2-(1-Naphthyloxy) ethylamines with Enhanced Affinity for Human 5-HT1Dβ (h5-HT1B) Serotonin Receptors

…, L Mazzocco, D Buekschkens, M Teitler…

Index: Ismaiel; Dukat; Law; Kamboj; Fan; Lee; Mazzocco; Buekschkens; Teitler; Pierson; Glennon Journal of Medicinal Chemistry, 1997 , vol. 40, # 26 p. 4415 - 4419

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Citation Number: 14

Abstract

Although the β-adrenergic antagonist propranolol (1) binds at rodent 5-HT1B serotonin receptors, it displays low affinity (K i> 10 000 nM) for its species homologue 5-HT1Dβ (ie, h5- HT1B) receptors. The structure of propranolol was systematically modified in an attempt to enhance its affinity for the latter population of receptors. Removal of the alkyl hydroxyl group, shortening of the O-alkyl chain from three to two methylene groups, and variation of the ...