(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)b enzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor

DOI: 10.1016/S0960-894X(96)00497-0

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2657 - 2662 (1996)

Update date:2022-08-03

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Authors:

De Paulis, Tomas

Trivedi, Bakula L.

Zhang, Zhang-Jin

Schmidt, Dennis E.

Ebert, Michael H.

Hewlett, William A.

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Article abstract of DOI:10.1016/S0960-894X(96)00497-0

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 (K(i) 0.05 ± 0.01 nM) and a moderate apparent lipophilicity (log P(app) 2.12) makes TRIZAC a promising ligand for studying 5-HT-3 receptors.

Full text of DOI:10.1016/S0960-894X(96)00497-0

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