Canna~Fangled Abstracts

Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome.

By December 3, 2014No Comments
2014 Dec 3. pii: S0960-894X(14)01257-8. doi: 10.1016/j.bmcl.2014.11.062. [Epub ahead of print]

pm1Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome.

Iwata Y1, Ando K2, Taniguchi K2, Koba N2, Sugiura A2, Sudo M2.

Author information

Abstract

Herein we report the identification of a highly potent and selective CB2 agonist, RQ-00202730 (40), obtained by lead optimization of the benzimidazole scaffold. Compound 40 showed strong agonistic activity with an EC50 of 19nM and excellent selectivity (>1300-fold) over the CB1 receptor. Compound 40 displayed a dose dependent analgesic effect on TNBS-induced visceral hypersensitivity in rats by oral administration (ED500.66mg/kg at 2.5h after oral administration). In addition, 40 did not show a significant effect on body temperature in rats after oral administration at 300mg/kg. These findings suggest that highly selective CB2 agonists will be effective agents for IBS therapy.
Copyright © 2014 Elsevier Ltd. All rights reserved.

KEYWORDS:

Benzimidazole; CB2 agonist; Cannabinoid receptor; Irritable bowel syndrome

PMID:

 25499880
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