A-796260

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H30N2O2
Molecular Weight	354.4858
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1(C)C(C(=O)C2=CN(CCN3CCOCC3)C4=C2C=CC=C4)C1(C)C

InChI

InChIKey=ZCFHOMLAFTWDFM-UHFFFAOYSA-N

InChI=1S/C22H30N2O2/c1-21(2)20(22(21,3)4)19(25)17-15-24(18-8-6-5-7-16(17)18)10-9-23-11-13-26-14-12-23/h5-8,15,20H,9-14H2,1-4H3

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Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17994110

A-796260 is a compound that acts as a potent and selective cannabinoid CB2 receptor agonist. The analgesic effects of A-796260 on activity-induced pain behavior were evaluated in a rat model, the results demonstrated that A-796260 may be a useful new pharmacological compound for further studying CB2 receptor pharmacology and for evaluating its role in the modulation of pain.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cannabinoid receptor 2 27 Target ID: P34972 Gene ID: 1269.0 Gene Symbol: CNR2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19921781	Agonist 2678		0.77 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Unknown 2578

PubMed

Title	Date	PubMed
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.	2010 Jan 14	19921781

Patents

Sample Use Guides

In Vivo Use Guide

Neuropathic pain model in rats: The analgesic effects of A-796260 on activity-induced pain behaviour were evaluated in a rat model of sodium monoiodoacetate (MIA)-induced osteoarthritic (OA) joint pain, observed 20 days following the i.a. injection of MIA. A-796260 demonstrated dose-related (3.5-35 mg/kg) reversal of activity-induced pain behaviour in osteoarthritic (OA) rats with effects comparable to celecoxib (38 mg kg−1 i.p.), a clinically relevant analgesic for OA pain.

Route of Administration: Intraperitoneal

In Vitro Use Guide

The receptor-binding potencies of A-796260 was determined in [3H]-CP 55,940 competition binding assays performed with membrane preparations generated from recombinant cell lines expressing the human CB1, human CB2, rat CB1 or rat CB2 receptors. A-796260 exhibited high binding potencies at both human and rat CB2 receptors with Ki values of 4.37 and 13.0 nM, respectively

Name

Type

Language

A-796260

Common Name

English

METHANONE, (1-(2-(4-MORPHOLINYL)ETHYL)-1H-INDOL-3-YL)(2,2,3,3-TETRAMETHYLCYCLOPROPYL)-

Systematic Name

English

A796,260

Code

English

Code System Code Type Description

EPA CompTox

DTXSID80101010