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Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.
Authors:J Ignacio Andrés  Jesús Alcázar  José M Alonso  Adolfo Díaz  Javier Fernández  Pilar Gil  Laura Iturrino  Encarna Matesanz  Theo F Meert  Anton Megens  Victor K Sipido
Institution:Janssen-Cilag, Basic Research Centre, Jarama s/n, 45007 Toledo, Spain. jandres@jaces.jnj.com
Abstract:Following the programme started at Janssen Research Foundation searching for 5-HT(2A/2C) antagonists, we now report on the synthesis of a series of substituted 2-(Dimethylaminomethyl)-2,3,3a,8-tetrahydrodibenzoc,f]isoxazolo2,3-a]azepine derivatives. The 5-HT(2A), 5-HT(2C) and H(1) receptor affinities as well as the mCPP antagonistic activity of the compounds synthesised is described.
Keywords:
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