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出 处:《Acta Pharmacologica Sinica》2002年第4期289-295,共7页中国药理学报(英文版)
基 金:Project supported by Deutsche Forschungsgemeinschaft, Bonn, Germany (DFG), Sonderforschungsbereich der Deutschen Forschungsgemeinschaft, Bonn, Germany (SFB), Al/245/8-1 and SFB-391-C5.
摘 要:AIM: To examine the effect of tachykinins on the ascending reflex pathway in rat small intestine, we used different selective neurokinin (NK) receptor antagonists (RA): a) NK1-RA: GR-82334 and CP-96.345, b) NK2-RA: MEN-10.376 and L-659.877. The aim was further to investigate the effect of substance P (SP) on the ascending excitatory and descending inhibitory reflex pathway. METHODS: The whole segments of rat ileum (10 cm in length) were studied in an organ bath. Ascending contraction of circle muscle was elicited by anal electrical stimulation (3 Hz, 1 ms, 20 V) and measured as change of intraluminal pressure by a perfused manometric system 2 cm and 4 cm orad of the stimulation site. RESULTS: GR-82334 and CP-96.345 (NK1-RA) caused a significant dose-related inhibition of the oral contraction at a distance of 4 cm: GR-82334 [area: -10 % +/- 8 % (10 nmol/L); -29 % +/ -10 % (1000 nmol/L). P瞄准:在老鼠在上升反射小径上检验 tachykinins 的效果小肠,我们使用了不同选择 neurokinin (NK ) 受体对手(RA ) :一) NK1-RA:GR-82334 和 CP-96.345, b ) NK2-RA:MEN-10.376 和 L-659.877。目的是进一步的在上升上调查物质 P (SP ) 的效果有刺激性、下降的禁止的反射小径。方法:老鼠回肠(在长度的 10 厘米) 的整个片断在机关洗澡被学习。圆肌肉的上升收缩被肛门电的刺激得到(3 Hz, 1 ms, 20 V ) 并且由一个酒的压力计的系统作为 intraluminal 压力的变化测量了刺激地点的 2 厘米和 4 厘米或广告。结果:GR-82334 和 CP-96.345 (NK1-RA ) 在 4 厘米的距离引起了口头的收缩的重要剂量相关的抑制:GR-82334 [区域:-10 %+/- 8 %(10 nmol/L ) ;-29 %+/-10 %(1000 nmol/L ) 。
关 键 词:Afferent Pathways Animals Biphenyl Compounds Efferent Pathways ILEUM In Vitro Male Muscle Contraction Muscle Smooth Neurokinin A Peptide Fragments Physalaemin RATS Rats Wistar Reaction Time Receptors Neurokinin-1 Receptors Neurokinin-2 REFLEX Research Support Non-U.S. Gov't Substance P TACHYKININS
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