(R)-AM1241

(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 (Cay-10010118), (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 (Cay-9000491) but not by either the CB1-selective inhibitor rimonabant (Cay-9000484) or the opioid receptor blocker naloxone (Cay-15594, Cay-ISO60191).Formal Name: (2-iodo-5-nitrophenyl)[1-[[(2R)-1-methyl-2-piperidinyl]methyl]-1H-indol-3-yl]methanone. CAS Number: 444912-51-0. Synonyms: (+)-AM1241. Molecular Formula: C22H22IN3O3. Formula Weight: 503.3. Purity: >98%. Formulation: (Request formulation change), A solution in acetonitrile. Solubility: DMF: 25 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 10 mg/ml, Ethanol: 5 mg/ml. lambdamax: 251, 310 nm. SMILES: O=C(C1=CC([N+]([O-])=O)=CC=C1I)C2=CN(C[C@H]3CCCCN3C)C4=CC=CC=C42. InChi Code: InChI=1S/C22H22IN3O3/c1-24-11-5-4-6-16(24)13-25-14-19(17-7-2-3-8-21(17)25)22(27)18-12-15(26(28)29)9-10-20(18)23/h2-3,7-10,12,14,16H,4-6,11,13H2,1H3/t16-/m1/s1. InChi Key: ZUHIXXCLLBMBDW-MRXNPFEDSA-N.