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结晶-8,是从两面针提出的一种单体。当浓度为1×10~(-6)～1×10~(-4)g/ml对正常离体豚鼠回肠活动无影响,但对乙酰胆硷、匹鲁卡品、氯化钡及组织胺所致肠肌收缩有明显的松弛作用;结晶-8腹腔注射10 mg/kg有明显抑制小鼠扭体反应;8～20 mg/kg明显提高家兔及大鼠痛阈,200μg/kg脑室注射亦有明显提高大鼠痛阈。其镇痛作用不被丙烯吗啡(5 mg/kg)所拮抗,而被利血平(4 mg/kg)所对抗。表明结晶-8的解痉作用直接作用于肠平滑肌。而镇痛作用具有中枢性,与吗啡受体无直接关系,但与脑内单胺类介质有关。
Crystalline-8, is a monomer proposed from the two-way needle. The concentration of 1 × 10 -6 -6 × -1 4 g / ml had no effect on the ileum of normal guinea pigs, but the effects of acetylcholine, pilocarpine, barium chloride and histamine Induced contraction of the intestine significantly relaxation effect; Crystalline -8 intraperitoneal injection of 10 mg / kg significantly inhibited writhing in mice; 8 ~ 20 mg / kg significantly increased rabbit and rat pain threshold, 200μg / kg intraventricular injection Also significantly increased rat pain threshold. Its analgesic effect was not antagonized by morphine (5 mg / kg) and was antagonized by reserpine (4 mg / kg). This indicates that the antispasmodic effect of crystalline-8 acts directly on the intestinal smooth muscle. The central analgesic effect, and morphine receptor is not directly related, but with the brain monoaminergic medium.