Agmatine suppresses peripheral sympathetic tone by inhibiting N-type Ca2+ channel activity via imidazoline I2 receptor activation

Kim, Young‐Hwan; Jeong, Ji-Hoon; Ahn, Dong-Won; Chung, Seungsoo

doi:10.1016/j.bbrc.2016.06.086

Cited by 7 publications

(1 citation statement)

References 37 publications

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“…The mechanism of this phenomenon is caused by expression on endothelial cells of I 1 R, phosphatidylinositolkinase (PI 3 K) activity of which leads to activation of eNOS (Joshi et al 2007;Maltsev et al 2013). It also matters that the activation of I 2 R can reduce the voltage-dependent activation of Ca 2+ -channels of neurons innervating the vessels (Kim et al 1999). Finally, the antihypertensive effect of imidazoline receptor agonists may be due to their nephroprotective and natriuretic activity (Smyth et al 1999, Elkomy et al 2018 (Fig.…”

Section: ) Effect On Vascular Tonementioning

confidence: 99%

Imidazoline receptors agonists: possible mechanisms of endothelioprotection

Солдатов¹,

Shmykova²,

Першина³

et al. 2018

RRP

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Imidazoline receptor agonists are one of the groups of contemporary antihypertensive drugs with the pleiotropic cardiovascular effects. In this review, the historical, physiological, pathophysiological aspects concerning imidazoline receptor agonists and possible mechanisms for their participation in endothelioprotection were considered. Illuminated the molecular biology of each subtype of imidazoline receptors and their significance in the pharmacological correction of cardiovascular disease. IR type 1 are localized in the brain nucleus, carrying out the descending tonic control of sympathetic activation, as well as in the endothelial cells of the vessels and kidneys. Their activation leads to a decrease in blood pressure, slowing the remodeling of the vascular wall and increasing sodium nares. IR type 2 is expressed predominantly in the adrenal gland, fat and muscle tissues. The physiological effects of their stimulation are associated with an increase in glucose utilization by peripheral tissues. IR type 3 are mainly present in pancreatic cells and are associated with the regulation of insulin secretion. Their stimulation leads to an increase in insulin liberation. Thus, IR agonists are able to improve endothelial function through various mechanisms, including blood pressure reduction, improvement in metabolic profile, and direct positive effects on the vascular wall. Current information on the pharmacological effects of this group compounds allows us to conclude that they are a promising group for correcting endothelial dysfunction and complications associated with it.

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