Jumblatt J E, North G T, Hackmiller R C
Department of Ophthalmology and Visual Sciences, University of Louisville School of Medicine, Kentucky Lions Eye Research Institute 40202.
Invest Ophthalmol Vis Sci. 1990 Jun;31(6):1103-8.
The effects of cholinergic agents on hormone-stimulated cyclic AMP (cAMP) accumulation were investigated in iris-ciliary body segments, excised ciliary processes, and isolated ciliary epithelium from albino rabbit eyes. In all three tissue preparations, the cholinergic agonist carbamylcholine markedly inhibited the stimulation of cAMP biosynthesis by vasoactive intestinal peptide VIP--a potent activator of nonpigmented ciliary epithelial adenylate cyclase. Carbamylcholine also attenuated cAMP increases mediated by isoproterenol, prostaglandin E2, and forskolin. The effects of carbamylcholine on VIP-induced cAMP synthesis were concentration dependent (EC50 = 23 nM), mimicked by selective muscarinic cholinergic agonists (oxotremorine, pilocarpine), and antagonized by atropine. Carbamylcholine- and clonidine-mediated inhibition of VIP-stimulated cAMP accumulation in ciliary processes were nonadditive, indicating that inhibitory muscarinic and alpha 2-adrenergic receptors coexist on VIP-responsive target cells. These findings suggest that the cholinergic system may have a direct role in modulation of ciliary epithelial adenylate cyclase and aqueous humor secretion.
研究了胆碱能药物对激素刺激的环磷酸腺苷(cAMP)积累的影响,实验对象为白化兔眼的虹膜睫状体节段、离体睫状突和分离的睫状体上皮。在所有这三种组织标本中,胆碱能激动剂氨甲酰胆碱显著抑制血管活性肠肽(VIP)对cAMP生物合成的刺激作用,VIP是无色素睫状上皮腺苷酸环化酶的一种有效激活剂。氨甲酰胆碱还减弱了由异丙肾上腺素、前列腺素E2和福斯高林介导的cAMP增加。氨甲酰胆碱对VIP诱导的cAMP合成的作用呈浓度依赖性(半数有效浓度=23 nM),选择性毒蕈碱胆碱能激动剂(震颤素、毛果芸香碱)可模拟该作用,而阿托品可拮抗该作用。氨甲酰胆碱和可乐定对睫状突中VIP刺激的cAMP积累的抑制作用不具有相加性,这表明抑制性毒蕈碱受体和α2 -肾上腺素能受体共存于对VIP有反应的靶细胞上。这些发现提示胆碱能系统可能在调节睫状上皮腺苷酸环化酶和房水分泌中具有直接作用。