Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-540, USA.
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 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).
2-氨基-6-氯-3,4-二氢喹唑啉盐酸盐（A6CDQ，4）与 5-羟色胺 3 型（5-HT3）受体结合，并在小鼠悬尾试验（TST）中显示出抗抑郁作用。经验表明，4 是一种 5-HT3 受体拮抗剂（使用青蛙卵母细胞的双电极电压钳记录；IC50=0.26μM），并且很容易穿透血脑屏障（logP=1.86）。5-HT3 受体拮抗剂是开发新型抗抑郁药的一种潜在方法，而 4 是一种结构新颖的 5-HT3 受体拮抗剂，在临床前抗抑郁模型（即小鼠 TST）中具有活性。
