(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo [2.2. 2] oct-3-yl) benzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor

T de Paulis, BL Trivedi, ZJ Zhang, DE Schmidt…

Index: De Paulis, Tomas; Trivedi, Bakula L.; Zhang, Zhang-Jin; Schmidt, Dennis E.; Ebert, Michael H.; Hewlett, William A. Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 22 p. 2657 - 2662

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Citation Number: 5

Abstract

TRIZAC is one of the most potent 5-HT-3 receptor antagonist reported to date, having 20-fold higher affinity than (S)-5-todozacopride. This high affinity (K1 0.05±0.01 nM) and a moderate apparent lipophilicity (log Papp 2.12) makes TRIZAC a promising ligand for studying 5-HT-3 receptors.

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