AI Article Synopsis
- A new class of indole compounds with 3-phenylacetyl variations has been created and tested for their binding strength to cannabinoid receptors CB1 and CB2.
- Compounds featuring a 2-substituted phenylacetyl group show strong binding affinity, while those with 4-substituents show little to no affinity, and 3-substituted compounds have moderate binding.
- Two specific compounds, JWH-251 and JWH-302, are identified as having a strong preference for the CB1 receptor and demonstrate high efficacy as agonists for that receptor, with partial agonist activity for the CB2 receptor.
Article Abstract
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 CB2 receptor. GTPgammaS determinations indicate that both compounds are highly efficacious agonists at the CB1 receptor and partial agonists at the CB2 receptor.
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| http://dx.doi.org/10.1016/j.bmcl.2005.06.008 | DOI Listing |
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