Overview of Antagonists Used for Determining the Mechanisms of Action Employed by Potential Vasodilators with Their Suggested Signaling Pathways

Abstract

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.

Mechanisms of Vasodilation Induced by Medicinal Plants: A Mini-Review

“…Endothelium-derived relaxing factors (EDRFs) as well as endothelium-derived contracting factors (EDCFs) elicit their vascular actions through interaction between the endothelium and vascular smooth muscle cells. 8 Responses elicited by endothelium-derived relaxing factors are usually studied, in vitro, in arterial rings precontracted with phenylephrine or noradrenaline. In endothelium-denuded rings, endothelium-dependent relaxation response to acetylcholine (Ach) is impaired.…”

“…In endothelium-denuded rings, endothelium-dependent relaxation response to acetylcholine (Ach) is impaired. 8,9 It has been extensively reported that in endothelium-intact rings, Ach-induced relaxation is completely reversed by NG-nitro-Larginine-methylester (L-NAME); a selective inhibitor of nitric oxide synthase. 1 In vascular tone regulation, both endothelium-derived relaxing factors (EDRFs) and endothelium-derived contracting factors (EDCFs) produce their effect via interaction between the endothelium and vascular smooth muscle cells.…”

“…Commonly used inhibitors include gandolinium, which inhibits SOCC and tharpsigargin, which inhibits SERCA. 8 Inhibition of the SERCA pump 25 results in an increase in intracellular Ca 2+ .…”

“…This is also associated with impaired ability of vessels to dilate. 7,8 Vasodilator drugs constitute a class of drugs commonly used in antihypertensive conditions. In this presentation, we discuss possible cellular mechanisms, based on experimental findings, by which some commonly used medicinal plants ameliorate blood pressure through vasodilator mechanisms involving relaxation of vascular smooth muscle.…”

Overview of the Microenvironment of Vasculature in Vascular Tone Regulation

“…However, before the vasculature-related research is carried out, the signaling mechanism pathways happening in the vasculature should be clearly understood. Previous reviews have shown that aortic ring assay is recommended as the “golden tool” in most of the in vitro pharmacological research, especially those related to vasculature, along with the protocols and suggested antagonists that are to be used for different mechanism studies [ 3 , 4 , 5 , 6 ].…”