(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

Autor:	B. L. Trivedi, William A. Hewlett, Dennis E. Schmidt, Michael H. Ebert, Tomas de Paulis, Zhang-Jin Zhang
Rok vydání:	1996
Předmět:	Chemistry Stereochemistry medicine.drug_class Organic Chemistry Clinical Biochemistry Pharmaceutical Science Ligand (biochemistry) Receptor antagonist Biochemistry chemistry.chemical_compound Drug Discovery Lipophilicity medicine Molecular Medicine Benzamide Receptor Molecular Biology 5-HT receptor
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 6:2657-2662
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(96)00497-0
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::aaf0d6b2a60d313289f6b6244bda0023 https://doi.org/10.1016/s0960-894x(96)00497-0 Zobrazit plný text záznamu Full Text from ScienceDirect