Endothelin-induced changes of second messengers in cultured human ciliary muscle cells.

作者: T Yorio , L DeSantis , I H Pang , S Matsumoto , P E Magnino

DOI:

关键词: Adenylyl cyclaseProstaglandin EInositolInternal medicineBiologyEndothelin receptorCalcium in biologySecond messenger systemCyclic adenosine monophosphatePhospholipase CEndocrinology

摘要: Purpose. To characterize the pharmacology of endothelin-induced changes in phospholipase C (PLC) activity, intracellular calcium concentration ([Ca 2+ ] i ), and cyclic adenosine monophosphate (cAMP) cultured human ciliary muscle (HCM) cells. Methods. Changes PLC activity HCM cells were determined by production [ 3 H]inositol phosphates. [Ca was single-cell dynamic fluorescence ratio imaging. Radioimmunoassays used to determine cAMP prostaglandin E 2 (PGE ) concentrations. Results. Endothelin-1 (ET-1) stimulated (mean EC 50 = 335 pM) activated mobilization These effects mediated endothelin ET A receptor subtype because an B receptor-selective agonist, sarafotoxin S6c, ineffective. Additionally, ET-1 inhibited pretreatment with a selective antagonist, BQ610 pK 9.96 for PLC). also PGE 12.0 nM) 5.2 these appeared mediate stimulatory effect on adenylyl cyclase blockade ET-1-induced 10 μM indomethacin completely blocked ET-1-activated production. Conclusions. increased subtype. production, likely enhanced prostaglandins.

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