256343-36-9Relevant articles and documents
4-(4-Fluorobenzoyl)-1-[2-(4-iodo-2,5-dimethoxyphenyl)ethyl]piperidine and its derivatives: Synthesis and affinity at 5-HT(2A), 5-HT(2B) and 5- HT(2C) serotonin receptors
Claudi, Francesco,Scoccia, Loredana,Giorgioni, Gianfabio,Accorroni, Beatrice,Marucci, Gabriella,Gessi, Stefania,Siniscalchi, Anna,Borea, Pier Andrea
, p. 843 - 852 (1999)
4-(4-Fluorobenzoyl)-1-[2-(4-iodo-2,5-dimethoxyphenyl)ethyl]piperidine (7) and its derivatives modified at the carbonyl group of the fluorobenzoyl moiety were prepared and evaluated for affinity at 5-HT(2A), 5-HT(2C) (rat cortex) and 5-HT(2B) (rat stomach fundus) serotonin receptors. Compound 7 bound the 5-HT(2A) sites with higher affinity (K(i) = 8.2 nM) than the 5- HT(2B) (K(b) = 1 290 nM) and 5-HT(2C) ones (K(i) = 54.2 nM). Modification of the benzoyl carbonyl group decreased the 5-HT(2A) and 5-HT(2C) affinities but did not significantly influence 5-HT(2B) affinity. This suggests that the carbonyl group is the determinant for the interaction with 5-HT(2A) and 5-HT(2C) receptor subtypes. Compound 7 was found to be a 5-HT(2A) receptor antagonist.