Delving into the Latest Updates on Compound 25r (West China Hospital) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

CB2

Action

agonists

Mechanism

CB2 agonists(Cannabinoid CB2 receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Inflammatory pain

Inactive Indication-

Originator Organization

West China Hospital

Active Organization

West China Hospital

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Selectively targeting the cannabinoid receptor CB2 is an attractive therapeutic strategy for the treatment of inflammatory pain without psychiatric side effects mediated by the cannabinoid receptor CB1. Herein, we report the discovery of 4-(1,2,4-oxadiazol-5-yl)azepan-2-one derivatives as a new class of CB2 agonists. Systematic structure-activity relationship investigations resulted in the identification of the most potent compound 25r. This compound displayed high selectivity for CB2 against CB1 (CB2 EC₅₀ = 21.0 nM, E_max = 87%, CB1 EC₅₀ > 30 μM, ratio CB1/CB2 > 1428) with favorable pharmacokinetic properties. Especially, 25r demonstrated significant efficacy in the analgesic model of rodent inflammatory pain. All the results suggest that compound 25r could serve as a lead compound for treating inflammatory pain and deserves further in-depth studies.

100 Deals associated with Compound 25r (West China Hospital)

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