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alpha-2 adrenergic agonist
REVIEW Clonidine treats high blood pressure by stimulating a2 receptors in the brain, which decreases cardiac output and peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic a2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, and inhibits the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone. It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1-receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure.
Greene N, Fisk L, Naven RT, Note RR, Patel ML, Pelletier DJ (2010). Developing structure-activity relationships for the prediction of hepatotoxicity. Chem Res Toxicol. 19;23(7):1215-22. PMID 20553011.
Reitz, DJ; Piletz, JE (1997). The imidazoline receptor in control of blood pressure by clonidine and allied drugs. American Journal of Physiology 273 (5): R1569-R1571.
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