Dion S, D'Orléans-Juste P, Drapeau G, Rhaleb N E, Rouissi N, Tousignant C, Regoli D
Department of Pharmacology Medical School, University of Sherbrooke, Québec, Canada.
Life Sci. 1987 Nov 16;41(20):2269-78. doi: 10.1016/0024-3205(87)90538-8.
The three mammalian neurokinins, substance P, neurokinin A and neurokinin B, as well as some agonists selective for their respective receptors, NK-P, NK-A and NK-B, were tested in a variety of pharmacological preparations in order to evaluate if the biological responses of the various tissues were mediated by single or multiple receptor types. Previous observations that the dog carotid artery, the rabbit pulmonary artery and the rat portal vein are selective preparations respectively for SP, NKA and NKB were confirmed in the present study by showing that only the respective selective agonists were active on these tissues. Multiple functional sites were demonstrated in intestinal tissues (guinea pig ileum, rat duodenum), which apparently contain the three neurokinin receptors. A large number of NK-P, together with some NK-A receptor sites were found in the guinea pig and rat urinary bladder. Similarly, the guinea pig trachea and the rabbit mesenteric vein contain NK-A and NK-P functional sites. Rat and rabbit vas deferens stimulated electrically respond as typical NK-A preparations, since they are almost insensitive to SP or NKB selective agonists. A mixture of NK-A and NK-B receptor sites has been shown to be present in the hamster urinary bladder: dog and human urinary bladder definitely contain NK-A receptors and the dog bladder also some NK-P functional sites.
对三种哺乳动物神经激肽,即P物质、神经激肽A和神经激肽B,以及一些对其各自受体具有选择性的激动剂,NK-P、NK-A和NK-B,在多种药理制剂中进行了测试,以评估各种组织的生物学反应是由单一还是多种受体类型介导的。先前的观察结果表明,犬颈动脉、兔肺动脉和大鼠门静脉分别是P物质、神经激肽A和神经激肽B的选择性制剂,本研究通过表明只有各自的选择性激动剂对这些组织有活性,证实了这一观察结果。在肠道组织(豚鼠回肠、大鼠十二指肠)中证明了多个功能位点,这些组织显然含有三种神经激肽受体。在豚鼠和大鼠膀胱中发现了大量的NK-P以及一些NK-A受体位点。同样,豚鼠气管和兔肠系膜静脉含有NK-A和NK-P功能位点。电刺激的大鼠和兔输精管表现为典型的神经激肽A制剂反应,因为它们对P物质或神经激肽B选择性激动剂几乎不敏感。已证明仓鼠膀胱中存在神经激肽A和神经激肽B受体位点的混合物:犬和人膀胱肯定含有神经激肽A受体,犬膀胱还含有一些NK-P功能位点。