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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 of AZD-6280

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

Molecular Formula C20H22N4O3
Molecular Weight 366.4137
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

Cmax

ValueDoseCo-administeredAnalytePopulation
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

ValueDoseCo-administeredAnalytePopulation
1686 ng × h/mL
40 mg single, oral
AZD-6280 plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
7.1 h
40 mg single, oral
AZD-6280 plasma
Homo sapiens

PubMed

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
Substance Class Chemical
Record UNII
B9Z1OEH19D
Record Status Validated (UNII)
Record Version