(S)-UH-301 ANTAGONIZES (R)-8-OH-DPAT-INDUCED CARDIOVASCULAR EFFECTS IN THE RAT

被引:18
作者
BJORK, L
LINDGREN, S
HACKSELL, U
LEWANDER, T
机构
[1] ASTRA LAKEMEDEL AB,RES CTR,S-15185 SODERTALJE,SWEDEN
[2] UNIV UPPSALA,DEPT ORGAN PHARMACEUT CHEM,S-75123 UPPSALA,SWEDEN
关键词
8-OH-DPAT (8-HYDROXY-2-(DIPROPYLAMINO)TETRALIN); UH-301; BLOOD PRESSURE; HEART RATE; 5-HT1A RECEPTOR ANTAGONISTS;
D O I
10.1016/0014-2999(91)90502-H
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The 5-HT1A-receptor antagonist (S)-UH-301 (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin) completely antagonized the hypotension and bradycardia induced by (R) = 8-OH DPAT ((R)-8-hydroxy-2-(dipropylamino)tetralin) in conscious rats. (S)-UH-301 alone induced a weak hypertension, which might be due to its 5-HT1A-receptor antagonistic properties. (R)-UH-301 induced effects similar to those of (R)-8-OH DPAT, i.e., a short initial phase of hypertension followed by a long-lasting hypotension and bradycardia. Thus, (R)-UH-301 behaves as a 5-HT1A-receptor agonist and (S)-UH-301 as a 5-HT1A-receptor antagonist, abolishing the effects induced by (R)-8-OH DPAT.
引用
收藏
页码:367 / 370
页数:4
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