CDN1163 is a SERCA2 allosteric activator. It increases Ca2+-ATPase activity and Ca2+ uptake by ER microsomes from obese mice. Rescues HEK cells from ER stress-induced cell death.
ML335 is a potent and selective TREK-1/2 Activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
AMPA Receptor Modulator-1 is a potent, oral active and selective AMPAR regulatory protein TARP γ-8 negative modulator with a pIC50 of 9.7, more selective over GluA1/γ-2 (pIC50=5).
LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC50 of 65 nM.
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively.
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
CLP290 is an orally available activator of the neuron-specific K+-Cl? cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications.
SN 6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor, and inhibits 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively.
Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization.
Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation.
Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current.
