Pinacidil

Description

Pinacidil is a peripheral vasodilator useful in the management of arterial hypertension of all degrees of seventy, usually in combination with a diuretic or beta-blocker. Preclinical evidence suggests that its hypotensive effect may be attributed to potassium channel activation.

Originator

Leo (Denmark)

The Uses of Pinacidil

Pinacidil Monohydrate is a K+ channel opener, used to induce relaxation of serotonin-produced contractions in porcine and human arterial rings. Vasodilator. Antihypertensive agent.

The Uses of Pinacidil

cardiac stimulant

The Uses of Pinacidil

Pinacidil monohydrate has been used:

• in repolarization studies by infusing into left anterior descending artery (LAD)
• to induce ATP-sensitive K⁺ (K_ATP) current in ventricular myocytes for electrophysiological studies
• as a KATP opener to treat myocardial cells

What are the applications of Application

Pinacidil monohydrate is a K+ channel activator

Definition

ChEBI: Pinacidil is an organic molecular entity.

brand name

Pindac (Leo).

Biochem/physiol Actions

Pinacidil is a KATP channel agonist. It protects cardiomyocytes by preventing loss of mitochondrial membrane potential. It prevents the caspase 3 activation in hypoxia/reoxygenation injury.

References

1) Hermsmeyer et al. (1988), Pinacidil actions on ion channels in vascular muscle; J. Cardiovasc. Pharmacol., 12(Suppl. 2) S17 2) Gollasch et al. (1995), Pinacidil relaxes porcine and human coronary arteries by activating ATP-dependent potassium channels in smooth muscle cells; J. Pharmacol. Exp. Therap., 275 681 3) Cohen & Kurz (1988), Pinacidil-induced vascular relaxation: comparison to other vasodilators and to classical mechanisms of vasodilation; J. Cardiovasc. Pharmacol., 12(Suppl. 2) S5 4) Teshima et al. (2003), Mitochondrial ATP-sensitive potassium channel activation protects cerebellar granule neurons from apoptosis induced by oxidative stress; Stroke, 34 1796 5) Xie et al. (2010), K(ATP) channel openers protect mesencephalic neurons against MPP+-induced cytotoxicity via inhibition of ROS protection; J. Neurosci. Res., 88 428 6) Zhang et al. (2008), Effects of ATP sensitive potassium channel opener on the mRNA and protein expressions of caspase-12 after cerebral ischemia-reperfusion in rats; Neurosci. Bull., 24 7