Shinkai M, Takayanagi I
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Jpn J Pharmacol. 1990 Oct;54(2):241-3. doi: 10.1254/jjp.54.241.
The contractile responses to substance P (SP), neurokinin A (NKA), Tyro-neurokinin B (Tyr-NKB), senktide (NK3 receptor selective agonist) and SP methyl ester (SPOMe, NK1 receptor selective agonist) were investigated in detrusor strips from guinea pigs. Except for senktide, all drugs induced a concentration-related contraction with the following rank order of potency: SPOMe greater than SP greater than NKA greater than or equal to Tyr-NKB. After desensitization of NK1 receptors with SPOMe, the rank order of potency was NKA greater than or equal to Tyr-NKB greater than SP greater than SPOMe. Both NK1 and NK2 receptors exist in the detrusor strip from guinea pigs.
在豚鼠逼尿肌条上研究了对P物质(SP)、神经激肽A(NKA)、酪胺神经激肽B(Tyr-NKB)、senktide(NK3受体选择性激动剂)和SP甲酯(SPOMe,NK1受体选择性激动剂)的收缩反应。除senktide外,所有药物均引起浓度依赖性收缩,其效力顺序如下:SPOMe大于SP大于NKA大于或等于Tyr-NKB。用SPOMe使NK1受体脱敏后,效力顺序为NKA大于或等于Tyr-NKB大于SP大于SPOMe。豚鼠逼尿肌条中同时存在NK1和NK2受体。