van den Brink Olivier W V, Delbridge Lea M, Rosenfeldt Franklin L, Penny Daniel, Esmore Donald S, Quick Deahne, Kaye David M, Pepe Salvatore
Cardiac Surgical Research Unit Melbourne, Australia.
Heart Lung Circ. 2003;12(3):178-87. doi: 10.1046/j.1444-2892.2003.00240.x.
Opiates have been used for thousands of years in the form of opium for relief of pain or fever and to induce sleep. However, it was only in the 1970s that the endogenous ligands for the opiate receptors were identified and termed opioid peptides. Opioid peptides activate G protein-coupled receptors in the central and autonomic nervous system, with marked effects on the regulation of pain perception, body temperature, respiration, heart rate and blood pressure. Cardiovascular regulatory effects of endogenous opioids were initially considered to originate from neural centres in the central nervous system, facilitating a regulatory role in neuro-transmission, as demonstrated by the presynaptic co-release from sympathetic neurones of norepinephrine with enkephalin or acetylcholine with enkephalin. However, opioid peptides of myocardial origin have also recently been shown to play a key role in local regulation of the heart. This brief review highlights the key features of the enkephalin opioids in the heart and the current understanding of their role in development, ageing, cardioprotection, hypertension, hypertrophy, and heart failure.
阿片类药物以鸦片的形式已被使用了数千年，用于缓解疼痛或发烧以及诱导睡眠。然而，直到20世纪70年代，阿片受体的内源性配体才被鉴定出来，并被称为阿片肽。阿片肽激活中枢和自主神经系统中的G蛋白偶联受体，对疼痛感知、体温、呼吸、心率和血压的调节有显著影响。内源性阿片类药物的心血管调节作用最初被认为起源于中枢神经系统的神经中枢，促进神经传递中的调节作用，如去甲肾上腺素与脑啡肽从交感神经元突触前共同释放，或乙酰胆碱与脑啡肽共同释放所证明的那样。然而，最近也表明心肌来源的阿片肽在心脏局部调节中起关键作用。这篇简短的综述强调了脑啡肽类阿片在心脏中的关键特征以及目前对它们在发育、衰老、心脏保护、高血压、肥大和心力衰竭中作用的理解。
