PHARMACOLOGICAL CHARACTERIZATION OF POSTJUNCTIONAL 5-HT RECEPTORS IN CEREBRAL-ARTERIES FROM THE SHEEP

被引:24
作者
GAW, AJ
WADSWORTH, RM
HUMPHREY, PPA
机构
[1] UNIV STRATHCLYDE,DEPT PHYSIOL & PHARMACOL,GLASGOW G1 1XW,SCOTLAND
[2] GLAXO GRP RES LTD,DIV PHARMACOL,WARE SG12 0DJ,HERTS,ENGLAND
关键词
5-HT[!sub]1[!/sub]-like receptors; 5-HT[!sub]2[!/sub] receptors; Cerebral artery; Endothelium; Haemolysate;
D O I
10.1016/0014-2999(90)90399-Q
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In the sheep cerebral vasculature 5-hydroxytryptamine (5-HT) caused a contraction of which ketanserin was found to be an effective antagonist (Basilar artery, pA2 = 9.33 ± 0.16; middle cerebral artery, pA2 = 9.19 ± 0.16; pial artery, pA2 = 9.47 ± 0.12). Sumatriptan (GR 43175), a selective 5-HT1-like receptor agonist, was also found to have a small contractile effect on the sheep cerebral vasculature (Basilar artery, pD2 = 6.26 ± 0.11; middle cerebral artery, pD2 = 6.25 ± 0.10; pial artery, pD2 = 6.13 ± 0.15). The contractile effect of sumatriptan was not antagonised by either ketanserin (1 μM) or MDL 72222 (1 μM). 5-HT therefore appears to cause contraction by stimulation of a mixed receptor population of 5-HT1-like and 5-HT2 receptors. In the sheep middle cerebral artery the addition of haemolysate was found to cause a contractile response and also to augment the contractile effects of both noradrenaline and 5-HT but only in the presence of a functional endothelium. However, 5-HT was never found to relax precontracted rings of the middle cerebral artery in either the presence or absence of a functional endothelium. These results indicate a basal release of EDRF in cerebral arteries that attenuates the effects of various constrictor agents. © 1990.
引用
收藏
页码:35 / 44
页数:10
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