nrcms

Zonisamide (AD 810) 是锌酶碳酸酐酶 (carbonic anhydrase) 的有效抑制剂，对人类线粒体同工酶 hCA II 和 hCA V 作用的 Ki 值分别为 35.2 nM 和 20.6 nM。Zonisamide 具有抗癫痫活性，在癫痫、癫痫发作和帕金森病的研究中具有价值。

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases in the spontaneous beating of NRCMs.3,4 1.Schwarz, D., Kisselev, P., Ericksen, S.S., et al.Arachidonic and eicosapentaenoic acid metabolism by human CYP1A1: Highly steroselective formation of 17(R), 18(S)-epoxyeicosatetraenoic acidBiochem. Pharmacol.67(8)1445-1457(2004) 2.Lauterbach, B., Barbosa-Sicard, E., Wang, M.H., et al.Cytochrome P450-dependent eicosapentaenoic acid metabolites are novel BK channel activatorsHypertension39(2 Pt. 2)609-613(2002) 3.Falck, J.R., Wallukat, G., Puli, N., et al.17(R),18(S)-Epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: Structure-activity relationships and stable analoguesJ. Med. Chem.54(12)4109-4118(2011) 4.Arnold, C., Markovic, M., Blossey, K., et al.Arachidonic acid-metabolizing cytochrome P450 enzymes are targets of omega-3 fatty acidsJ. Biol. Chem.285(43)32720-32733(2010)

19R(20S)-EpDPA is an oxylipin and a metabolite of docosahexaenoic acid .1,2It is formed from DHA by various cytochrome P450 (CYP) isoforms in a stereoselective manner.219R(20S)-EpDPA (30 nM) prevents calcium-induced increases in the spontaneous beating of isolated neonatal rat cardiomyocytes (NRCMs).3 1.Cinelli, M.A., Yang, J., Scharmen, A., et al.Enzymatic synthesis and chemical inversion provide both enantiomers of bioactive epoxydocosapentaenoic acidsJ. Lipid Res.59(11)2237-2252(2018) 2.Lucas, D., Goulitquer, S., Marienhagen, J., et al.Stereoselective epoxidation of the last double bond of polyunsaturated fatty acids by human cytochromes P450J. Lipid Res.51(5)1125-1133(2010) 3.Burke, J.E., and Dennis, E.A.Phospholipase A2 structure/function, mechanism, and signalingJ. Lipid Res.50(Suppl)S237-S242(2009)