Pinacidil Chemical Properties

Melting point:

164-165°

storage temp. 

RT

solubility 

ethanol: 14 mg/mL

form 

solid

pka

pKa (Uncertain)

color 

white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.

CAS DataBase Reference

85371-64-8(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-36/37/38

Safety Statements 

36

WGK Germany 

3

Toxicity

LD50 in mice, rats (mg/kg): 600, 570 orally (Petersen, 1978)

MSDS

• Language:English Provider:Pinacidil

Pinacidil Usage And Synthesis

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.

Chemical Properties

Crystalline, melting point 164-165°C. Acute toxicity LD50 mice, rats (mg/kg): 600, 570 oral.

Originator

Leo (Denmark)

Uses

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

Uses

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

Uses

cardiac stimulant

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 R K. Pinacidil actions on ion channels in vascular muscle.[J]. Journal of Cardiovascular Pharmacology, 1988, 12 Suppl 2: S17-22. DOI:10.1097/00005344-198812002-00005
[2] M GOLLASCH. Pinacidil relaxes porcine and human coronary arteries by activating ATP-dependent potassium channels in smooth muscle cells.[J]. Journal of Pharmacology and Experimental Therapeutics, 1995, 275 2: 681-692.
[3] M. COHEN K K. Pinacidil-induced vascular relaxation: comparison to other vasodilators and to classical mechanisms of vasodilation.[J]. Journal of Cardiovascular Pharmacology, 1988, 12 Suppl 2 1: S5-9. DOI:10.1097/00005344-198812002-00003
[4] YASUSHI TESHIMA. Mitochondrial ATP-sensitive potassium channel activation protects cerebellar granule neurons from apoptosis induced by oxidative stress.[J]. Stroke, 2003, 34 7: 1796-1802. DOI:10.1161/01.str.0000077017.60947.ae
[5] K(ATP) channel openers protect mesencephalic neurons against MPP+-induced cytotoxicity via inhibition of ROS protection
[6] HONG ZHANG. Effects of ATP sensitive potassium channel opener on the mRNA and protein expressions of caspase-12 after cerebral ischemia-reperfusion in rats.[J]. Neuroscience bulletin, 2008, 24 1: 7-12. DOI:10.1007/s12264-008-1227-7

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