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Bioorg Med Chem Lett. 2013 Nov 1;23(21):5945-8. doi: 10.1016/j.bmcl.2013.08.072. Epub 2013 Aug 24.

2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.

Author information

1
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-540, USA. Electronic address: mdukat@vcu.edu.

Abstract

2-Amino-6-chloro-3,4-dihydroquinazoline HCl (A6CDQ, 4) binds at 5-HT3 serotonin receptors and displays antidepressant-like action in the mouse tail suspension test (TST). Empirically, 4 was demonstrated to be a 5-HT3 receptor antagonist (two-electrode voltage clamp recordings using frog oocytes; IC50=0.26μM), and one that should readily penetrate the blood-brain barrier (logP=1.86). 5-HT3 receptor antagonists represent a potential approach to the development of new antidepressants, and 4 is an example of a structurally novel 5-HT3 receptor antagonist that is active in a preclinical antidepressant model (i.e., the mouse TST).

KEYWORDS:

5-HT(3) receptors; Antagonists; Antidepressants; TST (tail suspension test)

PMID:
24035337
DOI:
10.1016/j.bmcl.2013.08.072
[Indexed for MEDLINE]
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