Dage R C, Hsieh C P, Spedding M
J Cardiovasc Pharmacol. 1983 Jan-Feb;5(1):143-50. doi: 10.1097/00005344-198301000-00022.
A contribution by active vasodilation to the hypotensive effect of medroxalol was investigated in anesthetized dogs and reserpinized pithed rats. In anesthetized dogs, intravenous doses of medroxalol, which decreased blood pressure and heart rate, also produced a dose-related vasodilation in the isolated perfused gracilis muscle in situ. This vasodilator effect of medroxalol was completely blocked by propranolol; the hypotensive effect of medroxalol was inhibited 50% by propranolol but not at all by practolol. In reserpinized pithed rats with angiotensin-supported blood pressure, intravenous doses of medroxalol also produced propranolol-sensitive decreases in diastolic blood pressure and did not alter heart rate. Labetalol produced similar effects but was significantly less potent. Comparatively, equivalent amounts of isoproterenol and pindolol decreased diastolic blood pressure but increased heart rate. In the isolated guinea pig trachea, medroxalol produced a propranolol-sensitive relaxation at concentrations that antagonized the relaxant effects of salbutamol. Identical concentrations of medroxalol did not increase rate of isolated guinea pig atria. It is concluded that a substantial portion of the hypotensive effect of medroxalol is due to a beta 2-adrenergic-receptor-mediated vasodilation.
在麻醉犬和利血平化的脊髓麻醉大鼠中研究了活性血管舒张对美多心安降压作用的贡献。在麻醉犬中,静脉注射美多心安可降低血压和心率,同时在原位分离灌注的股薄肌中也产生剂量相关的血管舒张作用。美多心安的这种血管舒张作用可被普萘洛尔完全阻断;美多心安的降压作用可被普萘洛尔抑制50%,但不能被普拉洛尔抑制。在血管紧张素维持血压的利血平化脊髓麻醉大鼠中,静脉注射美多心安也可使舒张压产生普萘洛尔敏感的降低,且不改变心率。拉贝洛尔产生类似作用,但效力明显较弱。相比之下,等量的异丙肾上腺素和吲哚洛尔可降低舒张压,但增加心率。在分离的豚鼠气管中,美多心安在拮抗沙丁胺醇舒张作用的浓度下产生普萘洛尔敏感的舒张作用。相同浓度的美多心安不会增加分离的豚鼠心房的速率。得出的结论是,美多心安降压作用的很大一部分是由于β2-肾上腺素能受体介导的血管舒张。