potentials

Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. No activity at human mGlu1 receptors. Potentiates glutamate-induced calcium release with EC 50 of 60.1 nM.

Saclofen is a sulfonic analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that acts as a competitive antagonist of the GABAB receptor (IC50: 7.8 μM).1 This compound can be used to determine the functional roles for the GABAB receptor as

Helichrysetin has mild anti-HIV-1 PR activity. Helichrysetin has great potentials for development as an anticancer agent, it has cytotoxic effect on four selected cancer cell lines, A549, MCF-7, Ca Ski, and HT-29.

UCL 2077 is a subtype-selective blocker of the epilepsy-associated KCNQ channels and it also is a selective slow-afterhyperpolarization channel blocker,with IC50 of 500 nM in hippocampal neurons in culture, having minimal effects on Ca2+ channels, action potentials, input resistance, and the medium afterhyperpolarization.

4F 4PP oxalate is a 5-HT2A antagonist.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

Metipranolol (Betamann) is a type of β- Adrenergic receptors（ β- A potent antagonist of adrenergic receptor on guinea pig atria β 1- Adrenergic receptors and rat uterus β The 2-adrenergic receptor exhibited the beta blocking potentials (pA2) of 8.3 and 8.4, respectively. It is also a potent substituent in the 3H DHA binding assay, with a ligand concentration of 0.7 nM and a Ki of 39 ± 24 nM.

NMDAR antagonist 2 (compound 3I) is a blood-brain barrier permeable antagonist of NMDA receptors, exhibiting IC50 values of 4.42 μM and 214.75 μM at membrane potentials of -60 mV and 40 mV, respectively, for hGluN1 hGluN2A. This compound has been shown to mitigate hippocampal damage.

AUT2 is a Kv3.1 channel modulator with the potential to treat sensory hyperreactivity in patients with FXS by shifting the activation of high-threshold currents to more negative potentials. This shift reduces high-threshold K+ currents and increases low-threshold K+ currents in neurons, restoring wave IV of the ABR. Due to its ability to regulate neuronal excitability, AUT2 is also promising for the treatment of hearing impairments.

Rovatirelin (also known as S-0373) is a novel synthetic compound that mimics the action of thyrotropin-releasing hormone (TRH). This compound exhibits a higher affinity for human TRH receptors (Ki=702nM) compared to taltirelin (Ki=3877nM). In acutely isolated norepinephrine neurons of the rat locus coeruleus (LC), rovatirelin enhances the firing of spontaneous action potentials. Additionally, rovatirelin increases motor activity and may offer potential therapeutic benefits as an oral treatment for patients with SCD.

Gamma-DGG TFA is an antagonist of excitatory amino acids that can inhibit depolarization induced by NMDA, Kainate, and Quisqualate. In addition, it counteracts excitatory postsynaptic potentials (e.p.s.p.) in rat hippocampal slices.

Risotilide is a voltage-dependent potassium channel inhibitor. It can prolong cardiac action potentials and refractory periods.

AHR-12234 affects cardiac action potentials.

Chlordene, as a polychlorinated flame retardant, has bioaccumulation and biomagnification potentials.

Brevetoxin B is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. It binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Ajmaline hydrochloride is an alkaloid found in the root of Rauwolfia serpentina, and other plant sources. It is a class of Ia antiarrhythmic agent that apparently works by changing the shape and threshold of cardiac action potentials.

Vasicine is oxytocic and abortifacient agents.Vasicine, a potential natural cholinesterase inhibitor, has been in development for treatment of Alzheimer's disease. Vasicine can regulate the inflammatory reaction, have great potentials to develop safe medi

CT1-3 is a potent anti-cancer agent. CT1-3 regulates the JNK Bcl-2 Bax XIAP pathway, which induces mitochondria-mediated apoptosis. CT1-3 regulates the E-cadherin Snail axis to inhibit epithelial mesenchymal transition (EMT) potentials in human cancer cells (HCCs) and suppresses tumourigenesis. CT1-3 has anti-tumour effects in mouse models and does not show significant hepatotoxicity or nephrotoxicity.

Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent that reduces the maximum rate of phase 0 depolarization, increases the repolarization rate of phases 2 and 3, decreases the duration of action potentials, and shortens the effective refractory period.

Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current.

Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal slices. It protects against seizures induced by maximal electroshock (MES) in mice. Formulations containing phenytoin have been used in the treatment of tonic-clonic seizures and status epilepticus.

ProTx-II TFA is a potent and highly selective Nav1.7 sodium channel blocker, exhibiting an IC50 of 0.3 nM and demonstrating at least 100-fold selectivity over other sodium channel subtypes. It decreases channel conductance, shifts activation towards more positive potentials, and inhibits action potential propagation in nociceptors [1] [2].

Lotusine (hydroxide), a pure alkaloid isolated from the green seed embryos of Nelumbo nucifera Gaertn, influences action potentials in myocardial tissue and the slow inward current in cardiac Purkinje fibers [1].