✦ LIBER ✦

(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

✍ Scribed by Tomas de Paulis; Bakula L. Trivedi; Zhang-Jin Zhang; Dennis E. Schmidt; Michael H. Ebert; William A. Hewlett

Book ID: 104364643
Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 306 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00497-0

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✦ Synopsis

TRIZAC is one of the most potent 5-HT-3 receptor antagonist reported to date, having 20-fold higher affinity than (S)-5-iodozacopride. This high affinity (Ki 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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