Müller H, Glusa E
Institute of Pharmacology and Toxicology, Medical Academy Erfurt.
Pharmazie. 1992 Feb;47(2):137-9.
The vascular effect of the potential nootropic AWD 52-39 (1; N,N-diacetoxyethyl-9,10-dihydrolysergic acid amide) as well as its influence on noradrenaline- or 5-HT-induced vasoconstriction were studied in the isolated rat aorta and in anesthetized normotensive and pithed rats. Vasoconstriction was determined by measuring the increase in mean arterial pressure (MAP). Both in vitro and in pithed rats, 1 caused a slight vasoconstriction, whereas a dose-dependent short-lasting decrease in mean arterial pressure was found in normotensive rats. In vitro and in pithed rats, 1 exerted no influence on the noradrenaline-induced vasoconstriction, while the 5-HT-induced contractile response was significantly inhibited. These findings characterize 1 as a competitive antagonist at vascular 5-HT2 receptors without any alpha-adrenolytic effect.
研究了潜在的促智药AWD 52 - 39（1；N，N - 二乙酰氧基乙基 - 9,10 - 二氢麦角酸酰胺）的血管效应及其对去甲肾上腺素或5 - 羟色胺诱导的血管收缩的影响，实验在离体大鼠主动脉以及麻醉的正常血压大鼠和脊髓切断大鼠中进行。通过测量平均动脉压（MAP）的升高来确定血管收缩情况。在体外实验以及脊髓切断大鼠中，1引起轻微血管收缩，而在正常血压大鼠中发现平均动脉压呈剂量依赖性短暂下降。在体外实验和脊髓切断大鼠中，1对去甲肾上腺素诱导的血管收缩没有影响，而5 - 羟色胺诱导的收缩反应受到显著抑制。这些发现表明1是血管5 - HT2受体的竞争性拮抗剂，且没有任何α - 肾上腺素能阻断作用。
