Bentley J M, Adams D R, Bebbington D, Benwell K R, Bickerdike M J, Davidson J E P, Dawson C E, Dourish C T, Duncton M A J, Gaur S, George A R, Giles P R, Hamlyn R J, Kennett G A, Knight A R, Malcolm C S, Mansell H L, Misra A, Monck N J T, Pratt R M, Quirk K, Roffey J R A, Vickers S P, Cliffe I A
Vernalis Research Ltd, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA, UK.
Bioorg Med Chem Lett. 2004 May 3;14(9):2367-70. doi: 10.1016/j.bmcl.2003.05.001.
A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT(2) receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.
合成了一系列1-(1-吲哚基)-2-丙胺，并作为5-HT(2C)受体激动剂进行评估，用于治疗肥胖症。描述了前体吲哚的一般合成方法。报告了所有化合物在5-HT(2)受体亚型上的功能效力和放射性配体结合数据。发现许多化合物经口服给药后可减少大鼠的食物摄入量。
