KATP channel opener

Mitochondria KATP channels Cardiac KATP channel opening has a role in myocardial preconditioning, a paradoxical form of cardioprotection wherein brief ischemic episodes can protect the heart from subsequent lethal ischemic injury. Openers including BMS-180448 and BMS-191095 have been reported to possess preferential cardioprotective effects over vasorelaxant effects by activating mitochondria KAXP channels. 

Novel classes of Katp channel openers have been claimed to be useful in the management of pain and migraine (Mogensen et al. (Novo Nordisk), 1999 Carroll et al., (Abbott), 2000-2001). 

Katp channel openers seem to stimulate the release of endogenous opioids... 

Indeed, using the same experimental approach (i.e. i.c.v. administration of KAtp channel openers and blockers) it was shown that supraspinal KAtp channels are also involved in producing antinociceptive effects of several other classes of analgesic substances (Table 1). The KAtp channels involved in supraspinal antinociception are not... 

Asano, T., Dohi, S., lida, H. Antinociceptive action of epidural KATP channel openers via interaction with morphine and an a2-adrenergic agonist in rats, Anesthesia and Analgesia 2000, 90, 1146-1151. 

A series of 3-(alkylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1 -dioxides (168a-j) that are related to diazoxide (396) (a compound which induces hyperglycemia in vivo through decreased insulin secretion and is a potent pancreatic KATP channel opener) and pinacidil (397) were prepared and tested as inhibitors of insulin release from rat pancreatic islets. Of the compounds tested, BPDZ 44 (168g) was chosen for further study as a potential probe for KATP channels. The compounds tested were the most powerful inhibitors of insulin release reported at that time <93JMC32li>. 

O. Oldenburg, S.D. Critz, M.V. Cohen and J.M. Downey, Acetylcholine-induced production of reactive oxygen species in adult rabbit ventricular myocytes is dependent on phosphatidyl inositol 3 and Src-ki-nase activation and mitochondrial KATP channel opening, J. Mol. Cell. Cardiol. 35,653-660 (2003). 

AMI, acute myocardial infarction PTCA, percutaneous transluminal coronary angioplasty CABG, coronary artery bypass graft HF, heart failure LV, left ventricular Niconradil is a KATp channel opener ... 

Fedorov, V.V., Glukhov, A.V., Ambrosi, C.M., Kostecki, G., Chang, R., Janks, D., Schuessler, R.B., Moazami, N., Nichols, C.G., and Efimov, I.R. (2011) Effects of KATP channel openers diazoxide and pinacidil in coronary-perfused atria and ventricles from failing and non-failing human hearts. J. Mol. Cell. Cardiol. 51, 215-225. 

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