Pratiksha Institute of Pharmaceutical Sciences, Panikhaiti, Chandrapur Road, Guwahati, Assam, India.
Department of Pharmaceutical Chemistry, Shri Vishnu College of Pharmacy, Vishnupur (Affiliated to Andhra University), Bhimavaram, W.G. Dist., AP, India.
Curr Pharm Des. 2019;25(26):2792-2807. doi: 10.2174/1381612825666190716111245.
Adenosine mediates various physiological and pathological conditions by acting on its four P1 receptors (A1, A2A, A2B and A3 receptors). Omnipresence of P1 receptors and their activation, exert a wide range of biological activities. Thus, its modulation is implicated in various disorders like Parkinson's disease, asthma, cardiovascular disorders, cancer etc. Hence these receptors have become an interesting target for the researchers to develop potential therapeutic agents. Number of molecules were designed and developed in the past few years and evaluated for their efficacy in various disease conditions.
The main objective is to provide an overview of new chemical entities which have crossed preclinical studies and reached clinical trials stage following their current status and future prospective.
In this review we discuss current status of the drug candidates which have undergone clinical trials and their prospects.
Many chemical entities targeting various subtypes of P1 receptors are patented; twenty of them have crossed preclinical studies and reached clinical trials stage. Two of them viz adenosine and regadenoson are approved by the Food and Drug Administration.
This review is an attempt to highlight the current status, progress and probable future of P1 receptor ligands which are under clinical trials as promising novel therapeutic agents and the direction in which research should proceed with a view to come out with novel therapeutic agents.
腺苷通过作用于其四个 P1 受体（A1、A2A、A2B 和 A3 受体）来介导各种生理和病理状况。P1 受体的普遍存在及其激活，发挥了广泛的生物学活性。因此，其调节与帕金森病、哮喘、心血管疾病、癌症等各种疾病有关。因此，这些受体已成为研究人员开发潜在治疗药物的一个有趣目标。在过去几年中，已经设计和开发了许多分子，并评估了它们在各种疾病条件下的疗效。
主要目的是提供已通过临床前研究并进入临床试验阶段的新化学实体的概述，包括其当前状态和未来前景。
在这篇综述中，我们讨论了已进入临床试验阶段的候选药物的现状及其前景。
许多针对各种 P1 受体亚型的化学实体已获得专利；其中 20 种已通过临床前研究并进入临床试验阶段。其中两种，即腺苷和雷腺苷，已获得美国食品和药物管理局的批准。
本综述旨在强调目前处于临床试验阶段的 P1 受体配体的现状、进展和可能的未来，它们作为有前途的新型治疗药物，以及为了开发出新型治疗药物，研究应该进行的方向。
