864445-56-7Relevant articles and documents
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles
Huffman, John W.,Szklennik, Paul V.,Almond, Amanda,Bushell, Kristen,Selley, Dana E.,He, Hengjun,Cassidy, Michael P.,Wiley, Jenny L.,Martin, Billy R.
, p. 4110 - 4113 (2005)
A new class of cannabimimetic indoles, with 3-phenylacetyl or substituted 3-phenylacetyl substituents, has been prepared and their affinities for the cannabinoid CB1 and CB2 receptors have been determined. In general those compounds with a 2-substituted phenylacetyl group have good affinity for both receptors. The 4-substituted analogs have little affinity for either receptor, while the 3-substituted compounds are intermediate in their affinities. Two of these compounds, 1-pentyl-3-(2-methylphenylacetyl)indole (JWH-251) and 1-pentyl-3-(3-methoxyphenylacetyl)indole (JWH-302), have 5-fold selectivity for the CB1 receptor with modest affinity for the CB 2 receptor. GTPγS determinations indicate that both compounds are highly efficacious agonists at the CB1 receptor and partial agonists at the CB2 receptor.
