Blank M A, Brown J R, Hunter J C, Bloom S R, Tyers M B
Eur J Pharmacol. 1986 Dec 16;132(2-3):155-61. doi: 10.1016/0014-2999(86)90600-x.
The pharmacological effects of peptide histidine isoleucine (PHI), glucagon and secretin were compared with vasoactive intestinal polypeptide (VIP) on rabbit urethra and anococcygeus muscle. VIP and PHI dose-dependently inhibited induced contractions of both smooth muscle preparations. Cross-tachyphylaxis between VIP and PHI was demonstrated in the urethra preparation, suggesting that their activity is mediated via a common receptor or second messenger. Glucagon and secretin were without effect on either preparation. Radioimmunoassays demonstrated substantial concentrations of VIP and PHI in both urethra and anococcygeus tissue extracts. These observations suggest that PHI is an additional candidate together with VIP to mediate relaxation of rabbit urethra and anococcygeus muscle. When compared with VIP, Gila monster venom was found to inhibit both smooth muscle preparations, producing concentration-response curves parallel to those produced by VIP.
将肽组氨酸异亮氨酸(PHI)、胰高血糖素和促胰液素的药理作用与血管活性肠肽(VIP)对兔尿道和肛门尾骨肌的作用进行了比较。VIP和PHI剂量依赖性地抑制两种平滑肌制剂的诱发性收缩。在尿道制剂中证实了VIP和PHI之间的交叉快速耐受性,表明它们的活性是通过共同的受体或第二信使介导的。胰高血糖素和促胰液素对两种制剂均无作用。放射免疫分析表明,尿道和肛门尾骨肌组织提取物中存在大量的VIP和PHI。这些观察结果表明,PHI与VIP一起是介导兔尿道和肛门尾骨肌松弛的另一个候选物质。与VIP相比,发现吉拉毒蜥毒液可抑制两种平滑肌制剂,产生与VIP产生的浓度-反应曲线平行的曲线。