Douglas H, Kitchen I
Department of Biochemistry, University of Surrey, UK.
J Pharm Pharmacol. 1988 Sep;40(9):648-50. doi: 10.1111/j.2042-7158.1988.tb05328.x.
The cardiovascular effects of the four proenkephalin products [Met]-enkephalin (ME), [Leu]-enkephalin (LE), [Met]-enkephalyl-arg6phe7 (MEAP) and [Met]-enkephalyl-arg6-gly7-leu8 (MEAGL) have been studied on the isolated spontaneously beating rat atria and the perfused rat mesentery in-vitro. All four peptides (at concentrations up to 10(-6)M and in the presence of peptidase inhibitors) had no direct effect on atrial rate or contractility and did not alter responses to noradrenaline or field stimulation. In addition, the peptides had no effect on the perfusion pressure of the mesentery and did not alter vasoconstrictor responses to noradrenaline. The results show that proenkephalin products are without direct or modulating effects on atrial muscle or mesenteric vasculature of the rat, and suggest that there is no endogenous opioid control in these tissues.
已经在离体自发搏动的大鼠心房和体外灌注的大鼠肠系膜上研究了四种前脑啡肽产物——[甲硫氨酸]-脑啡肽(ME)、[亮氨酸]-脑啡肽(LE)、[甲硫氨酸]-脑啡肽-精氨酸6-苯丙氨酸7(MEAP)和[甲硫氨酸]-脑啡肽-精氨酸6-甘氨酸7-亮氨酸8(MEAGL)的心血管效应。所有这四种肽(浓度高达10⁻⁶M且存在肽酶抑制剂时)对心房率或收缩性均无直接影响,也不改变对去甲肾上腺素或场刺激的反应。此外,这些肽对肠系膜的灌注压力没有影响,也不改变对去甲肾上腺素的血管收缩反应。结果表明,前脑啡肽产物对大鼠心房肌或肠系膜血管系统没有直接或调节作用,提示这些组织中不存在内源性阿片样物质控制。