Mastrangelo D, Mathison R, Huggel H J, Dion S, D'Orléans-Juste P, Rhaleb N E, Drapeau G, Rovero P, Regoli D
Eur J Pharmacol. 1987 Feb 24;134(3):321-6. doi: 10.1016/0014-2999(87)90363-3.
The rat isolated portal vein is a pharmacological preparation more sensitive to neurokinin B than to any other neurokinin or tachykinin. The preparation is more sensitive to C-terminal partial sequences of substance P (SP) particularly SP-(6-11) than to the whole undecapeptide. The order of potency of neurokinins is as follows: neurokinin B greater than neurokinin A greater than substance P. The preparation shows high sensitivity also to kassinin and eledoisin. Comparative tests performed with strips of the rat portal vein suspended in a microbath under continuous perfusion (system 1) or in ordinary baths for isolated smooth muscles (system 2) have given similar results and have shown that the myotropic effect of neurokinin B is not modified by a variety of antagonists of endogenous agents as well as by inhibitors of the arachidonic acid cascade. The present results suggest that neurokinin B contracts the rat portal vein by activating specific receptors, presumably located on the smooth muscle membrane, different from those of biologically active amines and peptides which are active stimulants of the vein. Neurokinin B is ten times more active than neurokinin A and at least 100 times more than substance P. Such an order of potency of agonists suggests the existence of a new neurokinin receptor type, particularly sensitive to neurokinin B.
大鼠离体门静脉是一种药理制剂,对神经激肽B的敏感性高于任何其他神经激肽或速激肽。该制剂对P物质(SP)的C末端部分序列,尤其是SP-(6 - 11) 的敏感性高于对整个十一肽的敏感性。神经激肽的效力顺序如下:神经激肽B大于神经激肽A大于P物质。该制剂对蛙皮素和eledoisin也表现出高敏感性。在连续灌注的微浴槽中(系统1)或在用于离体平滑肌的普通浴槽中(系统2)对大鼠门静脉条进行的比较试验给出了相似的结果,并表明神经激肽B的肌otropic作用不受多种内源性物质拮抗剂以及花生四烯酸级联反应抑制剂的影响。目前的结果表明,神经激肽B通过激活特定受体使大鼠门静脉收缩,这些受体可能位于平滑肌膜上,与作为静脉活性刺激物的生物活性胺和肽的受体不同。神经激肽B的活性比神经激肽A高十倍,比P物质至少高一百倍。这种激动剂的效力顺序表明存在一种新的神经激肽受体类型,对神经激肽B特别敏感。