266352-94-7Relevant academic research and scientific papers
Butyrophenone analogues in the carbazole series as potential atypical antipsychotics: Synthesis and determination of affinities at D2, 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors
Masaguer, Christian F.,Ravina, Enrique,Fontenla, Jose Angel,Brea, Jose,Tristan, Helena,Loza, Maria Isabel
, p. 83 - 95 (2007/10/03)
We describe practical and efficient routes for synthesis of 2- aminomethyl-1,2,3,9-tetrahydro-4H-carbazol-4-ones using the Fischer indole synthesis or palladium-catalysed cyclization methodologies, as well as their affinities for D2, 5-HT(2A) and 5-HT(2C) receptors, and their activity at the 5-HT(2B) receptor. The most active compounds, 4b (QF 2003B) and 4c (QF 2004B), with a pK(i) (5-HT(2A)/D2) ratio of 1.28 show a potential antipsychotic profile according to Meltzer's classification. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
