Kimura S, Goto K, Ogawa T, Sugita Y, Kanazawa I
Neurosci Res. 1984 Dec;2(1-2):97-104. doi: 10.1016/0168-0102(84)90007-5.
Pharmacological studies were performed with neurokinin alpha and beta, new tachykinins isolated from porcine spinal cord, on smooth muscle preparations exhibiting two subtypes of substance P receptor (SP-P and SP-E receptors). The results showed that both neurokinin alpha and beta possessed the typical tachykinin activities and they exhibited SP-E-type ligand characteristics. The potency studies of SP6-11 and (Val8)SP6-11 have revealed that (VAL8)SP6-11 was comparable to SP6-11 in contracting the guinea-pig ileum (SP-P system), but greater than SP6-11 and also substance P in potentiating nerve stimulation-induced contraction of the rat vas deferens (SP-E system). The contractile response of the rat duodenum to neurokinin alpha was slow at onset and long-lasting compared with those to neurokinin beta and substance P. The residual immunoreactivity of each tachykinin in the organ bath decreased in parallel with the fading of the contractile response. The order of the half-life of each immunoreactive peptide was as follows: neurokinin alpha greater than neurokinin beta greater than substance P. The results were discussed from the viewpoints of structural significance in manifestation of pharmacological properties and in inactivation process, as well as the physiological roles of these novel mammalian tachykinins.
对从猪脊髓中分离出的新型速激肽神经激肽α和β，在表现出两种P物质受体亚型（SP-P和SP-E受体）的平滑肌制剂上进行了药理学研究。结果表明，神经激肽α和β均具有典型的速激肽活性，且表现出SP-E型配体特征。对SP6-11和(Val8)SP6-11的效能研究表明，(Val8)SP6-11在使豚鼠回肠收缩方面（SP-P系统）与SP6-11相当，但在增强神经刺激诱导的大鼠输精管收缩方面（SP-E系统）大于SP6-11以及P物质。与神经激肽β和P物质相比，大鼠十二指肠对神经激肽α的收缩反应起效缓慢且持续时间长。器官浴中每种速激肽的残留免疫反应性随着收缩反应的消退而平行下降。每种免疫反应性肽的半衰期顺序如下：神经激肽α＞神经激肽β＞P物质。从药理学特性表现和失活过程中的结构意义以及这些新型哺乳动物速激肽的生理作用等角度对结果进行了讨论。
