Aisaka K, Hattori Y, Ishihara T, Morita M, Kasé Y, Miyata T
Jpn J Pharmacol. 1985 Apr;37(4):345-53. doi: 10.1254/jjp.37.345.
Piperidine is an endogenous active amine. Intravenous or intra-arterial administration of piperidine produced vasodilation in anesthetized dogs. The vasodilative effect of piperidine was inhibited by atropine (0.3 mg/kg, i.v.). In the hind limb perfusion experiment in anesthetized dogs, piperidine produced vasodilation, while it showed no vasorelaxing action in various isolated canine arterial strip preparations. These results suggest that the vasodilation caused by piperidine may be produced through activation of muscarinic receptors and that piperidine may act on smaller resistance blood vessels but not on large conductance vessels. In addition, pipecolic acid and N-methyl piperidine, the respective precursor amino acid and metabolite of piperidine, were almost inactive, but nipecotic acid was 1/4 to 1/10 times as active as piperidine as vasodilators. It is suggested that the non-substituted amine moiety of piperidine is very important for the manifestation of vasodilative activity and that piperidine might play a role in regulation of peripheral vascular circulation.
哌啶是一种内源性活性胺。静脉内或动脉内给予哌啶可使麻醉犬血管舒张。哌啶的血管舒张作用被阿托品(0.3毫克/千克,静脉注射)抑制。在麻醉犬的后肢灌注实验中,哌啶可引起血管舒张,而在各种离体犬动脉条制备中它未表现出血管舒张作用。这些结果表明,哌啶引起的血管舒张可能是通过激活毒蕈碱受体产生的,且哌啶可能作用于较小的阻力血管而非大的传导血管。此外,哌啶酸和N - 甲基哌啶,分别是哌啶的前体氨基酸和代谢产物,几乎无活性,但烟碱酸作为血管舒张剂的活性是哌啶的1/4至1/10倍。提示哌啶的未取代胺部分对于血管舒张活性的表现非常重要,且哌啶可能在外周血管循环调节中起作用。