Holzer-Petsche U, Schimek E, Amann R, Lembeck F
Naunyn Schmiedebergs Arch Pharmacol. 1985 Aug;330(2):130-5. doi: 10.1007/BF00499905.
Recently, two kassinin-like tachykinins have been isolated from mammalian nervous tissue. The potencies of these peptides, substance K (neurokinin alpha) and neuromedin K (neurokinin beta) were compared with those of substance P, eledoisin, and kassinin in various pharmacological systems in vivo and in vitro. In contracting the isolated guinea-pig ileum and rabbit jejunum the potencies of eledoisin, kassinin, substance K, and neuromedin K were 13-80% that of substance P. In the rat vas deferens substance K and neuromedin K potentiated the electrically induced contractions with potencies similar to those of eledoisin and kassinin; they were 46-236 times as potent as substance P. In stimulating salivation in the rat after intravenous injection, eledoisin, kassinin, and substance K were respectively 2.3, 1.3 and 0.33 times as potent as substance P. In contrast, neuromedin K exhibited negligible activity. Each peptide tested led to a short fall in blood pressure after intravenous injection in the rabbit, substance P being 12-250 times as potent as the other peptides. Substance P was 20 times as potent as substance K or neuromedin K in inducing vasodilatation in the rat hind paw in vivo. Of the peptides tested, only substance P (10 nmol/min) significantly increased the release of histamine from the rat isolated hindquarter preparation. The results are discussed with respect to several theories of tachykinin receptor heterogeneity.
最近，从哺乳动物神经组织中分离出了两种类速激肽。在体内和体外的各种药理系统中，将这些肽（物质K（神经激肽α）和神经介素K（神经激肽β））的效力与P物质、蛙皮素和速激肽的效力进行了比较。在使离体豚鼠回肠和兔空肠收缩方面，蛙皮素、速激肽、物质K和神经介素K的效力为P物质的13 - 80%。在大鼠输精管中，物质K和神经介素K增强电诱导收缩的效力与蛙皮素和速激肽相似；它们的效力是P物质的46 - 236倍。在静脉注射后刺激大鼠唾液分泌方面，蛙皮素、速激肽和物质K的效力分别是P物质的2.3倍、1.3倍和0.33倍。相比之下，神经介素K的活性可忽略不计。在兔静脉注射后，每种受试肽都会导致血压短暂下降，P物质的效力是其他肽的12 - 250倍。在体内诱导大鼠后爪血管舒张方面，P物质的效力是物质K或神经介素K的20倍。在受试肽中，只有P物质（10 nmol/分钟）能显著增加大鼠离体后肢标本中组胺的释放。针对速激肽受体异质性的几种理论对结果进行了讨论。
