Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H+, K+- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases[1].
μ-Conotoxin-CnIIIC is a 22-residue conopeptide that can be isolated from Conus consors. μ-Conotoxin-CnIIIC is a potent and persistent blocker of NaV1.4 channel. μ-Conotoxin-CnIIIC has analgesic, anaesthetic and myorelaxant properties[1][2].
AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC50 of 0.5 nM.
(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
Fenoverine is an antispasmodic drug and inhibits calcium channel currents[1]. Fenoverine induces rhabdomyolysis[2].
Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist[1].
PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1[1].
Chloralose is widely used in neuroscience and veterinary medicine as an anesthetic and sedative.
ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
Ranolazine-d8 (CVT 303-d8) is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 µM, 0.71 µM, 0.6 μM, and 0.98 µM, respectively[1].
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors[1].
Optovin is a reversible photoactive TRPA1 activator; stimulates human TRPA1 channels in vitro and enables repeated photoactivation of motor behaviors in wild-type zebrafish (EC50 = 2 μM).IC50 value:Target: in vitro: Optovin is a rhodanine-containing small molecule with no previously annotated biological activity. Whereas DMSO-treated animals do not respond to photic stimuli, optovin-treated animals respond to light with vigorous motor excitation at an EC50 of 2 μM. Optovin-treated animals respond to 387 nm (violet) stimuli, but not to 485 nm (blue), 560 nm (green) or longer wavelengths. optovin strongly activated 33% (35/105) of DRG neurons. optovin acts on a molecular target expressed in mustard oil responsive mammalian DRG sensory neurons; perhaps on TRPA1 itself. TrpA1 is necessary for the optovin response [1].in vivo: Optovin also elicited nociceptive behaviors in adult mice. optovin shows activity on adult animals in vivo, and may be preferable to conventional TRPA1 ligands for achieving high-resolution spatiotemporal control.
YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions[1].
Tilapertin is an oral inhibitor of glycine transporter type-1 (GlyT1).
Concanamycin A (Antibiotic X 4357B; Concanamycin; X 4357B) is a macrolide antibiotic and a specific vacuolar type H+-ATPase (V-ATPase) inhibitor[1].
α-Conotoxin PeIA is an analgesic α-conotoxin.α-Conotoxin PeIA inhibits the α6β4, α9α10 and α3β2 nAChR.α-Conotoxin PeIA is also a potent inhibitor of N-type calcium channel via GABAB receptor activation[1][2][3].
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM. IC50 Value: 1.5 uM ( inhibit TBARS, LOOH and FPL formation)[1]in vitro: It was found that 10 uM amiodarone induces accumulation of ethidium bromide (5 ug/ml) in Saccharomyces cerevisiae cells. At the same time, in yeast cells with inactivated MDR genes, accumulation of ethidium bromide was 6-fold higher even without amiodarone. Addition of non-lethal concentrations of amiodarone to MDR-deficient cells caused an increase of intracellular ethidium bromide to the level, which was even lower than the level in amiodarone-treated wild-type cells [2]. Cells treated with amiodarone were seen to have detached from the dish, with cell rounding, cytoplasmic blebbing and irregularity in shape. An increase in the sub-G1 phase fraction, from 15.43 to 21.34% and 79.83% and a reduction in the G1 phase fraction, from 48.83 to 41.63% and 11.52%, were observed in cells treated with amiodarone at concentrations of 0.1 and 1 mM, respectively [3].in vivo: Chronic treatment with oral amiodarone for 4 weeks reduced i.p. when myocytes were dialyzed with patch-pipettes containing either 10 mM Na+ or 80 mM Na+. In myocytes from untreated rabbits, acute exposure to amiodarone in vitro reduced i.p. when patch pipettes contained 10 mM Na+ but had no effect on i.p. at 80 mM Na+. Amiodarone had no effect on the voltage dependence of the pump or the affinity of the pump for extracellular K+ either after chronic treatment or during acute exposure [4].Clinical trial: Continuous Versus Episodic Amiodarone Treatment for the Prevention of Permanent Atrial Fibrillation . Phase not specified
WS-3 is an agonist of TRPM8 with an EC50 of 3.7 μM.
Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina treatment[1][2][3].
Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. Dihydrokainic acid also shows epileptogenic effects[1].
NSC-609249 hydrochloride is an impurity of Verapamil (HY-14275). Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor[1][2].
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response[1][2].
GYKI 52466 is a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11 μM, respectively), GYKI 52466 can be used for the research of neurological disorders, such as Parkinson's disease[1].
Vanzacaftor is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR) for treating cystic fibrosis.
Cycleanine is a potent vascular selective Calcium antagonist. Cycleanine has analgesic, muscle relaxant and anti-inflammatory activities. Cycleanine has potential for anti-ovarian cancer acting through the apoptosis pathway[1][2].
Alpidem selectively binds to α1β2γ2 subunit-containing GABAA receptor with an IC50 of 17 nM and exerts anxiolytic effect[1].
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels[1].
8-Azido-ATP, a photoreactable nucleotide analog, is useful for the identification of proteins, such as DNA-dependent RNA polymerase[1].
GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant[1].