URAPIDIL INHIBITS 5-HYDROXYTRYPTAMINE INDUCED PLATELET-AGGREGATION AND C-14 5-HYDROXYTRYPTAMINE UPTAKE IN PLATELETS

被引:3
作者
STORCK, J [1 ]
KIRSTEN, R [1 ]
机构
[1] UNIV FRANKFURT, INST KLIN PHARMAKOL, THEODOR STERN KAI 7, W-6000 FRANKFURT 70, GERMANY
关键词
5-Hydroxytryptamine; Platelet Aggregation; Urapidil;
D O I
10.1185/03007999009110475
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
The effect of urapidil, an a1-antagonist with additional antihypertensive action via central 5HT1A agonism, was determined on platelet aggregation induced by 5HT and adrenaline. The 5HT uptake in human platelets was determined as well. Urapidil inhibited both the 5HT and adrenaline-induced human platelet aggregation and the 5HT uptake by platelets in vitro. The 5HT-induced aggregation was inhibited with a K1 value of 8.8 μM, the adrenaline-induced aggregation with a K1 value of 21.6 μM, and the 5HT uptake non-competitively witha K11 = 1 1.5 μM and a K12=13 μM. © 1990 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.
引用
收藏
页码:86 / 92
页数:7
相关论文
共 15 条
[1]  
ANGER C, 1988, J HYPERT S, pS63
[2]  
BALL SE, 1977, J PHYSIOL-LONDON, V272, pP98
[3]   EFFECTS OF 5-HYDROXYTRYPTAMINE ON PLATELET AGGREGATION [J].
BAUMGARTNER, HR ;
BORN, GVR .
NATURE, 1968, 218 (5137) :137-+
[4]   RELATIVE ACTIVITIES ON AND UPTAKE BY HUMAN BLOOD-PLATELETS OF 5-HYDROXYTRYPTAMINE AND SEVERAL ANALOGS [J].
BORN, GVR ;
JUENGJAROEN, K ;
MICHAL, F .
BRITISH JOURNAL OF PHARMACOLOGY, 1972, 44 (01) :117-+
[5]  
CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[6]  
de Gaetano G, 1978, PLATELETS MULTIDISCI, P373
[7]  
DECLERCK F, 1982, 5 HYDROXYTRYPTAMINE, P83
[8]   INFLUENCE OF URAPIDIL ON INVITRO PLATELET RESPONSE TO ADRENALINE AND OTHER AGGREGATING AGENTS [J].
EMANUELLI, G ;
ANFOSSI, G ;
LANZIO, M ;
MULARONI, E ;
CALCAMUGGI, G ;
BRUNELLO, F ;
BUSCA, GP ;
CIANI, D .
PHARMACOLOGICAL RESEARCH COMMUNICATIONS, 1988, 20 (10) :883-899
[9]  
FOZARD J R, 1987, British Journal of Pharmacology, V90, p24P
[10]   URAPIDIL AND SOME ANALOGS WITH HYPOTENSIVE PROPERTIES SHOW HIGH AFFINITIES FOR 5-HYDROXYTRYPTAMINE (5-HT) BINDING-SITES OF THE 5-HT1A SUBTYPE AND FOR ALPHA-1-ADRENOCEPTOR BINDING-SITES [J].
GROSS, G ;
HANFT, G ;
KOLASSA, N .
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1987, 336 (06) :597-601