TY - JOUR
T1 - 2-Amino-6-chloro-3,4-dihydroquinazoline
T2 - A novel 5-HT3 receptor antagonist with antidepressant character
AU - Dukat, Małgorzata
AU - Alix, Katie
AU - Worsham, Jessica
AU - Khatri, Shailesh
AU - Schulte, Marvin K.
PY - 2013/11/1
Y1 - 2013/11/1
N2 - 2-Amino-6-chloro-3,4-dihydroquinazoline HCl (A6CDQ, 4) binds at 5-HT 3 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 = 0.26 μM), and one that should readily penetrate the blood-brain barrier (log P = 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).
AB - 2-Amino-6-chloro-3,4-dihydroquinazoline HCl (A6CDQ, 4) binds at 5-HT 3 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 = 0.26 μM), and one that should readily penetrate the blood-brain barrier (log P = 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).
KW - 5-HT receptors
KW - Antagonists
KW - Antidepressants
KW - TST (tail suspension test)
UR - http://www.scopus.com/inward/record.url?scp=84885176023&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2013.08.072
DO - 10.1016/j.bmcl.2013.08.072
M3 - Article
C2 - 24035337
AN - SCOPUS:84885176023
SN - 0960-894X
VL - 23
SP - 5945
EP - 5948
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 21
ER -