P物质广泛分布于中枢、外周神经系统和某些组织,与痛觉、内脏传入和传出、炎症反应以及中枢对运动的调节均有密切关系。本文主要介绍P物质拮抗剂的构效关系、与受体结合的特性及其在中枢、外周神经系统 P 物质作用机理研究中的应用。P 物质拮抗剂的研究不仅可以为基础研究提供工具药,推进 P 物质作用机理的研究,而且可能发展成为新型的镇痛药和抗炎药。 Substance P is widely distributed in the central nervous system, peripheral nervous system and some tissues, and is closely related to the pain, visceral afferent and efferent, inflammatory reaction and the regulation of central to the movement. This article describes the structure-activity relationship of substance P antagonists, the characteristics of receptor binding and its application in the study of the mechanism of substance P in the central and peripheral nervous systems. Studies of substance P antagonists not only provide tools for basic research, promote the study of the mechanism of substance P, but also develop into new analgesics and anti-inflammatory drugs.