新型组胺H2受体拮抗剂尼扎替丁（LY 139037）对豚鼠回肠的兴奋作用。

The excitatory effect of the new histamine H2-receptor antagonist nizatidine (LY 139037) on the guinea pig ileum.

作者信息

Kounenis G, 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. 1987 Nov;10(11):669-72. doi: 10.1248/bpb1978.10.669.

DOI:10.1248/bpb1978.10.669

PMID:2895808

Abstract

The histamine H2-receptor antagonist, nizatidine (LY 139037), was tested for its effect on the intestinal smooth muscle. 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) caused a concentration-dependent contractile response by the guinea pig ileum. The average maximum response to nizatidine (3.2 X 10(-4) M) was about 89% of the average maximum response to eserine (3.2 X 10(-6) M). The contractile responses induced by nizatidine were not modified by pyrilamine (10(-8) and 10(-7) M). On the other hand, atropine (10(-8) and 3.2 X 10(-8) M) significantly prevented, while eserine (10(-8) and 3.2 X 10(-8) M) significantly enhanced the nizatidine-induced responses in a concentration-dependent manner. These findings suggest that nizatidine exerts an excitatory effect on the guinea pig ileum which seems to be associated with the cholinergic system, probably through a direct and/or an indirect mechanism (inhibition of acetylcholinesterase and/or increased release of acetylcholine).

摘要

对组胺H2受体拮抗剂尼扎替丁（LY 139037）对肠道平滑肌的作用进行了测试。在37摄氏度的台氏液中使用豚鼠回肠的离体节段。尼扎替丁（浓度从3.2×10⁻⁶到3.2×10⁻⁴ M）引起豚鼠回肠浓度依赖性的收缩反应。尼扎替丁（3.2×10⁻⁴ M）的平均最大反应约为毒扁豆碱（3.2×10⁻⁶ M）平均最大反应的89%。尼扎替丁诱导的收缩反应不受吡拉明（10⁻⁸和10⁻⁷ M）的影响。另一方面，阿托品（10⁻⁸和3.2×10⁻⁸ M）显著抑制，而毒扁豆碱（10⁻⁸和3.2×10⁻⁸ M）以浓度依赖性方式显著增强尼扎替丁诱导的反应。这些发现表明，尼扎替丁对豚鼠回肠发挥兴奋作用，这似乎与胆碱能系统有关，可能是通过直接和/或间接机制（抑制乙酰胆碱酯酶和/或增加乙酰胆碱释放）。