Adinazolam - CAS 37115-32-5
Catalog number:
37115-32-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H18ClN5
Molecular Weight:
351.839
COA:
Inquire
Targets:
5-HT Receptor
Description:
Adinazolam, a triazolobenzodiazepine, a high affinity for β-adrenoceptors (Kd = 0.061 nM) and alters the expression of serotonin 5-HT2 receptors in rat fronto-parietal hemicortex.
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Purity:
≥98%
Appearance:
A neat solid
Synonyms:
8-chloro-N,N-dimethyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-1-methanamine;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A high affinity for β-adrenoceptor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
Boiling Point:
527ºC at 760 mmHg
Density:
1.31g/cm3
InChIKey:
GJSLOMWRLALDCT-UHFFFAOYSA-N
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
Canonical SMILES:
CN(C)CC1=NN=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4
1.Prediction of modified release pharmacokinetics and pharmacodynamics from in vitro, immediate release, and intravenous data.
Lukacova V1, Woltosz WS, Bolger MB. AAPS J. 2009 Jun;11(2):323-34. doi: 10.1208/s12248-009-9107-2. Epub 2009 May 9.
The aim of this study was to demonstrate the value of mechanistic simulations in gaining insight into the behaviors of modified release (MR) formulations in vivo and to use the properly calibrated models for prediction of pharmacokinetics (PK) and pharmacodynamics (PD). GastroPlus (Simulations Plus, Inc.) was used to fit mechanistic models for adinazolam and metoprolol that describe the absorption, PK, and PD after intravenous (i.v.) and immediate release (IR) oral (p.o.) administration. The fitted model for adinazolam was then used to predict the PD profile for a MR formulation and to design a new formulation with desired onset and duration of action. The fitted metoprolol model was used to gain insight and to explain the in vivo behaviors of MR formulations. For each drug, a single absorption/PK model was fitted that provided simulated plasma concentration-time profiles closely matching observed in vivo profiles across several different i.
2.Kinetic characterization and identification of the enzymes responsible for the hepatic biotransformation of adinazolam and N-desmethyladinazolam in man.
Venkatakrishnan K1, von Moltke LL, Duan SX, Fleishaker JC, Shader RI, Greenblatt DJ. J Pharm Pharmacol. 1998 Mar;50(3):265-74.
The kinetics of the N-demethylation of adinazolam to N-desmethyladinazolam (NDMAD), and of NDMAD to didesmethyladinazolam (DDMAD), were studied with human liver microsomes using substrate concentrations in the range 10-1000 microM. The specific cytochrome P450 (CYP) isoforms mediating the biotransformations were identified using microsomes containing specific recombinant CYP isozymes expressed in human lymphoblastoid cells, and by the use of CYP isoform-selective chemical inhibitors. Adinazolam was demethylated by human liver microsomes to NDMAD, and NDMAD was demethylated to DDMAD; the substrate concentrations, Km, at which the reaction velocities were 50% of the maximum were 92 and 259 microM, respectively. Another metabolite of yet undetermined identity (U) was also formed from NDMAD (Km 498 microM). Adinazolam was demethylated by cDNA-expressed CYP 2C19 (Km 39 microM) and CYP 3A4 (Km 83 microM); no detectable activity was observed for CYPs 1A2, 2C9, 2D6 and 2E1.
3.Application of the Stages of Change Scale in a clinical drug trial.
Wilson M1, Bell-Dolan D, Beitman B. J Anxiety Disord. 1997 Jul-Aug;11(4):395-408.
The Stages of Change Scale (SOC: McConnaughy, Prochaska, & Velicer, 1983) was used to predict outcome among 131 outpatients with generalized anxiety disorder who were enrolled in a clinical drug trial. As predicted, subjects high on Precontemplation did not experience as much relief from anxiety as subjects low on Precontemplation, whereas subjects high on Contemplation or Action experienced more decrease in anxiety during the trial than subjects low on these stages. Contrary to our hypothesis, only Contemplation was related to illness severity changes, and scores on the Maintenance scale were not related to outcome. Of the four stage scores, only Maintenance was related to premature termination of treatment. There were no differences between drug (adinazolam) and placebo groups and only Action scores interacted with drug/placebo assignment in this study. Results suggest that the SOC may be useful in identifying individuals who are most likely to experience decreased anxiety while enrolled in a clinical drug trial.
4.Evaluation of a basic physiologically based pharmacokinetic model for simulating the first-time-in-animal study.
Germani M1, Crivori P, Rocchetti M, Burton PS, Wilson AG, Smith ME, Poggesi I. Eur J Pharm Sci. 2007 Jul;31(3-4):190-201. Epub 2007 Mar 24.
The objective of this study was to evaluate a physiologically based pharmacokinetic (PBPK) approach for predicting the plasma concentration-time curves expected after intravenous administration of candidate drugs to rodents. The predictions were based on a small number of properties that were either calculated based on the structure of the candidate drug (octanol:water partition coefficient, ionization constant(s)) or obtained from the typical high-throughput screens implemented in the early drug discovery phases (fraction unbound in plasma and hepatic intrinsic clearance). The model was tested comparing the predicted and the observed pharmacokinetics of 45 molecules. This dataset included six known drugs and 39 drug candidates from different discovery programs, so that the performance of the model could be evaluated in a real discovery case scenario. The plasma concentration-time curves were predicted with good accuracy, the pharmacokinetic parameters being on average two- to three-fold of actual values.
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CAS 37115-32-5 Adinazolam

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