Bausher L P, Gregory D S, Sears M L
Curr Eye Res. 1987 Mar;6(3):497-505. doi: 10.3109/02713688709025206.
The interaction between the alpha 2- and beta 2-adrenergic receptors of ciliary processes has been studied by examining dose-response curves for adrenergic agonist stimulation of cyclic AMP production by intact, excised rabbit ciliary processes. Stimulation of cyclic AMP production by 1-isoproterenol is maximum from 0.1 to 1.0 microM; at higher concentrations stimulation decreases and approaches basal levels. Decreased cyclic AMP production at high concentrations of isoproterenol is blocked by the specific alpha 2-adrenergic antagonist, yohimbine, but not by the alpha 1-adrenergic antagonist, prazosin. Ciliary processes from animals after bilateral cervical ganglionectomy also show reduced cyclic AMP production at high concentrations of isoproterenol and this reduction is blocked by yohimbine, but not prazosin. This experiment suggests that the inhibition at high concentrations of isoproterenol is mediated by postsynaptic alpha 2-adrenergic receptors. Cyclic AMP production is relatively insensitive to epinephrine and norepinephrine, but their responses are potentiated by yohimbine. Catecholamines and clonidine, a specific alpha 2-adrenergic agonist, exhibit dose-dependent inhibition of forskolin-stimulated cyclic AMP production by ciliary processes. I50s from the dose-response curves are consistent with the characteristic binding affinities of these adrenergic agonists for alpha 2-adrenergic receptors: clonidine = epinephrine greater than norepinephrine greater than isoproterenol. Inhibition of forskolin-stimulated cyclic AMP production by clonidine is blocked by yohimbine but not by prazosin.(ABSTRACT TRUNCATED AT 250 WORDS)
通过检测肾上腺素能激动剂刺激完整的、切除的兔睫状体产生环磷酸腺苷(cAMP)的剂量反应曲线,研究了睫状体中α2 - 和β2 - 肾上腺素能受体之间的相互作用。1 - 异丙肾上腺素刺激cAMP产生的最大值出现在0.1至1.0微摩尔/升之间;在更高浓度下,刺激作用减弱并接近基础水平。高浓度异丙肾上腺素导致的cAMP产生减少被特异性α2 - 肾上腺素能拮抗剂育亨宾所阻断,但不被α1 - 肾上腺素能拮抗剂哌唑嗪阻断。双侧颈神经节切除术后动物的睫状体在高浓度异丙肾上腺素作用下也显示cAMP产生减少,且这种减少被育亨宾阻断,而非哌唑嗪。该实验表明,高浓度异丙肾上腺素的抑制作用是由突触后α2 - 肾上腺素能受体介导的。cAMP产生对肾上腺素和去甲肾上腺素相对不敏感,但其反应可被育亨宾增强。儿茶酚胺和可乐定(一种特异性α2 - 肾上腺素能激动剂)对睫状体中福斯高林刺激的cAMP产生表现出剂量依赖性抑制。剂量反应曲线的半数抑制浓度(I50)与这些肾上腺素能激动剂对α2 - 肾上腺素能受体的特征性结合亲和力一致:可乐定 = 肾上腺素>去甲肾上腺素>异丙肾上腺素。可乐定对福斯高林刺激的cAMP产生的抑制作用被育亨宾阻断,但不被哌唑嗪阻断。(摘要截选至250字)