currents

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator that enhances hERG currents by slowing inactivation, promoting activation, reducing inactivation, and shortening atrial and ventricular repolarization in a complex manner.

NS-102 is a glutamate receptor and NMDA receptor antagonist that inhibits erythrocyanine (GluK2), which reduces glur6 receptor-mediated currents, and inhibits specific binding to the glur6 receptor.

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

Devapamil (Devapamilo) is a phenylalkylamine that blocks L-type calcium currents from the inner side of membrane cells in a use-dependent manner.

VU625 (VU007625) is a selective and potent AeKir1 inhibitor (IC50: 96.8 nM) that acts as a mosquito killer and inhibits AeKir1-mediated currents.

AZD-1305 is a novel anti-arrhythmic compound that primarily blocks the fast component of IKr, l-type calcium currents and intra-ward sodium currents in mammalian cells and ventricular cardiomyocytes and can be used in studies to reverse arrhythmias.

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Quinidine hydrochloride monohydrate is an optical isomer of quinine, extracted from the bark of the Cinchona tree and similar plant species. It prolongs cellular action potential and decreases automaticity. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.

Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

Clonixin (Clonixic acid) is a non-steroidal anti-inflammatory drug (NSAID) with analgesic properties. This compound has been reported to block prostaglandin synthesis, and to block inward calcium currents.

Spermidine (N-(3-Aminopropyl)-1,4-diaminobutane) inhibits NOS1 (nNOS). Spermidine binds and precipitates DNA and may be used for purification of DNA binding proteins. Spermidine activates PNK (polynucleotide kinase T4). Spermidine binds to and activates NMDA and has been shown to potentiate NMDA-induced currents in a concentration-dependent manner.

1-Octanol, a saturated fatty alcohol, functions as an inhibitor of T-type calcium channels (T-channels), showing an inhibitory concentration (IC50) of 4 μM for native T-currents[1]. Additionally, 1-Octanol is recognized for its potential as a biofuel, possessing diesel-like properties[2].

Oxodipine, a dihydropyridine-type calcium antagonist, inhibited KCl-induced aortic contraction in rabbits and reduced cardiac force in less potent rat ventricular test-paper contractions. In rat cultured neonatal ventricular myocytes, Oxodipine reduced L-type Ca currents (I) with an IC of 0.24 μM, and against T-type Ca currents (I) with an IC of 0.41 μM. Oxodipine causes constipation in mice and gingival hyperplasia in dogs.

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist, effectively and reversibly inhibiting currents through human, rat, and mouse TRPV4 orthologs with IC50 values of 486 nM, 133 nM, and 17 nM, respectively.

CGP 78608 hydrochloride is a specific antagonist at the glycine binding site of the NMDA receptor (IC50 = 6 nM). CGP 78608 hydrochloride exhibits anticonvulsant activity. CGP 78608 hydrochloride potentiates GluN1/GluN3A-mediated glycine currents (estimated EC50 = 26.3 nM).

10Panx Acetate is a mimetic inhibitory peptide that readily and reversibly inhibits the panx1 currents.

Pep2m, myristoylated acetate is a Cell-permeable, myristoylated form of pep2m. Peptide inhibitor of the interaction between the C-terminus of the GluA2 (AMPA receptor) subunit and N-ethylmaleimide-sensitive fusion protein (NSF), a protein that regulates A

ALX-1393 is a selective GlyT2 inhibitor that effectively reduces neuronal action potential activity in a concentration-dependent manner and inhibits the activity of spontaneous networks by inducing glycinergic tetanic currents in the abdominal horn of the spinal cord. Antiinjurious effects on thermal, mechanical and chemical stimuli in rat models of acute pain.

ORM-10103 is a novel potent and selective inhibitor of the Na+/Ca2+ exchanger (NCX).ORM-10103 inhibited NCX currents with estimated IC50 values of 55 and 67 nM at -80 and 20 mV, respectively, and reduced early and delayed postdepolarization in canine hearts.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

T16Ainh-A01 is a potent inhibitor of TMEM16A Chloride channel, inhibiting TMEM16A-mediated chloride currents (IC50 of 1 µM),and functions as a calcium-activated chloride channel (CaCC).

Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s: 2.7 μM and 18.6 μM for T-type and L-type currents).

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

GABAA receptor antagonist that binds the picrotoxin site and stabilizes the inactive form of the channel via allosteric interaction. Accelerates the decay of GABA-induced Cl- currents with little effect on peak amplitude. Also inhibits 5-HT3A receptors via a similar mechanism.

1-BCP (Piperonylic acid piperidide) is a centrally active drug that modulates AMPA receptor-gated currents.

Benzolamide (CL 11366) inhibits carbonic anhydrase effectively and low-threshold calcium currents in hippocampal pyramidal neurons.

Tipepidine hydrochloride is a reversible inhibitor of dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) (IC50: 7.0 μM), with antidepressant-like effect.

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.

VU 0546110, a selective inhibitor of the sperm-specific potassium channel SLO3 (IC50= 64 μM), demonstrates 40-fold selectivity over SLO1. It effectively blocks both heterologous SLO3 currents and endogenous K+ currents, inhibiting sperm hyperpolarization and preventing hyperactivated mobility.

DPNB-ABT 594 is a nitrobenzyl-caged ABT 594, a selective α4β2 nAChR agonist. One-photon uncaging evokes large inward currents and Ca2+transients on cell bodies and dendrites of medial habenular neurons in mouse brain slices. Two-photon uncaging induces fast nAChR-mediated currents. Photolyzed with high quantum yield of 0.20. Effective photolysis occurs using one- or two-photon excitation; one-photon uncaging requires illumination at 410 nm for 1.5-3 ms; two-photon uncaging requires illumination with appropriate two photon pulse laser at 710 nm for ~2 ms.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

Ambocin is a natural product from Pueraria mirifica. Ambocin blocks Ba2+ currents through CaV1.2 channels (IBa1.2) in a concentration-dependent manner and increases IKCa1.1.

Potent and selective μ opioid receptor antagonist (Ki values are 0.96 and >10,000 nM for μ and δ receptors respectively). Causes behavioral effects on central administration in vivo. Also increases K+ currents in rat locus ceruleus neurons in vitro via a

Potent and reversible Kv3.4 potassium channel blocker (IC50 = 47 nM); also attenuates inactivation of sodium currents by acting on Nav1.7 and Nav1.3 channels. Enhances TTX-sensitive sodium currents in rat small dorsal root ganglion neurons. Neuroprotective.

Potent rat Nav1.7, human Nav1.4 and rat Nav1.6 channel activator (EC50 values are 7, 10 and 47 nM, respectively). Exhibits minimal activation at mammalian Nav1.2, Nav1.3 and Nav1.5 (EC50 values >3 μM). Inhibits fast inactivation on all channels. Increases

Tamapin TFA, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small conductance Ca(2+)-activated K(+) (SK) channels, particularly the SK2 subtype (Potassium Channel). It is known to inhibit SK channel-mediated currents in the hippocampal pyramidal neurons.

(D(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, serving as an oxytocin receptor antagonist, effectively nullifies the augmentation of inhibitory postsynaptic currents in CA1 pyramidal neurons by oxytocin [1].

DPI-201-106 is a cardioselective inhibitor of the TTX-resistant h1 Na channel inactivation. DPI-201-106 inhibits the L-type calcium current, and inward and delayed rectifier potassium currents.

SYM2206 is a low affinity non-competitive AMPA receptor antagonist with an IC50 value of 1.6 μM.SYM2206 exhibits anticancer activity by blocking Nav1.6-mediated sustained currents and decreasing the survival of pancreatic cancer cells.

Mibefradil dihydrochloride (Ro 40-5967 (dihydrochloride)) is an blocker of calcium channel with moderate selectivity for T-type Ca2+ channels (T-type and L-type currents with IC50s of 2.7 μM and 18.6 μM, respectively).

5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4

Azemiopsin, a potent inhibitor of the nicotinic acetylcholine receptor (nAChR), demonstrates half maximal inhibitory concentrations (IC50s) of 0.18 μM for T. californica nAChR and 22 μM for human α7 nAChR. Moreover, it effectively blocks acetylcholine-induced currents in Xenopus oocytes that heterologously express human muscle-type nAChR [1].

Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877).

Ambroxol-d5 is intended for use as an internal standard for the quantification of ambroxol by GC- or LC-MS. Ambroxol is an expectorant and active metabolite of bromhexine. It decreases short-circuit currents in electrically stimulated isolated canine tracheal epithelial cells when applied submucosally. Ambroxol decreases IL-13-induced production of mucin 5AC (MUC5AC) in primary human airway epithelial cells and inhibits IL-13-induced decreases in the mucociliary transport rate of endogenous particles in the same cells. Ambroxol increases phenol red secretion, a marker of expectorant activity, in mice when administered at doses of 30, 60, or 120 mg/kg. Formulations containing ambroxol have been used in the treatment of acute or chronic respiratory conditions.

TRPV1-Tat, a peptide antagonist targeting transient receptor potential vanilloid 1 (TRPV1), is composed of amino acids 736-745 derived from TRPV1's A-kinase anchor protein (AKAP)-binding domain, combined with the HIV Tat-derived cell-penetrating peptide sequence. At a concentration of 200 µM, TRPV1-Tat effectively inhibits heat or phorbol 12-myristate 13-acetate (PMA014)-induced currents in primary mouse dorsal root ganglia via whole-cell patch-clamp assays. Additionally, when administered at dosages of 10 or 30 µM, it elevates the mechanical pain threshold in the hind paws of rats.

(R)-(+)-Bay-K-8644 is a Ca2+ channel and dihydropyridine agonist that inhibits Ba2+ currents (IBa), induces central respiratory depression in cats, and inhibits platelet activation through competitive antagonism of thromboxane A2-prostaglandin H2 receptors.