Tramontana M, Maggi C A, Evangelista S
Pharmacology Department, Istituto Farmacobiologico Malesci S.p.A., Firenze, Italy.
Jpn J Pharmacol. 1994 Jul;65(3):281-3. doi: 10.1254/jjp.65.281.
The effect of activation of tachykinin NK2-receptors on gastrointestinal propulsion was studied in vivo in conscious rats. The selective NK2-receptor agonist [beta Ala8]NKA-(4-10) produced an atropine-resistant specific increase of the small intestinal transit measured by the charcoal method. This effect was restricted to the small intestine since gastric emptying was not affected by [beta Ala8]NKA-(4-10). The newly developed polycyclic peptide NK2-receptor antagonist MEN 10,627 produced a dose-dependent inhibition of this stimulated transit. The spasmolytic effect of MEN 10,627 was highly selective because it did not affect stimulated intestinal transit induced by equieffective doses of carbachol and reserpine. These findings indicate that MEN 10,627 is a valuable tool for assessing the role of NK2-receptors in intestinal propulsive activity.
在清醒大鼠体内研究了速激肽NK2受体激活对胃肠推进的影响。选择性NK2受体激动剂[β丙氨酸8]神经激肽A（4-10）通过炭末法使小肠转运产生了阿托品抵抗性的特异性增加。这种作用仅限于小肠，因为胃排空不受[β丙氨酸8]神经激肽A（4-10）的影响。新开发的多环肽NK2受体拮抗剂MEN 10,627对这种刺激的转运产生剂量依赖性抑制。MEN 10,627的解痉作用具有高度选择性，因为它不影响等效应剂量的卡巴胆碱和利血平诱导的刺激小肠转运。这些发现表明，MEN 10,627是评估NK2受体在肠道推进活动中作用的有价值工具。
