A CB2 receptor agonist; selective for the CB2 over the CB1 receptor (Kis = 658 and >10

(S)-AM1241 – 1 mg

Brand:
Cayman
CAS:
444912-53-2
Storage:
-20
UN-No:
Non-Hazardous - 1648 / 3

(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).{18107} (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 (Item No. 10010118), (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats.{18108} The pain-reducing effect of (S)-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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SKU: 10490 - 1 mg Category:

Description

A CB2 receptor agonist; selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively); 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); produces antinociception to thermal, but not mechanical, pain in rats

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

Synonyms:  (−)-AM1241

Molecular weight: 503.3

CAS: 444912-53-2

Purity: ≥98%

Formulation: A solution in acetonitrile

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Pain Research

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