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

Structure Search

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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25493397 | https://adisinsight.springer.com/drugs/800027607

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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
77.23 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
248.9 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
676.82 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
728.67 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
731.4 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
676.82 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1247.21 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1495.56 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
439.39 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1514.66 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/28013354/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
328 ng/mL EXPERIMENT https://scholarlypublications.universiteitleiden.nl/access/item%3A2947570/download#page=68	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
1686 ng × h/mL EXPERIMENT https://scholarlypublications.universiteitleiden.nl/access/item%3A2947570/download#page=68	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:		AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.1 h EXPERIMENT https://scholarlypublications.universiteitleiden.nl/access/item%3A2947570/download#page=68	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:		AZD-6280 plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FED

PubMed

Title	Date	PubMed
Absorption, excretion, and metabolism of a potential GABA-A α2/3 receptor modulator in rats.	2011-05	21210737

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

Name

Type

Language

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

Preferred Name

English

AZD-6280

Common Name

English

AZD6280

Code

English

Code System Code Type Description

EPA CompTox

DTXSID60915944