Miao Y S, Zhang A Z, Lin C, Jiang M H, Jin G Z
Department of Pharmacology, School of Pharmacy, Shanghat Medical University, China.
Zhongguo Yao Li Xue Bao. 1991 May;12(3):260-2.
l-Stepholidine (SPD) has been shown to be effective in treating migraine, but its mechanism is not clear. So the effects of SPD on isolated rabbit basilar artery (BA), mesenteric artery (MA) and thoracic aorta (TA) were studied. The contractions of BA and MA were induced by KCl (10-160 mmol.L-1) and the contraction of TA was caused by 5-HT (0.1-100 mumol.L-1). Ketanserin was used as reference. SPD (0.1-0.2 mmol.L-1) relaxed the contractions of BA and MA induced by KCl in a noncompetitive manner with pD'2 3.4 +/- 0.3 and 4.0 +/- 0.3, respectively. SPD had no selectivity in BA and MA. SPD also inhibited the contraction of TA induced by 5-HT with pA2 9.7 +/- 2.0 and pD'2 5.4 +/- 0.6, which showed a dual of both competitive and noncompetitive antagonisms. These results suggested that SPD had a blockade effect on the calcium channel and 5-HT2 receptors.
左旋千金藤啶碱（SPD）已被证明对治疗偏头痛有效，但其作用机制尚不清楚。因此，研究了SPD对离体兔基底动脉（BA）、肠系膜动脉（MA）和胸主动脉（TA）的影响。BA和MA的收缩由氯化钾（10 - 160 mmol·L-1）诱导，TA的收缩由5-羟色胺（0.1 - 100 μmol·L-1）引起。酮色林用作对照。SPD（0.1 - 0.2 mmol·L-1）以非竞争性方式舒张由氯化钾诱导的BA和MA收缩，其pD'2分别为3.4±0.3和4.0±0.3。SPD对BA和MA无选择性。SPD还抑制由5-羟色胺诱导的TA收缩，其pA2为9.7±2.0，pD'2为5.4±0.6，表现出竞争性和非竞争性拮抗双重作用。这些结果表明，SPD对钙通道和5-HT2受体具有阻断作用。
