Membrane Transporters-Ion Channels

Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.

E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr).

Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A.

Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.

Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.

GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.

(S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.

Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility.

Pilsicainide is a water soluble selective Na+ channel blocker.

NPPB is a chloride channel blocker (IC50 = 80 nM) that has also been identified as a GPR35 agonist.

PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.

PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.

HMR 1556, a chromanol derivative, is a IKs blocker with IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.

GAL-021 a new intravenous BKCa-channel blocker.

XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.