Loh Yean Chun, Tan Chu Shan, Ch'ng Yung Sing, Ahmad Mariam, Asmawi Mohd Zaini, Yam Mun Fei
School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800 Minden, Penang, Malaysia.
Molecules. 2016 Apr 15;21(4):495. doi: 10.3390/molecules21040495.
This paper is a review on the types of antagonists and the signaling mechanism pathways that have been used to determine the mechanisms of action employed for vasodilation by test compounds. Thus, we exhaustively reviewed and analyzed reports related to this topic published in PubMed between the years of 2010 till 2015. The aim of this paperis to suggest the most appropriate type of antagonists that correspond to receptors that would be involved during the mechanistic studies, as well as the latest signaling pathways trends that are being studied in order to determine the route(s) that atest compound employs for inducing vasodilation. The methods to perform the mechanism studies were included. Fundamentally, the affinity, specificity and selectivity of the antagonists to their receptors or enzymes were clearly elaborated as well as the solubility and reversibility. All the signaling pathways on the mechanisms of action involved in the vascular tone regulation have been well described in previous review articles. However, the most appropriate antagonists that should be utilized have never been suggested and elaborated before, hence the reason for this review.
本文是一篇综述，内容涉及拮抗剂的类型以及用于确定受试化合物血管舒张作用机制的信号传导机制途径。因此，我们详尽地回顾并分析了2010年至2015年间发表在PubMed上的与此主题相关的报告。本文的目的是提出与机制研究中涉及的受体相对应的最合适的拮抗剂类型，以及为确定受试化合物诱导血管舒张所采用的途径而正在研究的最新信号通路趋势。文中还包括了进行机制研究的方法。从根本上说，明确阐述了拮抗剂对其受体或酶的亲和力、特异性和选择性，以及溶解度和可逆性。先前的综述文章已经对血管张力调节作用机制中的所有信号通路进行了详尽描述。然而，此前从未有人提出并阐述过应使用的最合适的拮抗剂，因此才有了本综述。
