Mehrabani P A, Bassett J R
School of Biological Sciences, Macquarie University, N.S.W., Australia.
Pharmacol Biochem Behav. 1990 Jan;35(1):99-103. doi: 10.1016/0091-3057(90)90211-y.
Using the ACTH analog [125I-Tyr23,Phe2,Nle4] ACTH(1-24), the existence of specific binding sites for ACTH in atrial membrane preparations was demonstrated. The dissociation constants (Kd), determined by Scatchard analysis were not significantly different for membrane preparations of adrenal gland or atrial tissue (being 6.40 x 10(-12)M and 8.86 x 10(-12)M respectively). No binding was observed to membrane preparations from kidney or lung. While the binding of the ACTH(1-24) analog to atrial membranes was inhibited by ACTH(1-24), it was not affected by norepinephrine or epinephrine. It was proposed that the ACTH(1-24) analog may bind to sites located on the adrenergic nerve endings associated with the cardiac tissue, and that such binding would interfere with the neuronal reuptake of the catecholamines.
使用促肾上腺皮质激素类似物[125I-酪氨酸23,苯丙氨酸2,亮氨酸4]促肾上腺皮质激素(1-24),证实了心房膜制剂中存在促肾上腺皮质激素的特异性结合位点。通过Scatchard分析确定的解离常数(Kd),肾上腺或心房组织的膜制剂之间无显著差异(分别为6.40×10(-12)M和8.86×10(-12)M)。在肾脏或肺的膜制剂中未观察到结合。虽然促肾上腺皮质激素(1-24)类似物与心房膜的结合受到促肾上腺皮质激素(1-24)的抑制,但不受去甲肾上腺素或肾上腺素的影响。有人提出,促肾上腺皮质激素(1-24)类似物可能与心脏组织相关的肾上腺素能神经末梢上的位点结合,并且这种结合会干扰儿茶酚胺的神经元再摄取。