Gazis D, Gonzalez G, Mendlowitz M
Can J Physiol Pharmacol. 1987 Jan;65(1):6-11. doi: 10.1139/y87-002.
To try to compare receptor compartment kinetics, receptor binding, and binding-response coupling for two smooth muscle types in vivo, pressor and uterine responses to oxypressin, an equipotent analog of oxytocin and vasopressin, were studied simultaneously in urethane-anesthetized, pentolinium-indomethacin treated rats. Access of peptide to the pressor and uterine receptor compartments and peptide-receptor dissociation rate had a negligible effect on the two responses. During both injections and infusions, the blood pressure response seemed to be determined largely by plasma levels of oxypressin. The uterine response to oxypressin, however, was paradoxical. The heights of individual uterine contractions seemed to be determined throughout by plasma oxypressin concentrations. The interval between contractions also seemed to be determined by plasma peptide concentrations during injections. However, as plasma peptide increased and reached steady state during infusion, contraction interval behaved as if plasma peptide concentrations were decreasing. This effect was more marked at the beginning of infusion. The implication of these results is that binding determines the pressor response to oxypressin and binding-response coupling does not change. In contrast, although binding determines the uterine response to oxypressin during injection and binding-response coupling appears constant, some factor in addition to binding affects the contraction interval portion of the uterine response and modifies the apparent binding-response coupling of this parameter during infusion.
为了在体内比较两种平滑肌类型的受体区室动力学、受体结合及结合 - 反应偶联,在氨基甲酸乙酯麻醉、经潘托铵 - 吲哚美辛处理的大鼠中,同时研究了对催产素和加压素的等效类似物氧加压素的升压反应和子宫反应。肽进入升压和子宫受体区室以及肽 - 受体解离速率对这两种反应的影响可忽略不计。在注射和输注过程中,血压反应似乎很大程度上由血浆中氧加压素的水平决定。然而,子宫对氧加压素的反应却自相矛盾。单个子宫收缩的高度似乎始终由血浆中氧加压素的浓度决定。收缩间隔在注射期间似乎也由血浆肽浓度决定。然而,随着血浆肽增加并在输注过程中达到稳态,收缩间隔表现得就好像血浆肽浓度在下降。这种效应在输注开始时更为明显。这些结果表明,结合决定了对氧加压素的升压反应且结合 - 反应偶联不变。相比之下,尽管结合决定了注射期间子宫对氧加压素的反应且结合 - 反应偶联似乎恒定,但除结合之外的某些因素会影响子宫反应的收缩间隔部分,并在输注期间改变该参数的表观结合 - 反应偶联。