Sjöberg T, Steen S, Skärby T, Norgren L, Andersson K E
Pharmacol Toxicol. 1987 Jan;60(1):43-50. doi: 10.1111/j.1600-0773.1987.tb01717.x.
A pharmacological characterization of the postjunctional alpha-adrenoceptors in human superficial epigastric artery and vein was performed, using several alpha-adrenoceptor subtype selective agonists, and the antagonists prazosin (alpha 1) and rauwolscine (alpha 2). In the arteries prazosin fulfilled the criteria for a competitive antagonism in concentrations 10(-9)-10(-7) M, giving a pA2-value of 9.17 in the Schild plot. Rauwolscine in concentrations 10(-8)-10(-6) M caused less pronounced but significant dextral shifts of the noradrenaline (NA) concentration-response curves. In the veins rauwolscine behaved like a competitive antagonist (10(-8)-10(-7) M). The pA2-value was 9.16. Prazosin 10(-9) M displaced the NA concentration-response curve, but higher concentrations (10(-8) and 10(-7) M) caused no further displacement. Prazosin reduced the Emax-values in the veins. In the arteries the rank order of potency for the agonists was: cirazoline (alpha 1) greater than NA greater than naphazoline (alpha 2) greater than guanfacine (alpha 2) greater than phenylephrine (alpha 1). The intrinsic activities of clonidine (alpha 2), ST 587 (alpha 1), B-HT 920 (alpha 2) and B-HT 933 (alpha 2) were too low to allow meaningful comparisons to be made. The rank order of potency in the veins was: NA greater than clonidine (alpha 2) greater than naphazoline (alpha 2) greater than guanfacine (alpha 2) greater than phenylephrine (alpha 1) greater than B-HT 920 (alpha 2) greater than cirazoline (alpha 1) greater than B-HT 933 (alpha 2). The intrinsic activity of ST 587 was low.(ABSTRACT TRUNCATED AT 250 WORDS)
利用几种α-肾上腺素能受体亚型选择性激动剂以及拮抗剂哌唑嗪(α1)和利血胺(α2),对人腹壁浅动脉和静脉的节后α-肾上腺素能受体进行了药理学特性研究。在动脉中,哌唑嗪在10^(-9)-10^(-7)M浓度下符合竞争性拮抗标准,在施尔德图中给出的pA2值为9.17。利血胺在10^(-8)-10^(-6)M浓度下导致去甲肾上腺素(NA)浓度-反应曲线出现不太明显但显著的右旋位移。在静脉中,利血胺表现为竞争性拮抗剂(10^(-8)-10^(-7)M),pA2值为9.16。10^(-9)M的哌唑嗪使NA浓度-反应曲线发生位移,但更高浓度(10^(-8)和10^(-7)M)未引起进一步位移。哌唑嗪降低了静脉中的Emax值。在动脉中,激动剂的效力顺序为:可乐定(α1)>NA>萘甲唑啉(α2)>胍法辛(α2)>去氧肾上腺素(α1)。可乐定(α2)、ST 587(α1)、B-HT 920(α2)和B-HT 933(α2)的内在活性过低,无法进行有意义的比较。在静脉中的效力顺序为:NA>可乐定(α2)>萘甲唑啉(α2)>胍法辛(α2)>去氧肾上腺素(α1)>B-HT 920(α2)>可乐定(α1)>B-HT 933(α2)。ST 587的内在活性较低。(摘要截断于250字)