AZD-6280

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H22N4O3
Molecular Weight	366.4137
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCCNC(=O)C1=NN=C2C(=CC=CC2=C1N)C3=CC(OC)=CC=C3OC

InChI

InChIKey=NVWCZRPXYVDQEE-UHFFFAOYSA-N

InChI=1S/C20H22N4O3/c1-4-10-22-20(25)19-17(21)14-7-5-6-13(18(14)23-24-19)15-11-12(26-2)8-9-16(15)27-3/h5-9,11H,4,10H2,1-3H3,(H2,21,23)(H,22,25)

HIDE SMILES / InChI

Description

AZD6280 was invented by AstraZeneca as a selective gamma-aminobutyric acid A receptor modulator with higher efficacy at the α2,3 subtypes (GABA-A(α2/3)). This drug participated in trials phase I for the treatment of generalized anxiety disorders, but AstraZeneca discontinued development of AZD 6280.

Originator

Approval Year

C_max

Value	Dose	Analyte	Population
179.03 nM	5 mg single, oral	AZD-6280 plasma	Homo sapiens
77.23 nM	5 mg single, oral	AZD-6280 plasma	Homo sapiens
248.9 nM	12 mg single, oral	AZD-6280 plasma	Homo sapiens
676.82 nM	20 mg single, oral	AZD-6280 plasma	Homo sapiens
728.67 nM	30 mg single, oral	AZD-6280 plasma	Homo sapiens
731.4 nM	30 mg single, oral	AZD-6280 plasma	Homo sapiens
676.82 nM	40 mg single, oral	AZD-6280 plasma	Homo sapiens
1247.21 nM	40 mg single, oral	AZD-6280 plasma	Homo sapiens
1495.56 nM	40 mg single, oral	AZD-6280 plasma	Homo sapiens
439.39 nM	40 mg single, oral	AZD-6280 plasma	Homo sapiens
1514.66 nM	40 mg single, oral	AZD-6280 plasma	Homo sapiens
328 ng/mL	40 mg single, oral	AZD-6280 plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
1686 ng × h/mL	40 mg single, oral		AZD-6280 plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.1 h	40 mg single, oral		AZD-6280 plasma	Homo sapiens

PubMed

Show entries

Title	Date	PubMed
Absorption, excretion, and metabolism of a potential GABA-A α2/3 receptor modulator in rats.	2011 May	21210737

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Patents

Sample Use Guides

In Vivo Use Guide

Single dose of oral solution or capsule(s). 3 times for the 2 subjects in Panel 1. Once for the 6 remaining subjects

Route of Administration: Oral

Show entries

Name

Type

Language

AZD-6280

Common Name

English

3-CINNOLINECARBOXAMIDE, 4-AMINO-8-(2,5-DIMETHOXYPHENYL)-N-PROPYL-

Systematic Name

English

AZD6280

Code

English

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Code System

Code

Type

Description

EPA CompTox

DTXSID60915944

PRIMARY

FDA UNII

B9Z1OEH19D

PRIMARY

PUBCHEM

23630026

PRIMARY

CAS

942436-93-3

PRIMARY

ChEMBL

CHEMBL1783256

PRIMARY

Showing 1 to 5 of 6 entries

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ACTIVE MOIETY


					B9Z1OEH19D

AZD-6280

SMILES

InChI

Originator

Approval Year

Cmax

AUC

T1/2

PubMed

Patents

Sample Use Guides

C_max

T_1/2