AM 630

Uses

AM630 has been used:

• as a cannabinoid 2(CB2) inhibitor to study the analgesic effect exerted by polysaccharopeptide from?Trametes versicolor (TPSP).
• as a CB2 antagonist along with β-caryophyllene (BCP) to study its effects on re-epithilialization of fibroblast cells.
• as a CB2 antagonist to study its interaction with 17-β-estradiol in primary human osteoblasts.

Uses

AM 630 acts as a potential CB2 receptor cannabinoid antagonist with application towards human lung cancer treatment and angiogenesis induction.

Definition

ChEBI: [6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-3-indolyl]-(4-methoxyphenyl)methanone is a N-acylindole.

Biological Activity

CB 2 antagonist/inverse agonist (K i = 31.2 nM) that displays 165-fold selectivity over CB 1 receptors. Behaves as a weak partial/inverse agonist at CB 1 receptors.

Biochem/physiol Actions

AM630 is an aminoalkylindole and acts as a competitive antagonist of CP 55,940 and WIN 55,212-2. It also behaves as a competitive antagonist of anandamide and (R)-(+)-arachidonyl-1′-hydroxy-2′-propylamide (AM356).

storage

Desiccate at +4°C

References

1. ross r a, brockie h c, stevenson l a, et al. agonist-inverse agonist characterization at cb1 and cb2 cannabinoid receptors of l759633, l759656 and am630. british journal of pharmacology, 1999, 126(3): 665-672. 2. patil m, patwardhan a, salas m m, et al. cannabinoid receptor antagonists am251 and am630 activate trpa1 in sensory neurons. neuropharmacology, 2011, 61(4): 778-788.