rimonabant

Rimonabant (SR141716) 是一种选择性的、能透过血脑屏障的中心大麻素受体 1 拮抗剂， Ki 值为 1.8 nM。它也能够抑制分枝杆菌膜蛋白 3。

Rimonabant hydrochloride (SR 141716A) 是中心大麻素受体 1 的高效选择性反向激动剂， Ki 值为1.8 nM。它也能够抑制分枝杆菌膜蛋白3。

N-Aminopiperidine hydrochloride (Piperidin-1-amine hydrochloride) 是大麻素受体 1 拮抗剂 Rimonabant（一种抗肥胖剂）的代谢物(M1)。

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

(R)-AM1241 binds to cannabinoid (CB) receptors and has greater than 100-fold selectivity for the CB2 over the CB1 receptor (Kis = 15 and 5,000 nM, respectively, in a membrane assay using human receptors). (R)-AM1241 acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively). Similar to the racemate AM1241 , (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (R)-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 .

(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 inhibitor of the CB1 receptor, exhibiting an IC50 value of 0.644 μM. This compound possesses the ability to penetrate the blood-brain barrier and has the potential to induce central nervous system (CNS) side effects similar to Rimonabant [1].