Chromenopyrazoles: non-psychoactive and selective CB₁ cannabinoid agonists with peripheral antinociceptive properties.

ABSTRACT: The unwanted psychoactive effects of cannabinoid receptor agonists have limited their development as medicines. These CB₁-mediated side effects are due to the fact that CB₁ receptors are largely expressed in the central nervous system (CNS). As it is known that CB₁ receptors are also located peripherally, there is growing interest in targeting cannabinoid receptors located outside the brain. A library of chromenopyrazoles designed analogously to the classical cannabinoid cannabinol were synthesized, characterized, and tested for cannabinoid activity. Radioligand binding assays were used to determine their affinities at CB₁ and CB₂ receptors. Structural features required for CB₁/CB₂ affinity and selectivity were explored by molecular modeling. Some compounds in the chromenopyrazole series w

SUBMITTER: Cumella J 

PROVIDER: S-EPMC4049093 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature