Wilffert B, van Heiningen P N, Mathy M J, de Jonge A, Thoolen M J, Timmermans P B, van Zwieten P A
Naunyn Schmiedebergs Arch Pharmacol. 1984 Nov;328(1):76-82. doi: 10.1007/BF00496110.
Interactions between the putative calcium entry promotor Bay k 8644 and both alpha 1- and alpha 2-adrenoceptor mediated increases in diastolic pressure were studied in the pithed normotensive rat. The alpha 2-adrenoceptor mediated pressor responses elicited by B-HT920, TL-99, DP-6,7-ADTN and B-HT958 were potentiated by Bay k 8644, reflected by a leftward shift and an increase in the maximum of the log dose-pressor response curves. The alpha 1-adrenoceptor-mediated effects elicited by cirazoline, methoxamine, (-)-amidephrine, St 587, (-)-phenylephrine and Sgd 101/75 were less enhanced by Bay k 8644. Only a leftward shift of the dose-response curves was observed, which was most pronounced for (-)-phenylephrine and Sgd 101/75. The alpha 1- and alpha 2-adrenoceptor-mediated pressor components of (-)-noradrenaline were similarly distinguished by Bay k 8644 as observed for the selective alpha 1- or alpha 2-adrenoceptor agonists. Effects of Bay k 8644 on the increase in diastolic pressure mediated by B-HT 920, St 587 and cirazoline were also studied after pretreatment with the calcium entry blocker nifedipine. After additional pretreatment with nifedipine the potentiation by Bay k 8644 observed for B-HT 920 and St 587 was more pronounced. The presence of nifedipine had no effect on the interaction between Bay k 8644 and cirazoline. It is concluded that Bay k 8644 behaves as a mirror image of nifedipine.+
在脊髓横断的正常血压大鼠中,研究了假定的钙内流促进剂Bay k 8644与α1 - 和α2 - 肾上腺素能受体介导的舒张压升高之间的相互作用。Bay k 8644增强了由B-HT920、TL-99、DP-6,7-ADTN和B-HT958引发的α2 - 肾上腺素能受体介导的升压反应,表现为对数剂量 - 升压反应曲线向左移位且最大值增加。Bay k 8644对由可乐定、甲氧明、(-)-去氧肾上腺素、St 587、(-)-去氧肾上腺素和Sgd 101/75引发的α1 - 肾上腺素能受体介导的效应增强作用较小。仅观察到剂量 - 反应曲线向左移位,这在(-)-去氧肾上腺素和Sgd 101/75中最为明显。与选择性α1 - 或α2 - 肾上腺素能受体激动剂的情况类似,Bay k 8644同样区分了(-)-去甲肾上腺素的α1 - 和α2 - 肾上腺素能受体介导的升压成分。在用钙内流阻滞剂硝苯地平预处理后,还研究了Bay k 8644对由B-HT 920、St 587和可乐定介导的舒张压升高的影响。在用硝苯地平进一步预处理后,观察到Bay k 8644对B-HT 920和St 587的增强作用更为明显。硝苯地平的存在对Bay k 8644与可乐定之间的相互作用没有影响。得出的结论是,Bay k 8644的作用表现为硝苯地平的镜像。