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| Pinacidil Basic information |
| Product Name: | Pinacidil | | Synonyms: | Pinacidil monohydrate (Synonyms: Pinacidil hydrate);Pinacidil monohydrate (Pinacidil hydrate);(+/-)-N-Cyano-N'-4-pyridinyl-N''-(1,2,2-trimethylpropyl)guanidine;Pinacidil;Hndac;(±)-N-Cyano-N’-4-pyridinyl-N’’-(1，2，2-trimethylpropyl)guanidine monohydrate;Guanidine, N-cyano-N'-4-pyridinyl-N''-(1,2,2-trimethylpropyl)-, monohydrate;Pinacidil Hydrate | | CAS: | 85371-64-8 | | MF: | C13H19N5.H2O | | MW: | 263.34 | | EINECS: | 622-053-4 | | Product Categories: | INOCOR | | Mol File: | 85371-64-8.mol |
| Pinacidil Chemical Properties |
| Melting point | 164-165° | | storage temp. | RT | | solubility | ethanol: 14 mg/mL | | form | solid | | pka | pKa 空 (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) |
| 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) |
| 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. | | 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+ (KATP) current in ventricular myocytes for electrophysiological studies
- as a KATP opener to treat myocardial cells
| | Uses | cardiac stimulant | | 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 |
| Pinacidil Preparation Products And Raw materials |
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