A CB2 receptor agonist and inverse agonist; greater than 100-fold selective for the CB2 (Ki = 15 nM) over the CB1 receptor (Ki = 5

(R)-AM1241 – 10 mg

Brand:
Cayman
CAS:
444912-51-0
Storage:
-20
UN-No:
De Minimis - 1648 / 3

(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).{18107} (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 (Item No. 10010118), (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats.{18108} The pain-reducing effect of (R)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 (Item No. 9000491) but not by either the CB1-selective inhibitor rimonabant (Item No. 9000484) or the opioid receptor blocker naloxone (Item No. 15594 | ISO60191).  

 

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Description

A CB2 receptor agonist and inverse agonist; greater than 100-fold selective for the CB2 (Ki = 15 nM) over the CB1 receptor (Ki = 5,000 nM); acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist of rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively); produces antinociception to thermal, but not mechanical, pain in rats

Formal name: (2-iodo-5-nitrophenyl)[1-[[(2R)-1-methyl-2-piperidinyl]methyl]-1H-indol-3-yl]methanone

Synonyms:  (+)-AM1241

Molecular weight: 503.3

CAS: 444912-51-0

Purity: ≥98%

Formulation: A solution in acetonitrile

Application||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Pain Research

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