Bausher L P
Department of Ophthalmology and Visual Science, Yale University School of Medicine, New Haven, Connecticut, USA.
J Ocul Pharmacol Ther. 1995 Summer;11(2):135-43. doi: 10.1089/jop.1995.11.135.
The effects of endothelins on cyclic AMP production have been studied in rabbit and human ciliary processes. Endothelins inhibit basal, isoproterenol-, and VIP-stimulated cyclic AMP production in rabbit ciliary processes and forskolin-stimulated cyclic AMP production in rabbit and human ciliary processes. EC50s for inhibition of forskolin-stimulated cyclic AMP production using rabbit tissue were similar: ET-1, 70 nM; ET-2, 40 nM; ET-3, 70 nM; maximum inhibition was about 76% for each ligand. These data are consistent with the presence of an ETB receptor. Endothelin-like immunoreactivity in rabbit aqueous humor was measured to be 226 pg/ml.
已经在兔和人睫状体中研究了内皮素对环磷酸腺苷(cAMP)生成的影响。内皮素抑制兔睫状体中的基础、异丙肾上腺素和血管活性肠肽(VIP)刺激的cAMP生成,以及兔和人睫状体中福斯可林刺激的cAMP生成。使用兔组织抑制福斯可林刺激的cAMP生成的半数有效浓度(EC50)相似:内皮素-1(ET-1)为70 nM;内皮素-2(ET-2)为40 nM;内皮素-3(ET-3)为70 nM;每种配体的最大抑制率约为76%。这些数据与ETB受体的存在一致。测得兔房水中内皮素样免疫反应性为226 pg/ml。