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H2受体拮抗剂尼扎替丁对乙酰胆碱酯酶的抑制作用。

Inhibition of acetylcholinesterase by the H2-receptor antagonist nizatidine.

作者信息

Kounenis G, Voutsas D, Koutsoviti-Papadopoulou M, Elezoglou V

机构信息

Department of Pharmacology, Veterinary Faculty, Aristotelian University of Thessaloniki, Greece.

出版信息

J Pharmacobiodyn. 1988 Nov;11(11):767-71. doi: 10.1248/bpb1978.11.767.

Abstract

The purpose of the present investigation was to study if the stimulating effect of nizatidine on the intestinal smooth muscle is related to the acetylcholinesterase activity. Isolated segments of guinea pig ileum were used in Tyrode solution at 37 degrees C. Nizatidine (from 3.2 x 10(-6) to 3.2 x 10(-4) M) exerted a concentration-dependent contractile effect on the guinea pig ileum. The average maximum activity (mean +/- S.E.M.) of nizatidine (3.2 x 10(-4) M) was 96.21 +/- 6.19% of the average maximum activity of neostigmine (3.2 x 10(-6) M). The acetylcholine-induced contractions (from 10(-8) to 3.2 x 10(-6) M) were augmented by nizatidine (from 10(-5) to 10(-4) M) in a similar way to that by neostigmine (from 10(-8) to 10(-7) M). The acetylcholine-induced contractions were prevented by acetylcholinesterase (0.1 unit/ml). This acetylcholinesterase activity was inhibited by nizatidine (from 10(-5) to 10(-4) M) and this inhibition was similar to that of neostigmine (from 10(-8) to 10(-7) M). These findings suggest that the stimulating effect of nizatidine on the intestinal smooth muscle of the guinea pig ileum could be explained by the inhibition of acetycholinesterase activity.

摘要

本研究的目的是探讨尼扎替丁对肠道平滑肌的刺激作用是否与乙酰胆碱酯酶活性有关。在37℃的台氏液中使用豚鼠回肠的离体肠段。尼扎替丁(浓度从3.2×10⁻⁶至3.2×10⁻⁴M)对豚鼠回肠产生浓度依赖性的收缩作用。尼扎替丁(3.2×10⁻⁴M)的平均最大活性(均值±标准误)为新斯的明(3.2×10⁻⁶M)平均最大活性的96.21±6.19%。尼扎替丁(浓度从10⁻⁵至10⁻⁴M)增强乙酰胆碱诱导的收缩(浓度从10⁻⁸至3.2×10⁻⁶M),其方式与新斯的明(浓度从10⁻⁸至10⁻⁷M)相似。乙酰胆碱酯酶(0.1单位/毫升)可阻断乙酰胆碱诱导的收缩。尼扎替丁(浓度从10⁻⁵至10⁻⁴M)可抑制这种乙酰胆碱酯酶活性,且这种抑制作用与新斯的明(浓度从10⁻⁸至10⁻⁷M)相似。这些发现表明,尼扎替丁对豚鼠回肠肠道平滑肌的刺激作用可通过抑制乙酰胆碱酯酶活性来解释。

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