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研究萘甲异喹(NI)对离体豚鼠回肠平滑肌的作用。NI(10、30μmol/L)可明显抑制离体豚鼠回肠的自发性收缩,能拮抗组胺、乙酰胆碱和5-羟色胺对回肠的收缩效应,表现为非竞争性拮抗,其pD'2分别为5.36±0.49、4.74±0.32和4.81±0.51。NI(10、30μmol/L)尚能抑制CaCl2和BaCl2引起的离体豚鼠回肠收缩,并可抑制组胺引起肠组织内Ca2+浓度升高。结果提示:NI能抑制肠平滑肌细胞外Ca2+内流及细胞内Ca2+释放引起的平滑肌收缩,可能是一非特异性钙拮抗剂。
To investigate the effect of nalmetrane (NI) on guinea pig ileum smooth muscle. NI (10,30μmol / L) significantly inhibited spontaneous contraction of guinea pig ileum and antagonized the contractile effect of histamine, acetylcholine and serotonin on ileum, showing non-competitive antagonism with pD’2 of 5 .36 ± 0.49, 4.74 ± 0.32 and 4.81 ± 0.51. NI (10,30 μmol / L) can still inhibit the ileal contraction of isolated guinea pigs induced by CaCl2 and BaCl2, and inhibit the histamine to cause the increase of intestinal Ca2 + concentration. The results suggest that NI can inhibit smooth muscle contraction caused by influx of extracellular Ca2 + and release of intracellular Ca2 + in intestinal smooth muscle cells, which may be a nonspecific calcium antagonist.