Naruse S, Yasui A, Kishida S, Kadowaki M, Hoshino M, Ozaki T, Robberecht P, Christophe J, Yanaihara C, Yanaihara N
Peptides. 1986;7 Suppl 1:237-40. doi: 10.1016/0196-9781(86)90192-0.
The effect of helodermin on vascular physiology was studied in anesthetized dogs using a synthetic replicate of helodermin and helodermin related peptides. Intraarterial infusion of helodermin caused a dose-dependent increase in femoral blood flow. Helodermin was 16 times less potent than VIP and 5 times more potent than PHM (human PHI). The helodermin effect lasted significantly longer; the half-life of the helodermin effect was 6.5 times longer than VIP. Synthetic helodermin (Hd) N-terminal fragment Hd(1-27)NH2 retained substantial activity similar to the full helodermin molecule but the prolonged effect was lost. Hd(7-35) and Hd(22-35) were inactive in this system. Intravenous injection of synthetic helodermin produced prolonged systemic hypotension and tachycardia; and, similar to VIP, it increased the common carotid arterial blood flow while those of the superior mesenteric and femoral arteries were decreased. The results demonstrate the VIP-like vasodilating activity and cardiovascular effects of helodermin in anesthetized dogs.
使用合成的海洛德明及其相关肽复制品，在麻醉犬身上研究了海洛德明对血管生理的影响。动脉内输注海洛德明可使股血流量呈剂量依赖性增加。海洛德明的效力比血管活性肠肽（VIP）低16倍，比胰高血糖素样肽（PHM，人胰高血糖素样肽I）高5倍。海洛德明的作用持续时间明显更长；海洛德明作用的半衰期比VIP长6.5倍。合成海洛德明（Hd）的N端片段Hd(1 - 27)NH2保留了与完整海洛德明分子相似的大量活性，但失去了延长的作用。Hd(7 - 35)和Hd(22 - 35)在该系统中无活性。静脉注射合成海洛德明可产生长时间的全身性低血压和心动过速；并且，与VIP相似，它增加了颈总动脉血流量，而肠系膜上动脉和股动脉的血流量减少。结果证明了海洛德明在麻醉犬身上具有类似VIP的血管舒张活性和心血管效应。
