Identification

Name
Adinazolam
Accession Number
DB00546  (APRD00724)
Type
Small Molecule
Groups
Approved
Description

Adinazolam (Deracyn®) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and was never available to the public.

Structure
Thumb
Synonyms
  • 8-Chloro-1-((dimethylamino)methyl)-6-phenyl-4H-S-triazolo(4,3-a)(1,4)benzodiazepine
  • Adinazolamum
Product Ingredients
IngredientUNIICASInChI Key
Adinazolam mesylateNT8S62A72757938-82-6FENBITQPWFCMEB-UHFFFAOYSA-N
International/Other Brands
Deracyn (Upjohn)
Categories
UNII
KN08449444
CAS number
37115-32-5
Weight
Average: 351.833
Monoisotopic: 351.125073308
Chemical Formula
C19H18ClN5
InChI Key
GJSLOMWRLALDCT-UHFFFAOYSA-N
InChI
InChI=1S/C19H18ClN5/c1-24(2)12-18-23-22-17-11-21-19(13-6-4-3-5-7-13)15-10-14(20)8-9-16(15)25(17)18/h3-10H,11-12H2,1-2H3
IUPAC Name
({12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaen-3-yl}methyl)dimethylamine
SMILES
CN(C)CC1=NN=C2CN=C(C3=CC=CC=C3)C3=C(C=CC(Cl)=C3)N12

Pharmacology

Indication

For the treatment of anxiety and status epilepticus.

Structured Indications
Not Available
Pharmacodynamics

Adinazolam is a benzodiazepine derivative used to treat anxiety, status epilepticus, and for sedation induction and anterograde amnesia. Adinazolam binds with high affinity to the GABA benzodiazepine receptor complex. Considerable evidence suggest that the central pharmacologic/therapeutic actions of alprazolam are mediated via interaction with this receptor complex.

Mechanism of action

Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit delta
potentiator
Human
AGamma-aminobutyric acid receptor subunit epsilon
potentiator
Human
AGamma-aminobutyric acid receptor subunit pi
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-3
potentiator
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic. The main metabolite is N-desmethyladinazolam. The other two metabolites are alpha-hydroxyalprazolam and estazolam.

Route of elimination
Not Available
Half life

Less than 3 hours.

Clearance
Not Available
Toxicity

Signs of overdose may include muscle weakness, ataxia, dysarthria and particularly in children paradoxical excitement. In more severe cases diminished reflexes, confusion, and coma may ensue.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe metabolism of Adinazolam can be decreased when combined with Abiraterone.Approved
AmiodaroneThe metabolism of Adinazolam can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Adinazolam can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Adinazolam can be decreased when combined with Armodafinil.Approved, Investigational
AtazanavirThe metabolism of Adinazolam can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Adinazolam can be decreased when combined with Atomoxetine.Approved
BoceprevirThe metabolism of Adinazolam can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Adinazolam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Adinazolam can be decreased when it is combined with Bosentan.Approved, Investigational
CarbamazepineThe metabolism of Adinazolam can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Adinazolam can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Adinazolam can be decreased when combined with Chloramphenicol.Approved, Vet Approved
CholecalciferolThe metabolism of Adinazolam can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Adinazolam can be decreased when combined with Cimetidine.Approved
CitalopramThe metabolism of Adinazolam can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Adinazolam can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Adinazolam can be decreased when combined with Clemastine.Approved
ClotrimazoleThe metabolism of Adinazolam can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Adinazolam can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Adinazolam can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Adinazolam can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Adinazolam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Adinazolam can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Adinazolam can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Adinazolam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Adinazolam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Adinazolam can be decreased when combined with Delavirdine.Approved
DihydroergotamineThe metabolism of Adinazolam can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Adinazolam can be decreased when combined with Diltiazem.Approved
DoxycyclineThe metabolism of Adinazolam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Adinazolam can be decreased when combined with Dronedarone.Approved
EfavirenzThe metabolism of Adinazolam can be decreased when combined with Efavirenz.Approved, Investigational
EnzalutamideThe serum concentration of Adinazolam can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Adinazolam can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe metabolism of Adinazolam can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Adinazolam can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe metabolism of Adinazolam can be decreased when combined with Etravirine.Approved
FluconazoleThe metabolism of Adinazolam can be decreased when combined with Fluconazole.Approved
FluoxetineThe metabolism of Adinazolam can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe metabolism of Adinazolam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Adinazolam can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Adinazolam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Adinazolam can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Adinazolam can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Adinazolam can be decreased when combined with Gemfibrozil.Approved
IdelalisibThe serum concentration of Adinazolam can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Adinazolam can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Adinazolam can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Adinazolam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Adinazolam can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Adinazolam can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Adinazolam can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Adinazolam can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Adinazolam can be decreased when combined with Ketoconazole.Approved, Investigational
LobeglitazoneThe metabolism of Adinazolam can be decreased when combined with Lobeglitazone.Approved
LopinavirThe metabolism of Adinazolam can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Adinazolam can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Adinazolam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Adinazolam can be decreased when it is combined with Lumacaftor.Approved
MifepristoneThe serum concentration of Adinazolam can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Adinazolam can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Adinazolam can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Adinazolam can be decreased when combined with Modafinil.Approved, Investigational
NefazodoneThe metabolism of Adinazolam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Adinazolam can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Adinazolam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Adinazolam can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Adinazolam can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Adinazolam can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Adinazolam can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Adinazolam can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Adinazolam can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Adinazolam can be increased when it is combined with Palbociclib.Approved
PantoprazoleThe metabolism of Adinazolam can be decreased when combined with Pantoprazole.Approved
PentobarbitalThe metabolism of Adinazolam can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Adinazolam can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Adinazolam can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Adinazolam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Adinazolam can be increased when combined with Primidone.Approved, Vet Approved
RanolazineThe metabolism of Adinazolam can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Adinazolam can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Adinazolam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Adinazolam can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Adinazolam can be decreased when combined with Ritonavir.Approved, Investigational
SaquinavirThe metabolism of Adinazolam can be decreased when combined with Saquinavir.Approved, Investigational
SertralineThe metabolism of Adinazolam can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Adinazolam can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Adinazolam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Adinazolam can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Adinazolam can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Adinazolam can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Adinazolam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Adinazolam can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Adinazolam can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Adinazolam can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Adinazolam can be decreased when it is combined with Tocilizumab.Approved
TopiramateThe metabolism of Adinazolam can be decreased when combined with Topiramate.Approved
TranylcypromineThe metabolism of Adinazolam can be decreased when combined with Tranylcypromine.Approved
VenlafaxineThe metabolism of Adinazolam can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Adinazolam can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Adinazolam can be decreased when combined with Voriconazole.Approved, Investigational
YohimbineThe therapeutic efficacy of Adinazolam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZiprasidoneThe metabolism of Adinazolam can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Adinazolam can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
  3. File SE, Pellow S: Triazolobenzodiazepines antagonize the effects of anxiogenic drugs mediated at three different central nervous system sites. Neurosci Lett. 1985 Oct 24;61(1-2):115-9. [PubMed:2867497]
External Links
Human Metabolome Database
HMDB14686
KEGG Drug
D02770
PubChem Compound
37632
PubChem Substance
46509054
ChemSpider
34519
BindingDB
82439
ChEBI
251412
ChEMBL
CHEMBL328250
Therapeutic Targets Database
DAP001251
PharmGKB
PA164783813
Wikipedia
Adinazolam
ATC Codes
N05BA07 — Adinazolam

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP4.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0672 mg/mLALOGPS
logP2.57ALOGPS
logP2.24ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)18.38ChemAxon
pKa (Strongest Basic)6.66ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area46.31 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity112.31 m3·mol-1ChemAxon
Polarizability37.15 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9382
Caco-2 permeable+0.6532
P-glycoprotein substrateSubstrate0.666
P-glycoprotein inhibitor IInhibitor0.5
P-glycoprotein inhibitor IIInhibitor0.942
Renal organic cation transporterInhibitor0.8284
CYP450 2C9 substrateNon-substrate0.8375
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateInhibitor0.6707
CYP450 2C9 inhibitorInhibitor0.5
CYP450 2D6 inhibitorNon-inhibitor0.7089
CYP450 2C19 inhibitorNon-inhibitor0.6787
CYP450 3A4 inhibitorNon-inhibitor0.7326
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7718
Ames testNon AMES toxic0.8085
CarcinogenicityNon-carcinogens0.6543
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6288 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9259
hERG inhibition (predictor II)Non-inhibitor0.6971
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as 1,2,4-triazolo[4,3-a][1,4]benzodiazepines. These are aromatic compounds containing a 1,4-benzodiazepine fused to and sharing a nitrogen atom with a 1,2,4-triazole ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,2,4-triazolo[4,3-a][1,4]benzodiazepines
Alternative Parents
Aralkylamines / Benzene and substituted derivatives / Aryl chlorides / Triazoles / Heteroaromatic compounds / Trialkylamines / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds
show 2 more
Substituents
1,2,4-triazolo[4,3-a][1,4]benzodiazepine / Aralkylamine / Aryl chloride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Azole / Heteroaromatic compound / 1,2,4-triazole / Ketimine
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
triazolobenzodiazepine (CHEBI:251412)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA2
Uniprot ID
P47869
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA3
Uniprot ID
P34903
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Transporter activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRA5
Uniprot ID
P31644
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG1
Uniprot ID
Q8N1C3
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight
53594.49 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRG2
Uniprot ID
P18507
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight
54161.78 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRG3
Uniprot ID
Q99928
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight
54288.16 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB2
Uniprot ID
P47870
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-2
Molecular Weight
59149.895 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-gated chloride ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRD
Uniprot ID
O14764
Uniprot Name
Gamma-aminobutyric acid receptor subunit delta
Molecular Weight
50707.835 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRE
Uniprot ID
P78334
Uniprot Name
Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight
57971.175 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the ute...
Gene Name
GABRP
Uniprot ID
O00591
Uniprot Name
Gamma-aminobutyric acid receptor subunit pi
Molecular Weight
50639.735 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA...
Gene Name
GABRR2
Uniprot ID
P28476
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight
54150.41 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Potentiator
General Function
Gaba-a receptor activity
Specific Function
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name
GABRR3
Uniprot ID
A8MPY1
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight
54271.1 Da
References
  1. Lahti RA, Sethy VH, Barsuhn C, Hester JB: Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine. Neuropharmacology. 1983 Nov;22(11):1277-82. [PubMed:6320036]
  2. Sethy VH, Collins RJ, Daniels EG: Determination of biological activity of adinazolam and its metabolites. J Pharm Pharmacol. 1984 Aug;36(8):546-8. [PubMed:6148400]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. Venkatakrishnan K, von Moltke LL, Duan SX, Fleishaker JC, Shader RI, Greenblatt DJ: Kinetic characterization and identification of the enzymes responsible for the hepatic biotransformation of adinazolam and N-desmethyladinazolam in man. J Pharm Pharmacol. 1998 Mar;50(3):265-74. [PubMed:9600717]
  2. 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]
  3. The P450 Program [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. Venkatakrishnan K, von Moltke LL, Duan SX, Fleishaker JC, Shader RI, Greenblatt DJ: Kinetic characterization and identification of the enzymes responsible for the hepatic biotransformation of adinazolam and N-desmethyladinazolam in man. J Pharm Pharmacol. 1998 Mar;50(3):265-74. [PubMed:9600717]
  2. 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]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:39