Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Cellular and Molecular Research Center, Research Institute for Health Development, Kurdistan University of Medical Sciences, Sanandaj, Iran; Neurosciences Research Center, Kurdistan University of Medical Sciences, Sanandaj, Iran.
Pharmacol Ther. 2019 Aug;200:69-84. doi: 10.1016/j.pharmthera.2019.04.007. Epub 2019 Apr 24.
Since the discovery of the histamine H receptor in 1983, tremendous advances in the pharmacological aspects of H receptor antagonists/inverse agonists have been accomplished in preclinical studies. At present, there are several drug candidates that reached clinical trial studies for various indications. However, entrance of these candidates to the pharmaceutical market is not free from challenges, and a variety of difficulties is engaged with their developmental process. In this review, the potential role of H receptors in the pathophysiology of various central nervous system, metabolic and allergic diseases is discussed. Thereafter, the current status for H receptor antagonists/inverse agonists in ongoing clinical trial studies is reviewed and obstacles in developing these agents are emphasized.
自 1983 年发现组胺 H 受体以来，在临床前研究中，H 受体拮抗剂/反向激动剂的药理学方面取得了巨大进展。目前，有几种候选药物已进入各种适应症的临床试验研究。然而，这些候选药物进入医药市场并非没有挑战，它们的开发过程中存在各种困难。在这篇综述中，讨论了 H 受体在各种中枢神经系统、代谢和过敏性疾病的病理生理学中的潜在作用。随后，回顾了正在进行的临床试验研究中 H 受体拮抗剂/反向激动剂的现状，并强调了开发这些药物的障碍。
