STIMULATORY EFFECTS OF PROSTAGLANDIN-D2 ANALOGS ON ADENYLATE-CYCLASE IN RABBIT IRIS CILIARY BODY MEMBRANE-FRACTIONS

被引：11

作者：

GOH, Y ^{[1
]}

NAKAJIMA, M ^{[1
]}

机构：

[1] OSAKA MED COLL,TAKATSUKI,OSAKA 569,JAPAN

来源：

EXPERIMENTAL EYE RESEARCH | 1990年 / 51卷 / 05期

关键词：

adenylate cyclase; GTP regulatory protein; intraocular pressure; iris-ciliary body complex; prostaglandin D[!sub]2[!/sub; prostaglandin D[!sub]2[!/sub] analogue; prostaglandin D[!sub]2[!/sub] receptor; rabbit;

D O I：

10.1016/0014-4835(90)90089-D

中图分类号：

R77 [眼科学];

学科分类号：

100212 ;

摘要：

Effects of prostaglandin (PG) D2 analogues on the adenylate cyclase activity in membrane fractions of the iris-ciliary body complex were studied. PGD2 dose-dependently activated the adenylate cyclase with a maximal activity increase of about 60%. The concentration required to cause a half-maximal stimulation (EC50) was about 5 × 10-7 m. The stimulatory effect of PGD2 was totally dependent on GTP with EC50 for GTP at about 10-7 m. The rank order of potency of PGD2 analogues for stimulating the adenylate cyclase and BW245C (a selective PGD2 agonist) > PGD3 > PGD2 > 9β-PGD2. PGD2 metabolites and PGD2 analogues which have little hypotensive activity were essentially ineffective in stimulating the adenylate cyclase. This rank order was strikingly similar to that reported previously for their intraocular pressure-lowering effects. One exception was PGD2 methylester. This compound, though reportedly effective in reducing IOP, failed to activate the adenylate cyclase by itself, presumably because its hypotensive effect is due to its hydrolyzed product, PGD2. These results indicate that the abilities of PGD2 analogues to stimulate the adenylate cyclase of the iris-ciliary body complex in GTP-dependent manner are highly correlated with their ocular hypotensive activities, and suggest that a PGD2 receptor-stimulatory GTP-binding protein-adenylate cyclase complex is involved in the PGD2-induced ocular hypotension. © 1990.

引用

页码：585 / 590

页数：6

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