6 products were found matching "Cay15030"!

Varenicline is a full agonist of alpha7 subunit-containing neuronal nicotinic acetylcholine receptors (nAChRs, EC50 = 18 µM) and a partial agonist of alpha4beta2 subunit-containing nAChRs (EC50 = 2.3 µM). Formulations containing varenicline have been used as aids in smoking cessation.Formal Name:...

Mibefradil is a general calcium channel blocker that shows modest selectivity for T-type channels over L-type channels (IC50 = 2.7 and 18.6 µM, respectively). It is a potent vasodilator, increasing coronary artery flow with an EC50 value of 54 nM. Mibefradil has minimal negative inotropic effects, supporting its use...

JSH-23 is an inhibitor of NF-kappaB, blocking its translocation into the nucleus (IC50 = 7.1 µM). It does not affect degradation of the inhibitor of NF-kappaB, IkappaB. JSH-23 interferes with NF-kappaB-mediated gene expression and apoptosis in RAW 264.7 cells treated with lipopolysaccharide. It has also been used to...

Cilostazol is a phosphodiesterase 3A (PDE3A) inhibitor (IC50 = 0.2 µM for the platelet enzyme). It is selective for PDE3A over PDE1, -2, -4, and -5 (IC50s = >5 µM for all). Cilostazol inhibits collagen- or ADP-induced aggregation of isolated rabbit platelets (IC50s = 29 and 31 µM, respectively). In vivo, cilostazol...

Ziprasidone is an atypical antipsychotic. It is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 36.31 nM for inhibition of forskolin-induced adenylate cyclase activity in HeLa cells expressing human receptors), as well as an inverse agonist of 5-HT1D receptors (IC50 = 2.69 nM) and a partial...

Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or...