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Identification
NameAdinazolam
Accession NumberDB00546  (APRD00724)
TypeSmall Molecule
GroupsApproved
DescriptionAdinazolam (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
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DeracynUpjohn
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIKN08449444
CAS number37115-32-5
WeightAverage: 351.833
Monoisotopic: 351.125073308
Chemical FormulaC19H18ClN5
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub Class1,4-benzodiazepines
Direct Parent1,4-benzodiazepines
Alternative Parents
Substituents
  • 1,4-benzodiazepine
  • Phenyl-1,3,4-triazole
  • Phenyl-1,2,4-triazole
  • Phenyltriazole
  • Aralkylamine
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Triazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketimine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of anxiety and status epilepticus.
PharmacodynamicsAdinazolam 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 actionAdinazolam 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.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

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

SubstrateEnzymesProduct
Adinazolam
desmethyladinazolamDetails
Adinazolam
Not Available
EstazolamDetails
Adinazolam
Not Available
alpha-HydroxyalprazolamDetails
Route of eliminationNot Available
Half lifeLess than 3 hours.
ClearanceNot Available
ToxicitySigns 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
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
References
Synthesis ReferenceNot Available
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
ATC CodesN05BA07
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe metabolism of Adinazolam can be decreased when combined with Abiraterone.
AmiodaroneThe metabolism of Adinazolam can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Adinazolam can be increased when it is combined with Aprepitant.
ArmodafinilThe metabolism of Adinazolam can be decreased when combined with Armodafinil.
AtazanavirThe metabolism of Adinazolam can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Adinazolam can be decreased when combined with Atomoxetine.
BexaroteneThe serum concentration of Adinazolam can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Adinazolam can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Adinazolam can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Adinazolam can be decreased when it is combined with Bosentan.
CarbamazepineThe metabolism of Adinazolam can be increased when combined with Carbamazepine.
CeritinibThe serum concentration of Adinazolam can be increased when it is combined with Ceritinib.
ChloramphenicolThe metabolism of Adinazolam can be decreased when combined with Chloramphenicol.
CholecalciferolThe metabolism of Adinazolam can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Adinazolam can be decreased when combined with Cimetidine.
CitalopramThe metabolism of Adinazolam can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Adinazolam can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Adinazolam can be decreased when combined with Clemastine.
ClotrimazoleThe metabolism of Adinazolam can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Adinazolam can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Adinazolam can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Adinazolam can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Adinazolam can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Adinazolam can be decreased when it is combined with Dabrafenib.
DarunavirThe metabolism of Adinazolam can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Adinazolam can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Adinazolam can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Adinazolam can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Adinazolam can be decreased when it is combined with Dexamethasone.
DihydroergotamineThe metabolism of Adinazolam can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Adinazolam can be decreased when combined with Diltiazem.
DoxycyclineThe metabolism of Adinazolam can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Adinazolam can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Adinazolam can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Adinazolam can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Adinazolam can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Adinazolam can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe metabolism of Adinazolam can be decreased when combined with Esomeprazole.
EtravirineThe serum concentration of Adinazolam can be decreased when it is combined with Etravirine.
FluconazoleThe metabolism of Adinazolam can be decreased when combined with Fluconazole.
FluoxetineThe metabolism of Adinazolam can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Adinazolam can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Adinazolam can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Adinazolam can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Adinazolam can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Adinazolam can be increased when it is combined with Fusidic Acid.
GemfibrozilThe metabolism of Adinazolam can be decreased when combined with Gemfibrozil.
IdelalisibThe serum concentration of Adinazolam can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Adinazolam can be decreased when combined with Imatinib.
IndinavirThe metabolism of Adinazolam can be decreased when combined with Indinavir.
IsavuconazoniumThe metabolism of Adinazolam can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Adinazolam can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Adinazolam can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Adinazolam can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Adinazolam can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Adinazolam can be decreased when combined with Ketoconazole.
LopinavirThe metabolism of Adinazolam can be decreased when combined with Lopinavir.
LovastatinThe metabolism of Adinazolam can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Adinazolam can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Adinazolam can be decreased when it is combined with Lumacaftor.
MifepristoneThe metabolism of Adinazolam can be decreased when combined with Mifepristone.
MitotaneThe serum concentration of Adinazolam can be decreased when it is combined with Mitotane.
MoclobemideThe metabolism of Adinazolam can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Adinazolam can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Adinazolam can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Adinazolam can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Adinazolam can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Adinazolam can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Adinazolam can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Adinazolam can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Adinazolam can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Adinazolam can be decreased when combined with Olaparib.
OmeprazoleThe metabolism of Adinazolam can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Adinazolam can be increased when it is combined with Osimertinib.
PalbociclibThe serum concentration of Adinazolam can be increased when it is combined with Palbociclib.
PantoprazoleThe metabolism of Adinazolam can be decreased when combined with Pantoprazole.
PentobarbitalThe metabolism of Adinazolam can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Adinazolam can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Adinazolam can be increased when combined with Phenytoin.
PosaconazoleThe metabolism of Adinazolam can be decreased when combined with Posaconazole.
PrimidoneThe metabolism of Adinazolam can be increased when combined with Primidone.
RanolazineThe metabolism of Adinazolam can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Adinazolam can be increased when combined with Rifabutin.
RifampicinThe metabolism of Adinazolam can be increased when combined with Rifampicin.
RifapentineThe metabolism of Adinazolam can be increased when combined with Rifapentine.
RitonavirThe metabolism of Adinazolam can be decreased when combined with Ritonavir.
SaquinavirThe metabolism of Adinazolam can be decreased when combined with Saquinavir.
SertralineThe metabolism of Adinazolam can be decreased when combined with Sertraline.
SildenafilThe metabolism of Adinazolam can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Adinazolam can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Adinazolam can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Adinazolam can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Adinazolam can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Adinazolam can be decreased when combined with Sulfisoxazole.
TelaprevirThe metabolism of Adinazolam can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Adinazolam can be decreased when combined with Telithromycin.
TiclopidineThe metabolism of Adinazolam can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Adinazolam can be decreased when it is combined with Tocilizumab.
TopiramateThe metabolism of Adinazolam can be decreased when combined with Topiramate.
TranylcypromineThe metabolism of Adinazolam can be decreased when combined with Tranylcypromine.
VenlafaxineThe metabolism of Adinazolam can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Adinazolam can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Adinazolam can be decreased when combined with Voriconazole.
YohimbineThe therapeutic efficacy of Adinazolam can be decreased when used in combination with Yohimbine.
ZiprasidoneThe metabolism of Adinazolam can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
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
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
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
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
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRG2
Uniprot ID:
P18507
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
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRB1
Uniprot ID:
P18505
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB2
Uniprot ID:
P47870
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB3
Uniprot ID:
P28472
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
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
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 uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to ...
Gene Name:
GABRP
Uniprot ID:
O00591
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 receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR1
Uniprot ID:
P24046
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 receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR2
Uniprot ID:
P28476
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
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
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 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. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23