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Identification
NameAlimemazine
Accession NumberDB01246  (APRD00258)
TypeSmall Molecule
GroupsApproved, Vet Approved
DescriptionA phenothiazine derivative that is used as an antipruritic. [PubChem]
Structure
Thumb
Synonyms
Alimemazine
Methylpromazine
Repeltin
Trimeprazine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Panectyl 2.5 Liq 2.5mg/5mlLiquid2.5 mgOralAventis Pharma Inc1960-12-312003-07-22Canada
Panectyl Tab 2.5mgTablet2.5 mgOralErfa Canada 2012 Inc1959-12-31Not applicableCanada
Panectyl Tab 5mgTablet5 mgOralErfa Canada 2012 Inc1959-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlimezineNot Available
NedeltranNot Available
PanectylNot Available
TheralenNot Available
TheraleneNot Available
VallerganNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Alimemazine tartrate
4330-99-8
Thumb
  • InChI Key: AJZJIYUOOJLBAU-RNKHSWPKSA-N
  • Monoisotopic Mass: 746.317176732
  • Average Mass: 746.978
DBSALT000183
Categories
UNII76H78MJJ52
CAS number84-96-8
WeightAverage: 298.446
Monoisotopic: 298.150369404
Chemical FormulaC18H22N2S
InChI KeyZZHLYYDVIOPZBE-UHFFFAOYSA-N
InChI
InChI=1S/C18H22N2S/c1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)21-18-11-7-5-9-16(18)20/h4-11,14H,12-13H2,1-3H3
IUPAC Name
dimethyl[2-methyl-3-(10H-phenothiazin-10-yl)propyl]amine
SMILES
CC(CN(C)C)CN1C2=CC=CC=C2SC2=CC=CC=C12
Pharmacology
IndicationUsed to prevent and relieve allergic conditions which cause pruritus (itching) and urticaria (some allergic skin reactions).
Structured Indications
PharmacodynamicsTrimeprazine (also known as Alimemazine) is a tricyclic antihistamine, similar in structure to the phenothiazine antipsychotics, but differing in the ring-substitution and chain characteristics. Trimeprazine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, trimeprazine is not used clinically as an anti-psychotic. It acts as an anti-histamine, a sedative, and an anti-emetic (anti-nausea). Trimeprazine is used principally as an anti-emetic, to prevent motion sickness or as an anti-histamine in combination with other medications in cough and cold preparations. Tricyclic antihistamines are also structurally-related to the tricyclic antidepressants, explaining the antihistaminergic adverse effects of these two drug classes and also the poor tolerability profile of tricyclic H1-antihistamines.
Mechanism of actionTrimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding.
TargetKindPharmacological actionActionsOrganismUniProt ID
Histamine H1 receptorProteinyes
antagonist
HumanP35367 details
Related Articles
AbsorptionWell absorbed in the digestive tract.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySymptoms of overdose clumsiness or unsteadiness, seizures, severe drowsiness, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath, shuffling walk, tic-like (jerky) movements of head and face, trembling and shaking of hands, and insomnia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Alimemazine.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Alimemazine.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Alimemazine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Alimemazine.Experimental, Illicit
5'-Deoxy-5'-MethylthioadenosineThe serum concentration of Alimemazine can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine.Experimental
AcebutololAlimemazine may increase the hypotensive activities of Acebutolol.Approved
AlfentanilAlimemazine may increase the hypotensive activities of Alfentanil.Approved, Illicit
AlphacetylmethadolAlimemazine may increase the hypotensive activities of Alphacetylmethadol.Experimental, Illicit
AlprenololAlimemazine may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminum phosphateAluminum phosphate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AmodiaquineThe serum concentration of Alimemazine can be increased when it is combined with Amodiaquine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Amoxapine.Approved
AmphetamineAmphetamine may decrease the sedative activities of Alimemazine.Approved, Illicit
Aop200704Alimemazine may increase the hypotensive activities of Aop200704.Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Alimemazine.Approved, Investigational
ArotinololAlimemazine may increase the hypotensive activities of Arotinolol.Approved
ArtemetherThe serum concentration of Alimemazine can be increased when it is combined with Artemether.Approved
ArtemisininThe serum concentration of Alimemazine can be increased when it is combined with Artemisinin.Investigational
ArtesunateThe serum concentration of Alimemazine can be increased when it is combined with Artesunate.Approved
AtenololAlimemazine may increase the hypotensive activities of Atenolol.Approved
AtovaquoneThe serum concentration of Alimemazine can be increased when it is combined with Atovaquone.Approved
BefunololAlimemazine may increase the hypotensive activities of Befunolol.Experimental
BenzphetamineBenzphetamine may decrease the sedative activities of Alimemazine.Approved, Illicit
Benzylpenicilloyl PolylysineAlimemazine may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Alimemazine.Approved
BetaxololAlimemazine may increase the hypotensive activities of Betaxolol.Approved
Betulinic AcidThe serum concentration of Alimemazine can be increased when it is combined with Betulinic Acid.Investigational
BevantololAlimemazine may increase the hypotensive activities of Bevantolol.Approved
BezitramideAlimemazine may increase the hypotensive activities of Bezitramide.Experimental, Illicit, Withdrawn
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
BisoprololAlimemazine may increase the hypotensive activities of Bisoprolol.Approved
BopindololAlimemazine may increase the hypotensive activities of Bopindolol.Approved
BucindololAlimemazine may increase the hypotensive activities of Bucindolol.Investigational
BufuralolAlimemazine may increase the hypotensive activities of Bufuralol.Experimental, Investigational
BupranololAlimemazine may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineAlimemazine may increase the hypotensive activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolAlimemazine may increase the hypotensive activities of Butorphanol.Approved, Illicit, Vet Approved
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CarfentanilAlimemazine may increase the hypotensive activities of Carfentanil.Illicit, Vet Approved
CarteololAlimemazine may increase the hypotensive activities of Carteolol.Approved
CarvedilolAlimemazine may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololAlimemazine may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of Alimemazine can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Alimemazine.Illicit, Withdrawn
CitalopramThe risk or severity of adverse effects can be increased when Alimemazine is combined with Citalopram.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Clomipramine.Approved, Vet Approved
CodeineAlimemazine may increase the hypotensive activities of Codeine.Approved, Illicit
DapoxetineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Dapoxetine.Investigational
DapsoneThe serum concentration of Alimemazine can be increased when it is combined with Dapsone.Approved, Investigational
DextroamphetamineDextroamphetamine may decrease the sedative activities of Alimemazine.Approved, Illicit
DextromoramideAlimemazine may increase the hypotensive activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneAlimemazine may increase the hypotensive activities of Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineAlimemazine may increase the hypotensive activities of Dezocine.Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Alimemazine.Approved, Illicit
DihydroartemisininThe serum concentration of Alimemazine can be increased when it is combined with Dihydroartemisinin.Approved
DihydrocodeineAlimemazine may increase the hypotensive activities of Dihydrocodeine.Approved, Illicit
DihydroetorphineAlimemazine may increase the hypotensive activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineAlimemazine may increase the hypotensive activities of Dihydromorphine.Experimental, Illicit
DiphenoxylateAlimemazine may increase the hypotensive activities of Diphenoxylate.Approved, Illicit
DoxycyclineThe serum concentration of Alimemazine can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEAlimemazine may increase the hypotensive activities of DPDPE.Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Alimemazine is combined with Escitalopram.Approved, Investigational
EsmololAlimemazine may increase the hypotensive activities of Esmolol.Approved
EthylmorphineAlimemazine may increase the hypotensive activities of Ethylmorphine.Approved, Illicit
EtoperidoneThe risk or severity of adverse effects can be increased when Alimemazine is combined with Etoperidone.Approved
EtorphineAlimemazine may increase the hypotensive activities of Etorphine.Illicit, Vet Approved
FenfluramineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Fenfluramine.Illicit, Withdrawn
FentanylAlimemazine may increase the hypotensive activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Fluvoxamine.Approved, Investigational
HalofantrineThe serum concentration of Alimemazine can be increased when it is combined with Halofantrine.Approved
HeroinAlimemazine may increase the hypotensive activities of Heroin.Approved, Illicit
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Alimemazine.Approved, Investigational
HydrocodoneAlimemazine may increase the hypotensive activities of Hydrocodone.Approved, Illicit
HydromorphoneAlimemazine may increase the hypotensive activities of Hydromorphone.Approved, Illicit
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide may decrease the sedative activities of Alimemazine.Approved
HydroxychloroquineThe serum concentration of Alimemazine can be increased when it is combined with Hydroxychloroquine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Indalpine.Investigational, Withdrawn
IndenololAlimemazine may increase the hypotensive activities of Indenolol.Withdrawn
KetobemidoneAlimemazine may increase the hypotensive activities of Ketobemidone.Approved
LabetalolAlimemazine may increase the hypotensive activities of Labetalol.Approved
LevobunololAlimemazine may increase the hypotensive activities of Levobunolol.Approved
Levomethadyl AcetateAlimemazine may increase the hypotensive activities of Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Alimemazine is combined with Levomilnacipran.Approved
LevorphanolAlimemazine may increase the hypotensive activities of Levorphanol.Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Alimemazine.Approved, Investigational
LofentanilAlimemazine may increase the hypotensive activities of Lofentanil.Illicit
Lu AA21004The risk or severity of adverse effects can be increased when Alimemazine is combined with Lu AA21004.Investigational
LumefantrineThe serum concentration of Alimemazine can be increased when it is combined with Lumefantrine.Approved
MagaldrateMagaldrate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Withdrawn
Magnesium carbonateMagnesium carbonate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MefloquineThe serum concentration of Alimemazine can be increased when it is combined with Mefloquine.Approved
MephedroneMephedrone may decrease the sedative activities of Alimemazine.Investigational
MephentermineMephentermine may decrease the sedative activities of Alimemazine.Approved
MethadoneAlimemazine may increase the hypotensive activities of Methadone.Approved
Methadyl AcetateAlimemazine may increase the hypotensive activities of Methadyl Acetate.Approved, Illicit
MethamphetamineMethamphetamine may decrease the sedative activities of Alimemazine.Approved, Illicit
MetipranololAlimemazine may increase the hypotensive activities of Metipranolol.Approved
MetoprololAlimemazine may increase the hypotensive activities of Metoprolol.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Alimemazine is combined with Milnacipran.Approved
MizoribineThe serum concentration of Alimemazine can be increased when it is combined with Mizoribine.Investigational
MMDAMMDA may decrease the sedative activities of Alimemazine.Experimental, Illicit
MorphineAlimemazine may increase the hypotensive activities of Morphine.Approved, Investigational
NadololAlimemazine may increase the hypotensive activities of Nadolol.Approved
NalbuphineAlimemazine may increase the hypotensive activities of Nalbuphine.Approved
NormethadoneAlimemazine may increase the hypotensive activities of Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Olanzapine.Approved, Investigational
OpiumAlimemazine may increase the hypotensive activities of Opium.Approved, Illicit
OxprenololAlimemazine may increase the hypotensive activities of Oxprenolol.Approved
OxycodoneAlimemazine may increase the hypotensive activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneAlimemazine may increase the hypotensive activities of Oxymorphone.Approved, Investigational, Vet Approved
ParoxetineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Paroxetine.Approved, Investigational
PenbutololAlimemazine may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineAlimemazine may increase the hypotensive activities of Pentazocine.Approved, Vet Approved
PethidineAlimemazine may increase the hypotensive activities of Pethidine.Approved
PhenterminePhentermine may decrease the sedative activities of Alimemazine.Approved, Illicit
PindololAlimemazine may increase the hypotensive activities of Pindolol.Approved
PiritramideAlimemazine may increase the hypotensive activities of Piritramide.Investigational
PractololAlimemazine may increase the hypotensive activities of Practolol.Approved
PrimaquineThe serum concentration of Alimemazine can be increased when it is combined with Primaquine.Approved
ProguanilThe serum concentration of Alimemazine can be increased when it is combined with Proguanil.Approved
PropranololAlimemazine may increase the hypotensive activities of Propranolol.Approved, Investigational
PseudoephedrinePseudoephedrine may decrease the sedative activities of Alimemazine.Approved
PyrimethamineThe serum concentration of Alimemazine can be increased when it is combined with Pyrimethamine.Approved, Vet Approved
PyronaridineThe serum concentration of Alimemazine can be increased when it is combined with Pyronaridine.Investigational
QuinacrineThe serum concentration of Alimemazine can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Alimemazine can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Alimemazine can be increased when it is combined with Quinine.Approved
RadicicolThe serum concentration of Alimemazine can be increased when it is combined with Radicicol.Experimental
RemifentanilAlimemazine may increase the hypotensive activities of Remifentanil.Approved
RitobegronRitobegron may decrease the sedative activities of Alimemazine.Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Alimemazine.Approved
SertralineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Sertraline.Approved
SinefunginThe serum concentration of Alimemazine can be increased when it is combined with Sinefungin.Experimental
SotalolAlimemazine may increase the hypotensive activities of Sotalol.Approved
SufentanilAlimemazine may increase the hypotensive activities of Sufentanil.Approved, Investigational
SulfadoxineThe serum concentration of Alimemazine can be increased when it is combined with Sulfadoxine.Approved
SulfametopyrazineThe serum concentration of Alimemazine can be increased when it is combined with Sulfametopyrazine.Approved, Withdrawn
tafenoquineThe serum concentration of Alimemazine can be increased when it is combined with tafenoquine.Investigational
TapentadolAlimemazine may increase the hypotensive activities of Tapentadol.Approved
ThiopentalThe risk or severity of adverse effects can be increased when Alimemazine is combined with Thiopental.Approved, Vet Approved
TimololAlimemazine may increase the hypotensive activities of Timolol.Approved
TramadolAlimemazine may increase the hypotensive activities of Tramadol.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Alimemazine is combined with Trazodone.Approved, Investigational
TrimethoprimThe serum concentration of Alimemazine can be increased when it is combined with Trimethoprim.Approved, Vet Approved
VilazodoneThe risk or severity of adverse effects can be increased when Alimemazine is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Vortioxetine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Alimemazine is combined with Zimelidine.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesR06AD01
AHFS Codes
  • 04:04.12
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9738
Blood Brain Barrier+0.9886
Caco-2 permeable+0.7965
P-glycoprotein substrateSubstrate0.6637
P-glycoprotein inhibitor IInhibitor0.6501
P-glycoprotein inhibitor IIInhibitor0.7613
Renal organic cation transporterNon-inhibitor0.5286
CYP450 2C9 substrateNon-substrate0.7739
CYP450 2D6 substrateSubstrate0.748
CYP450 3A4 substrateSubstrate0.5224
CYP450 1A2 substrateNon-inhibitor0.804
CYP450 2C9 inhibitorNon-inhibitor0.9195
CYP450 2D6 inhibitorInhibitor0.9381
CYP450 2C19 inhibitorNon-inhibitor0.8436
CYP450 3A4 inhibitorNon-inhibitor0.6702
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6487
Ames testNon AMES toxic0.7784
CarcinogenicityNon-carcinogens0.9034
BiodegradationNot ready biodegradable0.9968
Rat acute toxicity3.1217 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9819
hERG inhibition (predictor II)Inhibitor0.818
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
LiquidOral2.5 mg
TabletOral2.5 mg
TabletOral5 mg
Prices
Unit descriptionCostUnit
Panectyl 5 mg Tablet0.37USD tablet
Panectyl 2.5 mg Tablet0.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point68 °CPhysProp
boiling point150-175 °C at 3.00E-01 mm HgPhysProp
water solubility0.942 mg/LNot Available
logP4.71HANSCH,C ET AL. (1995)
pKa9.05SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.00835 mg/mLALOGPS
logP4.82ALOGPS
logP4.41ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)9.42ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity93.37 m3·mol-1ChemAxon
Polarizability34.83 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.83 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiazines
Sub ClassPhenothiazines
Direct ParentPhenothiazines
Alternative Parents
Substituents
  • Phenothiazine
  • Alkyldiarylamine
  • Diarylthioether
  • Benzenoid
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55783.61 Da
References
  1. Santos DE, Liu GJ, Takeuchi H: Blockers for excitatory effects of achatin-I, a tetrapeptide having a D-phenylalanine residue, on a snail neurone. Eur J Pharmacol. 1995 Jan 16;272(2-3):231-9. [PubMed:7713167 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23