rimonabant

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

N-Aminopiperidine hydrochloride (Piperidin-1-amine hydrochloride) is a metabolite (M1) of the canabinoid receptor 1 antagonist Rimonabant, an antiobesity agent.

AM6538, a long-acting, high-affinity, and pseudo-irreversible cannabinoid antagonist structurally analogous to rimonabant, is a valuable tool for assessing the apparent efficacy of cannabinoid partial and full agonists. It also holds potential for future investigations requiring temporary reductions in cannabinoid receptor availability[1].

(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (S)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

CB1-IN-2 (Compound 4g) is a potent and selective CB1 receptor inhibitor with an IC50 value of 0.644 μM. It can penetrate the blood-brain barrier and may induce central nervous system (CNS) side effects similar to Rimonabant [1].