Glusa E, Markwardt F
Arch Int Pharmacodyn Ther. 1986 Oct;283(2):303-11.
The effect of dihydrolysergic acid amide (DLSA) on responses of human blood platelets and isolated postmortem femoral veins to serotonin and catecholamines was studied in vitro in comparison to dihydroergotamine (DHE). DLSA inhibited the 5-HT-potentiated, ADP-induced platelet aggregation in approximately the same concentration range as DHE. It was three orders of magnitude less potent in inhibiting the adrenaline-induced aggregation and specific binding of 3H-yohimbine to intact platelets than DHE. In femoral vein strips, DLSA caused an increase in tone in the same concentration range (0.01-1.0 mumol/l) as DHE; however, its efficacy was somewhat lower. At concentrations of 0.1 to 1.0 mumol/l it antagonized the 5-HT-induced contractile response in a noncompetitive manner, the antagonist potency being one order of magnitude lower than that of DHE. DLSA (1 mumol/l) did not inhibit the noradrenaline-induced venoconstriction. The results show that DLSA possesses agonist activity in femoral veins and 5-HT-antagonist activity in platelets and veins.
与双氢麦角胺（DHE）相比，在体外研究了双氢麦角酰二乙胺（DLSA）对人血小板以及离体股静脉对血清素和儿茶酚胺反应的影响。DLSA抑制5-羟色胺（5-HT）增强的、二磷酸腺苷（ADP）诱导的血小板聚集，其浓度范围与DHE大致相同。在抑制肾上腺素诱导的血小板聚集以及3H-育亨宾与完整血小板的特异性结合方面，其效力比DHE低三个数量级。在股静脉条中，DLSA在与DHE相同的浓度范围（0.01 - 1.0 μmol/L）内引起张力增加；然而，其效力略低。在0.1至1.0 μmol/L的浓度下，它以非竞争性方式拮抗5-HT诱导的收缩反应，其拮抗效力比DHE低一个数量级。DLSA（1 μmol/L）不抑制去甲肾上腺素诱导的静脉收缩。结果表明，DLSA在股静脉中具有激动剂活性，在血小板和静脉中具有5-HT拮抗剂活性。
