(−)-5-Methyl-8-hydroxy-(di-n-propylamino) tetralin: A new 5-HT 1A receptor antagonist

…, M Mathé-Allainmat, B Brémont, I Malagié…

Index: Trillat, Anne-Cecile; Mathe-Allainmat, Monique; Bremont, Beatrice; Malagie, Isabelle; Jacquot, Christian; Gardier, Alain M.; Langlois, Michel European Journal of Medicinal Chemistry, 1998 , vol. 33, # 6 p. 437 - 444

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Citation Number: 5

Abstract

−(±)-5-Me-8-OH-DPAT 4 was synthesized by a new synthetic pathway recently described by us. The (+)-and (−)-enantiomers 4 were prepared from the primary amine 8 by crystallisation of the (+)-and (−)-mandelic acid salts. The enantiomers reacted with propyl iodide and were demethylated by 48% HBr to the (+)-and (−)-4 compounds. These compounds had good affinity for 5-HT1A receptors (Ki= 32.9±0.8 and 45.6±2 nM, respectively) but lacked ...

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