Departamento de Farmacología y Fisiología (Fisiología), Facultad de Veterinaria, Universidad de Zaragoza, Miguel Servet 177, Zaragoza, Spain.
Acta Pharmacol Sin. 2011 Apr;32(4):487-94. doi: 10.1038/aps.2010.227. Epub 2011 Mar 28.
To study the role of the tachykinin receptors in spontaneous contractions of longitudinal and circular smooth muscle from rabbit small intestine and to determine the mechanism of action of Substance P (SP).
Rabbit duodenum, jejunum and ileum segments were prepared. The spontaneous contractions of longitudinal and circular smooth muscle were recorded using a computer via an isometric force transducer. The specific agonists and antagonists of tachykinin receptors were added into the organ bath.
The agonists of tachykinin NK1 receptor (SP and [Sar9] SP), NK2 receptor (NKA and (β-Ala8)-NKA), and NK3 receptor (NKB and Senktide) all induced contractions in the small intestine. The contractions were diminished by NK1 receptor antagonist L-733,060, NK2 receptor antagonist GR-94800, and NK3 receptor antagonist SB 218795. Contractions caused by SP were also reduced by atropine, verapamil, PKC inhibitor staurosporine, and PLC inhibitor U73122.
Ttachykinin NK1, NK2, and NK3 receptors mediate the contractions of the smooth muscle in rabbit intestine. Furthermore, SP acts directly on smooth muscle cells through the tachykinin NK1 receptor.
研究速激肽受体在兔小肠纵行和环形平滑肌自发性收缩中的作用,并确定 P 物质(SP)的作用机制。
制备兔十二指肠、空肠和回肠段。通过等长力换能器,使用计算机记录纵行和环形平滑肌的自发性收缩。向器官浴中加入速激肽受体的特定激动剂和拮抗剂。
速激肽 NK1 受体(SP 和 [Sar9] SP)、NK2 受体(NKA 和(β-Ala8)-NKA)和 NK3 受体(NKB 和 Senktide)的激动剂均引起小肠收缩。这些收缩被 NK1 受体拮抗剂 L-733,060、NK2 受体拮抗剂 GR-94800 和 NK3 受体拮抗剂 SB 218795 减弱。SP 引起的收缩也被阿托品、维拉帕米、PKC 抑制剂 staurosporine 和 PLC 抑制剂 U73122 减弱。
速激肽 NK1、NK2 和 NK3 受体介导兔肠平滑肌的收缩。此外,SP 通过速激肽 NK1 受体直接作用于平滑肌细胞。