Correlation Engine 2.0
Clear Search sequence regions

Sizes of these terms reflect their relevance to your search.

Partial agonists of peripheral cannabinoid receptors (CBRs) have potential therapeutic applications in several medical conditions. However, (-)-trans-Δ9-tetrahydrocannabinol (THC), the principal active component of marijuana, which is a partial agonist of CB1 and CB2 penetrates the central nervous system (CNS) and produces adverse effects. Peripherally restricted partial agonists of CBRs, particularly of CB1, can be used to treat illnesses safely and effectively with a better therapeutic index. Here, we report on our efforts to synthesize pyrazole partial CBR agonists with peripheral selectivity, resulting in lead compound 40. This compound is a potent partial agonist of CB1 with ∼ 5-fold higher plasma biodistribution over brain and represents an early lead for optimization. Copyright © 2023 Elsevier Ltd. All rights reserved.


George Amato, Scott Runyon, Vineetha Vasukuttan, Ann M Decker, Elaine A Gay, Lucas Laudermilk, Rangan Maitra. Discovery of 1,3-disubstituted pyrazole peripheral cannabinoid receptor partial agonists. Bioorganic & medicinal chemistry letters. 2023 Sep 01;93:129430

Expand section icon Mesh Tags

Expand section icon Substances

PMID: 37543275

View Full Text