40995-78-6Relevant academic research and scientific papers
5-Methyl-1-(3-pyridylcarbamoyl)-1,2,3,5-tetrahydropyrroloindole: A Novel 5-HT2C/5-HT2B Receptor Antagonist with Improved Affinity, Selectivity, and Oral Activity
Forbes, Ian T.,Ham, Peter,Booth, Deborah H.,Martin, Roger T.,Thompson, Mervyn,et al.
, p. 2524 - 2530 (1995)
The preparation of a series of conformationally restricted analogues of indolylurea 1, namely tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described.The binding affinities of these compounds at 5-HT2A, 5-HT2B, and 5-HT2C receptors were determined.Of these compounds, the 1,2,3,5-tetrahydropyrroloindole derivative, compound 11, was found to have high affinity for the 5-HT2C (pK1 8.0) and 5-HT2B receptors (pA2 8.5), with excellent selectivity over the 5-HT2A and various other receptors (pK1B 8.8), and an in vivo functional model, mCPP-induced hypolocomotion (ID50 5.5 mg/kg po). 11 should therefore be of significant utility as a pharmacological tool to delineate the functional significance of blockade of 5-HT2B and 5-HT2C receptors.
