COEXPRESSION OF 5-HT2A AND 5-HT4 RECEPTORS COUPLED TO DISTINCT SIGNALING PATHWAYS IN HUMAN INTESTINAL MUSCLE-CELLS

被引：52

作者：

KUEMMERLE, JF ^{[1
]}

MURTHY, KS ^{[1
]}

GRIDER, JR ^{[1
]}

MARTIN, DC ^{[1
]}

MAKHLOUF, GM ^{[1
]}

机构：

[1] VIRGINIA COMMONWEALTH UNIV,MED COLL VIRGINIA,DEPT PHYSIOL,RICHMOND,VA 23298

来源：

GASTROENTEROLOGY | 1995年 / 109卷 / 06期

关键词：

D O I：

10.1016/0016-5085(95)90745-9

中图分类号：

R57 [消化系及腹部疾病];

学科分类号：

摘要：

Background & Aims: The type and function of 5-hydroxytryptamine (5-HT) receptors on intestinal muscle cells in humans are not known. 5-HT receptors were characterized pharmacologically and by radioligand binding. Methods: Contraction, relaxation, inositol 1,4,5-triphosphate (IP3) and adenosine 3',5'-cyclic monophosphate (cAMP) formation, and 5-HT binding were measured in dispersed muscle cells and in cells in which only one receptor type was preserved by selective receptor protection. Results: 5-HT binding was completely inhibited by 5-HT and partially by 5-HT2A (ketanserin), 5HT(4) (SDZ-205,557), and 5HT(1p) (N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan amide; 5-HTP-DP) receptor antagonists. 5-HT caused contraction that was inhibited by ketanserin and augmented by SDZ-205,557 and 5-HTP-DP. In the presence of ketanserin, 5-HT caused relaxation of cholecystokinin-contracted cells that was inhibited by SDZ-205,557 and 5-HTP-DP. 5HT increased IP3, which was inhibited by ketanserin, and cAMP, which was inhibited by SDZ-205,557 and 5-HTP-DP. In cells with only 5-HT2A receptors, 5-HT caused contraction only, and residual binding was inhibited by ketanserin. In cells with only 5-HT4/5-HT1p receptors, 5-HT caused only relaxation and residual binding was inhibited by SDZ-205,557 and 5-HTP-DP. Conclusions: 5-HT2A receptors mediating contraction and 5-HT4 receptors mediating relaxation coexist on human intestinal muscle cells. The 5HT(4) receptors are closely similar or identical to 5HT(1p) receptors.

引用

页码：1791 / 1800

页数：10

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