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PubMed1982

[General pharmacology of lisuride hydrogen maleate--actions on isolated organs, especially on smooth muscles].

Pharmacological actions of lisuride hydrogen maleate (lisuride) were studied by using isolated organs. 1) Lisuride at 2.2 microM exerted a negative chronotropic effect on guinea-pig atria, the effect being antagonized completely by 2.9 microM sulpiride. 2) alpha-Adrenolytic action of lisuride was observed in the rat vas deferens and beta-adrenolytic action in the rabbit trachea, respectively. The former (ID50 = 64 nM) was potent and equivalent to that of phentolamine, whereas the latter (ID50 = 26 microM) was only 1/30 as compared to that of propranolol. 3) Anti-5-hydroxytryptamine action (ID50 = 11 nM) was detected in the rat stomach and anti-histamine (ID50 = 15 nM) in the guinea-pig ileum, respectively. In these respective activities, lisuride was equipotent to methysergide and diphenhydramine. 4) Lisuride showed a spasmodic action, which may be categolized as an ergot alkaloid action, on the guinea-pig ileum and on rabbit renal artery. A weak positive inotropic action of lisuride was also observed in guinea-pig atria. In the rat uterus, however, no uterotonic action of lisuride was detected. It is concluded that, in addition to its known effects on the central nervous system, lisuride possesses potent peripheral anti-5-hydroxytryptamine and anti-histamine activities.

Animals↗
PubMed1996

Effects of quinazoline (3H, 1H)-4-one-2-thiones with axial and central chirality on the contractile response of smooth muscle.

Quinazolines are versatile nitrogen heterocyclic compounds displaying a broad spectrum of biological and pharmacological activities. The influence of some new synthesized quinazolines with axial and central chirality was studied on the isometric muscle tension of rat ileum, rat uterus, and porcine coronary artery. While structural changes of the compounds showed only little influence on peristaltic movement of the ileum, quinazoline derivatives induced a relaxation in the uterus and in the coronary artery depending on the kind and position of the substituent. The introduction of axial chirality into the molecule of modification of the side chain caused an increase in the pharmacological action. These effects could not be inhibited by sympatholytics. So far the mechanisms and receptors causing the spasmolysis are unknown.

Animals↗