Imidazoline-modified benzylimidazolines as h5-HT1D/1B serotonergic ligands

被引：25
作者：
Prisinzano, T
Law, H
Dukat, M
Slassi, A
MaClean, N
Demchyshyn, L
Glennon, RA
机构：
[1] Virginia Commonwealth Univ, Sch Pharm, Dept Med Chem, Richmond, VA 23298 USA
[2] NPS Allelix Corp, Mississauga, ON, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 03期
关键词：
D O I：
10.1016/S0968-0896(00)00275-3
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Sumatriptan, a h5-HT1D and h5-HT1B receptor agonist used clinically as a migraine-abortive, produces certain side effects thought to result from its affinity for h(5)-HT1B receptors. The present investigation extends our work with benzylimidazolines as novel non-tryptamine h5-(HT1D/1B) ligands. The effect of N-methylation, N-benzylation, ring-aromatization, and variation of the imidazoline ring on affinity both at h5-HT1D and h5-HT1B receptors was examined. Several compounds were identified with good affinity and enhanced(i.e., > 100-fold) h5-HT1D versus h5-HT1B selectivity. (C) 2001 Elsevier Science Ltd. All rights reserved.
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收藏
页码：613 / 619
页数：7
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