Hökfelt Tomas, Bartfai Tamas, Bloom Floyd
Department of Neuroscience, Karolinska Institute, Stockholm, Sweden.
Lancet Neurol. 2003 Aug;2(8):463-72. doi: 10.1016/s1474-4422(03)00482-4.
The role of peptides as signalling molecules in the nervous system has been studied for more than 30 years. Neuropeptides and their G-protein-coupled receptors are widely distributed throughout the body and they commonly occur with, and are complementary to, classic neurotransmitters. The functions of neuropeptides range from neurotransmitter to growth factor. They are present in glial cells, are hormones in the endocrine system, and are messengers in the immune system. Much evidence indicates that neuropeptides are of particular importance when the nervous system is challenged (eg, by stress, injury, or drug abuse). These features and the large number of neuropeptides and neuropeptide receptors provide many opportunities for the discovery of new drug targets for the treatment of nervous-system disorders. In fact, receptor-subtype-selective antagonists and agonists have been developed, and recently a substance P receptor (neurokinin 1) antagonist has been shown to have clinical efficacy in the treatment of major depression and chemotherapy-induced emesis. Several other neuropeptide receptor ligands are in clinical trials for various indications.
肽作为神经系统中的信号分子，其作用已被研究了30多年。神经肽及其G蛋白偶联受体广泛分布于全身，它们通常与经典神经递质共存并相互补充。神经肽的功能范围从神经递质到生长因子。它们存在于神经胶质细胞中，是内分泌系统中的激素，也是免疫系统中的信使。大量证据表明，当神经系统受到挑战时（例如，受到压力、损伤或药物滥用），神经肽尤为重要。这些特性以及大量的神经肽和神经肽受体为发现治疗神经系统疾病的新药物靶点提供了许多机会。事实上，已经开发出了受体亚型选择性拮抗剂和激动剂，最近一种P物质受体（神经激肽1）拮抗剂已被证明在治疗重度抑郁症和化疗引起的呕吐方面具有临床疗效。其他几种神经肽受体配体正在针对各种适应症进行临床试验。
