Bioorganic & Medicinal Chemistry Letters 1998-12-01

Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.

M Perez, P J Pauwels, I Pallard-Sigogneau, C Fourrier, P Chopin, C Palmier, V Colovray, S Halazy

Index: Bioorg. Med. Chem. Lett. 8(23) , 3423-8, (1998)

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Abstract

Hybrid molecules built up by covalent coupling of aminopropanol derivatives (especially pindolol) with antidepressant drugs like fluoxetine, paroxetine or milnacipran were found to be potent and silent 5-HT1A antagonists (KB < 1 nM for 7c and 9a).