WHAT INTRACRANIAL TISSUES IN HUMANS CONTAIN SUMATRIPTAN-SENSITIVE SEROTONIN 5-HT1-TYPE RECEPTORS

被引:13
作者
DEKEYSER, J [1 ]
VAUQUELIN, G [1 ]
DEBACKER, JP [1 ]
DEVOS, H [1 ]
WILCZAK, N [1 ]
机构
[1] VRIJE UNIV BRUSSELS,PROT CHEM LAB,B-1090 BRUSSELS,BELGIUM
关键词
SUMATRIPTAN; SEROTONIN RECEPTOR; CRANIAL BLOOD VESSEL; CORONARY ARTERY; BLOOD PLATELET; BRAIN; HUMAN; MIGRAINE;
D O I
10.1016/0304-3940(93)90858-I
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
We investigated the presence of sumatriptan-sensitive serotonin (5-HT)(1) receptors in different human tissues by using a radioligand-binding technique with [H-3]5-HT. Sumatriptan displaced [H-3]5-HT from frontal cortical and striatal membranes in a biphasic manner, with a high-affinity site corresponding to binding to the 5-HT1D receptor. In blood platelet membranes, sumatriptan displaced [H-3]S-HT with a 100-fold lower affinity. Sumatriptan failed to displace [H-3]5-HT in membranes from large cerebral arteries, pial vessels, coronary arteries and dura mater. These findings suggest that either there are no sumatriptan-sensitive 5-HT1 receptors on intracranial blood vessels or they are so small in number that they cannot be detected by the radioligand-binding technique. Other mechanisms, possibly centrally mediated, may be responsible for the antimigraine action of sumatriptan.
引用
收藏
页码:63 / 66
页数:4
相关论文
共 20 条
[1]   SEROTONIN INDUCED ACTIN POLYMERIZATION AND ASSOCIATION WITH CYTOSKELETAL ELEMENTS IN CULTURED BOVINE AORTIC ENDOTHELIUM [J].
ALEXANDER, JS ;
HECHTMAN, HB ;
SHEPRO, D .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1987, 143 (01) :152-158
[2]   THE ANTIMIGRAINE DRUG, SUMATRIPTAN (GR43175), SELECTIVELY BLOCKS NEUROGENIC PLASMA EXTRAVASATION FROM BLOOD-VESSELS IN DURA MATER [J].
BUZZI, MG ;
MOSKOWITZ, MA .
BRITISH JOURNAL OF PHARMACOLOGY, 1990, 99 (01) :202-206
[3]   ANTIMIGRAINE DRUG SUMATRIPTAN INCREASES BLOOD-FLOW VELOCITY IN LARGE CEREBRAL-ARTERIES DURING MIGRAINE ATTACKS [J].
CAEKEBEKE, JFV ;
FERRARI, MD ;
ZWETSLOOT, CP ;
JANSEN, J ;
SAXENA, PR .
NEUROLOGY, 1992, 42 (08) :1522-1526
[4]   SUBTYPES OF ADRENERGIC AND DOPAMINERGIC RECEPTORS IN BOVINE CEREBRAL BLOOD-VESSELS [J].
DEKEYSER, J ;
EBINGER, G ;
DEBACKER, JP ;
CONVENTS, A ;
VANDERHEYDEN, P ;
VAUQUELIN, G .
NEUROSCIENCE LETTERS, 1988, 85 (02) :272-276
[5]   [H-3] SCH-23390 LABELS A NOVEL 5-HYDROXYTRYPTAMINE BINDING-SITE IN HUMAN-BLOOD PLATELET MEMBRANES [J].
DEKEYSER, J ;
WALRAEVENS, H ;
CONVENTS, A ;
EBINGER, G ;
VAUQUELIN, G .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1989, 162 (03) :437-445
[6]   THE SELECTIVE CAROTID ARTERIAL VASOCONSTRICTOR ACTION OF GR43175 IN ANESTHETIZED DOGS [J].
FENIUK, W ;
HUMPHREY, PPA ;
PERREN, MJ .
BRITISH JOURNAL OF PHARMACOLOGY, 1989, 96 (01) :83-90
[7]  
FERRARI MD, 1991, NEW ENGL J MED, V325, P316
[8]   SEROTONIN METABOLISM IN MIGRAINE [J].
FERRARI, MD ;
ODINK, J ;
TAPPARELLI, C ;
VANKEMPEN, GMJ ;
PENNINGS, EJM ;
BRUYN, GW .
NEUROLOGY, 1989, 39 (09) :1239-1242
[9]   MIGRAINE PAIN ASSOCIATED WITH MIDDLE CEREBRAL-ARTERY DILATATION - REVERSAL BY SUMATRIPTAN [J].
FRIBERG, L ;
OLESEN, J ;
IVERSEN, HK ;
SPERLING, B .
LANCET, 1991, 338 (8758) :13-17
[10]   LOCALIZATION OF H-3 DIHYDROERGOTAMINE BINDING-SITES IN THE CAT CENTRAL-NERVOUS-SYSTEM - RELEVANCE TO MIGRAINE [J].
GOADSBY, PJ ;
GUNDLACH, AL .
ANNALS OF NEUROLOGY, 1991, 29 (01) :91-94