.Approved, Investigational
MethylphenobarbitalThe metabolism of Bioallethrin can be increased when combined with Methylphenobarbital.Approved
MevastatinThe therapeutic efficacy of Mevastatin can be increased when used in combination with Bioallethrin.Experimental
MicafunginThe therapeutic efficacy of Micafungin can be increased when used in combination with Bioallethrin.Approved, Investigational
MiconazoleThe therapeutic efficacy of Miconazole can be increased when used in combination with Bioallethrin.Approved, Investigational, Vet Approved
MidostaurinThe metabolism of Bioallethrin can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Bioallethrin can be increased when it is combined with Mifepristone.Approved, Investigational
MiltefosineThe therapeutic efficacy of Miltefosine can be increased when used in combination with Bioallethrin.Approved, Investigational
MitotaneThe serum concentration of Bioallethrin can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Bioallethrin can be decreased when combined with Moclobemide.Approved, Investigational
ModafinilThe metabolism of Bioallethrin can be decreased when combined with Modafinil.Approved, Investigational
MonensinThe therapeutic efficacy of Monensin can be increased when used in combination with Bioallethrin.Vet Approved
MyxothiazolThe therapeutic efficacy of Myxothiazol can be increased when used in combination with Bioallethrin.Experimental
NabiloneThe metabolism of Bioallethrin can be decreased when combined with Nabilone.Approved, Investigational
NafcillinThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Nafcillin.Approved, Investigational
NaftifineThe therapeutic efficacy of Naftifine can be increased when used in combination with Bioallethrin.Approved
NatamycinThe therapeutic efficacy of Natamycin can be increased when used in combination with Bioallethrin.Approved
NefazodoneThe metabolism of Bioallethrin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Bioallethrin can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Bioallethrin can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Bioallethrin can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Bioallethrin can be decreased when combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of hypotension can be increased when Nicergoline is combined with Bioallethrin.Approved, Investigational
NifuratelThe therapeutic efficacy of Nifuratel can be increased when used in combination with Bioallethrin.Experimental
NiguldipineThe risk or severity of hypotension can be increased when Niguldipine is combined with Bioallethrin.Experimental
Nikkomycin ZThe therapeutic efficacy of Nikkomycin Z can be increased when used in combination with Bioallethrin.Investigational
NilotinibThe metabolism of Bioallethrin can be decreased when combined with Nilotinib.Approved, Investigational
NitroprussideBioallethrin may increase the hypotensive activities of Nitroprusside.Approved, Investigational
NitroxolineThe therapeutic efficacy of Nitroxoline can be increased when used in combination with Bioallethrin.Approved
NortriptylineThe risk or severity of hypotension can be increased when Nortriptyline is combined with Bioallethrin.Approved
NystatinThe therapeutic efficacy of Nystatin can be increased when used in combination with Bioallethrin.Approved, Vet Approved
OlanzapineThe risk or severity of hypotension can be increased when Olanzapine is combined with Bioallethrin.Approved, Investigational
OlaparibThe metabolism of Bioallethrin can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Bioallethrin can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OmoconazoleThe therapeutic efficacy of Omoconazole can be increased when used in combination with Bioallethrin.Experimental
OsimertinibThe serum concentration of Bioallethrin can be increased when it is combined with Osimertinib.Approved
OxiconazoleThe therapeutic efficacy of Oxiconazole can be increased when used in combination with Bioallethrin.Approved
PafuramidineThe therapeutic efficacy of Pafuramidine can be increased when used in combination with Bioallethrin.Investigational
PalbociclibThe serum concentration of Bioallethrin can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe risk or severity of hypotension can be increased when Paliperidone is combined with Bioallethrin.Approved
PantoprazoleThe metabolism of Bioallethrin can be decreased when combined with Pantoprazole.Approved
PentamidineThe therapeutic efficacy of Pentamidine can be increased when used in combination with Bioallethrin.Approved, Investigational
PentobarbitalThe metabolism of Bioallethrin can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PhenobarbitalThe metabolism of Bioallethrin can be increased when combined with Phenobarbital.Approved, Investigational
PhenoxybenzamineThe risk or severity of hypotension can be increased when Phenoxybenzamine is combined with Bioallethrin.Approved
PhentolamineThe risk or severity of hypotension can be increased when Phentolamine is combined with Bioallethrin.Approved
PhenytoinThe metabolism of Bioallethrin can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Bioallethrin can be decreased when combined with Pioglitazone.Approved, Investigational
PitolisantThe serum concentration of Bioallethrin can be decreased when it is combined with Pitolisant.Approved, Investigational
PizotifenThe risk or severity of hypotension can be increased when Pizotifen is combined with Bioallethrin.Approved
PosaconazoleThe metabolism of Bioallethrin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrazosinThe risk or severity of hypotension can be increased when Prazosin is combined with Bioallethrin.Approved
PrimidoneThe metabolism of Bioallethrin can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe risk or severity of hypotension can be increased when Promazine is combined with Bioallethrin.Approved, Vet Approved
PropericiazineThe risk or severity of hypotension can be increased when Propericiazine is combined with Bioallethrin.Approved, Investigational
PropiomazineThe risk or severity of hypotension can be increased when Propiomazine is combined with Bioallethrin.Approved
PropiverineThe risk or severity of hypotension can be increased when Propiverine is combined with Bioallethrin.Approved, Investigational
PyrimethamineThe metabolism of Bioallethrin can be decreased when combined with Pyrimethamine.Approved, Investigational, Vet Approved
PyrrolnitrinThe therapeutic efficacy of Pyrrolnitrin can be increased when used in combination with Bioallethrin.Experimental
QuetiapineThe risk or severity of hypotension can be increased when Quetiapine is combined with Bioallethrin.Approved
QuinidineThe risk or severity of hypotension can be increased when Quinidine is combined with Bioallethrin.Approved, Investigational
QuinineThe metabolism of Bioallethrin can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Bioallethrin can be decreased when combined with Rabeprazole.Approved, Investigational
RacepinephrineThe risk or severity of hypotension can be increased when Racepinephrine is combined with Bioallethrin.Approved
RadicicolThe therapeutic efficacy of Radicicol can be increased when used in combination with Bioallethrin.Experimental
RanolazineThe metabolism of Bioallethrin can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Bioallethrin can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Bioallethrin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Bioallethrin can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe risk or severity of hypotension can be increased when Rifaximin is combined with Bioallethrin.Approved, Investigational
RisperidoneThe risk or severity of hypotension can be increased when Risperidone is combined with Bioallethrin.Approved, Investigational
RosiglitazoneThe metabolism of Bioallethrin can be decreased when combined with Rosiglitazone.Approved, Investigational
RucaparibThe metabolism of Bioallethrin can be decreased when combined with Rucaparib.Approved, Investigational
Salicylhydroxamic AcidThe therapeutic efficacy of Salicylhydroxamic Acid can be increased when used in combination with Bioallethrin.Experimental
Salicylic acidThe therapeutic efficacy of Salicylic acid can be increased when used in combination with Bioallethrin.Approved, Investigational, Vet Approved
SaquinavirThe metabolism of Bioallethrin can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Bioallethrin can be decreased when used in combination with Sarilumab.Approved, Investigational
SecobarbitalThe metabolism of Bioallethrin can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe therapeutic efficacy of Sertaconazole can be increased when used in combination with Bioallethrin.Approved, Investigational
SertralineThe metabolism of Bioallethrin can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Bioallethrin can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe risk or severity of hypotension can be increased when Silodosin is combined with Bioallethrin.Approved
SiltuximabThe serum concentration of Bioallethrin can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Bioallethrin can be increased when it is combined with Simeprevir.Approved
SinefunginThe therapeutic efficacy of Sinefungin can be increased when used in combination with Bioallethrin.Experimental
SirolimusThe therapeutic efficacy of Sirolimus can be increased when used in combination with Bioallethrin.Approved, Investigational
SorafenibThe metabolism of Bioallethrin can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Bioallethrin can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Bioallethrin can be increased when it is combined with Stiripentol.Approved
SulconazoleThe therapeutic efficacy of Sulconazole can be increased when used in combination with Bioallethrin.Approved
SulfadiazineThe metabolism of Bioallethrin can be decreased when combined with Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleThe metabolism of Bioallethrin can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Bioallethrin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamoxifenThe metabolism of Bioallethrin can be decreased when combined with Tamoxifen.Approved
TamsulosinThe risk or severity of hypotension can be increased when Tamsulosin is combined with Bioallethrin.Approved, Investigational
TavaboroleThe therapeutic efficacy of Tavaborole can be increased when used in combination with Bioallethrin.Approved, Investigational
TelaprevirThe metabolism of Bioallethrin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Bioallethrin can be decreased when combined with Telithromycin.Approved
TerazosinThe risk or severity of hypotension can be increased when Terazosin is combined with Bioallethrin.Approved
TerbinafineThe therapeutic efficacy of Terbinafine can be increased when used in combination with Bioallethrin.Approved, Investigational, Vet Approved
TerconazoleThe therapeutic efficacy of Terconazole can be increased when used in combination with Bioallethrin.Approved
TeriflunomideThe metabolism of Bioallethrin can be decreased when combined with Teriflunomide.Approved
ThiamylalThe metabolism of Bioallethrin can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Bioallethrin can be increased when combined with Thiopental.Approved, Vet Approved
ThioproperazineThe risk or severity of hypotension can be increased when Thioproperazine is combined with Bioallethrin.Approved
ThioridazineThe risk or severity of hypotension can be increased when Thioridazine is combined with Bioallethrin.Approved, Withdrawn
ThymolThe therapeutic efficacy of Thymol can be increased when used in combination with Bioallethrin.Approved
TicagrelorThe metabolism of Bioallethrin can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Bioallethrin can be decreased when combined with Ticlopidine.Approved
TioconazoleThe therapeutic efficacy of Tioconazole can be increased when used in combination with Bioallethrin.Approved
TocilizumabThe serum concentration of Bioallethrin can be decreased when it is combined with Tocilizumab.Approved
TolazolineThe risk or severity of hypotension can be increased when Tolazoline is combined with Bioallethrin.Approved, Vet Approved
TolbutamideThe metabolism of Bioallethrin can be decreased when combined with Tolbutamide.Approved, Investigational
TolciclateThe therapeutic efficacy of Tolciclate can be increased when used in combination with Bioallethrin.Experimental
TolnaftateThe therapeutic efficacy of Tolnaftate can be increased when used in combination with Bioallethrin.Approved, Investigational, Vet Approved
TopiramateThe metabolism of Bioallethrin can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Bioallethrin can be decreased when combined with Topiroxostat.Approved, Investigational
TranylcypromineThe metabolism of Bioallethrin can be decreased when combined with Tranylcypromine.Approved, Investigational
TrazodoneThe risk or severity of hypotension can be increased when Trazodone is combined with Bioallethrin.Approved, Investigational
TrifluoperazineThe risk or severity of hypotension can be increased when Trifluoperazine is combined with Bioallethrin.Approved, Investigational
TrimazosinThe risk or severity of hypotension can be increased when Trimazosin is combined with Bioallethrin.Experimental
TrimethoprimThe metabolism of Bioallethrin can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimetrexateThe therapeutic efficacy of Trimetrexate can be increased when used in combination with Bioallethrin.Approved, Investigational
TrimipramineThe risk or severity of hypotension can be increased when Trimipramine is combined with Bioallethrin.Approved
UrapidilThe risk or severity of hypotension can be increased when Urapidil is combined with Bioallethrin.Investigational
Valproic AcidThe metabolism of Bioallethrin can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Bioallethrin can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Bioallethrin can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Bioallethrin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Bioallethrin can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Bioallethrin can be decreased when combined with Voriconazole.Approved, Investigational
WortmanninThe therapeutic efficacy of Wortmannin can be increased when used in combination with Bioallethrin.Experimental
ZafirlukastThe metabolism of Bioallethrin can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Bioallethrin can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Bioallethrin can be decreased when combined with Zucapsaicin.Approved, Investigational
ZuclopenthixolThe risk or severity of hypotension can be increased when Zuclopenthixol is combined with Bioallethrin.Approved, Investigational
Food Interactions
Not Available

References

General References
  1. Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. [PubMed:8841090]
  2. Cao Z, Shafer TJ, Murray TF: Mechanisms of pyrethroid insecticide-induced stimulation of calcium influx in neocortical neurons. J Pharmacol Exp Ther. 2011 Jan;336(1):197-205. doi: 10.1124/jpet.110.171850. Epub 2010 Sep 29. [PubMed:20881019]
  3. Clark JM, Matsumura F: The action of two classes of pyrethroids on the inhibition of brain Na-Ca and Ca + Mg ATP hydrolyzing activities of the American cockroach. Comp Biochem Physiol C. 1987;86(1):135-45. [PubMed:2881709]
  4. Gusovsky F, Hollingsworth EB, Daly JW: Regulation of phosphatidylinositol turnover in brain synaptoneurosomes: stimulatory effects of agents that enhance influx of sodium ions. Proc Natl Acad Sci U S A. 1986 May;83(9):3003-7. [PubMed:2422664]
  5. Staatz CG, Bloom AS, Lech JJ: Effect of pyrethroids on [3H]kainic acid binding to mouse forebrain membranes. Toxicol Appl Pharmacol. 1982 Jul;64(3):566-9. [PubMed:7135402]
  6. Hildebrand ME, McRory JE, Snutch TP, Stea A: Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin. J Pharmacol Exp Ther. 2004 Mar;308(3):805-13. doi: 10.1124/jpet.103.058792. Epub 2003 Nov 21. [PubMed:14634047]
  7. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
  8. Miyamoto J: Degradation, metabolism and toxicity of synthetic pyrethroids. Environ Health Perspect. 1976 Apr;14:15-28. [PubMed:789062]
  9. WHO SPECIFICATIONS AND EVALUATIONS FOR PUBLIC HEALTH PESTICIDES: Bioallethrin [Link]
  10. HSDB: Allethrins [Link]
External Links
PubChem Compound
15558638
PubChem Substance
347829312
ChemSpider
18923353
ChEBI
39118
ChEMBL
CHEMBL1788403
Wikipedia
Bioallethrin
ATC Codes
P03AC02 — BioallethrinP03AC52 — Bioallethrin, combinations
MSDS
Download (273 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
ShampooTopical
AerosolTopical
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
boiling point (┬░C)165-170WHO SPECIFICATIONS AND EVALUATIONS FOR PUBLIC HEALTH PESTICIDES : BIOALLETHRIN
water solubility4.6 mg/LWHO SPECIFICATIONS AND EVALUATIONS FOR PUBLIC HEALTH PESTICIDES : BIOALLETHRIN
logP4.7WHO SPECIFICATIONS AND EVALUATIONS FOR PUBLIC HEALTH PESTICIDES : BIOALLETHRIN
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

1. Voltage gated sodium channel
Kind
Protein group
Organism
human
Pharmacological action
Unknown
Actions
Modulator
Curator comments
Bioallethrin slows the opening and closing of the channel.
References
  1. Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. [PubMed:8841090]
Kind
Protein
Organism
Pediculus humanus
Pharmacological action
Yes
Actions
Modulator
Curator comments
Bioallethrin slows the opening and closing of the channel.
General Function
Mediates the voltage-dependent sodium ion permeability of excitable membranes.
Specific Function
Calcium ion binding
Gene Name
Not Available
Uniprot ID
Q86DI9
Uniprot Name
Sodium channel protein
Molecular Weight
233296.52 Da
References
  1. Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. [PubMed:8841090]
3. Voltage-dependent N-type calcium channel
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
Curator comments
Seems to be a weak agonist at N-type but blocker at L, T, and P/Q-type.
References
  1. Cao Z, Shafer TJ, Murray TF: Mechanisms of pyrethroid insecticide-induced stimulation of calcium influx in neocortical neurons. J Pharmacol Exp Ther. 2011 Jan;336(1):197-205. doi: 10.1124/jpet.110.171850. Epub 2010 Sep 29. [PubMed:20881019]
Kind
Protein group
Organism
Homo sapiens
Pharmacological action
Unknown
Actions
Blocker
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...

Components:
References
  1. Hildebrand ME, McRory JE, Snutch TP, Stea A: Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin. J Pharmacol Exp Ther. 2004 Mar;308(3):805-13. doi: 10.1124/jpet.103.058792. Epub 2003 Nov 21. [PubMed:14634047]
Kind
Protein group
Organism
Homo sapiens
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...

Components:
References
  1. Hildebrand ME, McRory JE, Snutch TP, Stea A: Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin. J Pharmacol Exp Ther. 2004 Mar;308(3):805-13. doi: 10.1124/jpet.103.058792. Epub 2003 Nov 21. [PubMed:14634047]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Blocker
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...

Components:
References
  1. Hildebrand ME, McRory JE, Snutch TP, Stea A: Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin. J Pharmacol Exp Ther. 2004 Mar;308(3):805-13. doi: 10.1124/jpet.103.058792. Epub 2003 Nov 21. [PubMed:14634047]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Curator comments
Only metabolized by the CYP2C9*2 variant.
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Highly active in the 7-alpha-hydroxylation of testosterone, progesterone and androstenedione.
Gene Name
Cyp2a1
Uniprot ID
P11711
Uniprot Name
Cytochrome P450 2A1
Molecular Weight
55994.635 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Specific Function
Aromatase activity
Gene Name
Cyp1a1
Uniprot ID
P00185
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
59392.695 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Specific Function
Arachidonic acid epoxygenase activity
Gene Name
Cyp2c6
Uniprot ID
P05178
Uniprot Name
Cytochrome P450 2C6
Molecular Weight
56002.315 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Metabolizes testosterone mainly in positions 2 alpha and 16 alpha.
Specific Function
Arachidonic acid epoxygenase activity
Gene Name
Cyp2c11
Uniprot ID
P08683
Uniprot Name
Cytochrome P450 2C11
Molecular Weight
57180.595 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Testosterone 6-beta-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
Cyp3a1
Uniprot ID
P04800
Uniprot Name
Cytochrome P450 3A1
Molecular Weight
57917.375 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]
Kind
Protein
Organism
Rat
Pharmacological action
No
Actions
Substrate
General Function
Testosterone 6-beta-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
Cyp3a2
Uniprot ID
P05183
Uniprot Name
Cytochrome P450 3A2
Molecular Weight
57731.215 Da
References
  1. Scollon EJ, Starr JM, Godin SJ, DeVito MJ, Hughes MF: In vitro metabolism of pyrethroid pesticides by rat and human hepatic microsomes and cytochrome p450 isoforms. Drug Metab Dispos. 2009 Jan;37(1):221-8. doi: 10.1124/dmd.108.022343. Epub 2008 Oct 23. [PubMed:18948380]

Drug created on June 23, 2017 14:47 / Updated on July 02, 2018 19:55