Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca2+ oscillations in cardiomyocytes.

Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats.

AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits KATP channels.

Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.

Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B 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.

Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.

Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.

3-Methyl-GABA is an activator of GABA aminotransferase with anticonvulsant activity.

PF-06305591 dihydrate 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.

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.

Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.

PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.

TTA-A2 is a potent, selective and orally active t-type voltage gated calcium?channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.

QAQ dichloride, a photoswitchable voltage-gated Nav and Kv channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC50 of 61 nM.

Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.

NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively.

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.

Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator.

(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.

Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death.

TPC2-A1-P is a powerful membrane-permeant Na+-selective two-pore channel 2 (TPC2) agonist. TPC2-A1-P activates a Na+ current and promotes endosome fusion with the plasma membrane. TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.

Chlorahololide C, a lindenane sesquiterpenoid dimer, is isolated from Chloranthus holostegius. Chlorahololide C is a potent and selective potassium channel blocker, with an IC50 of 3.6 μM.

L-DAB HBR (L-DABA, L-2,4-Diaminobutyric acid) is an of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity.

SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at theα+/γ- subunit interface.

Cyclic ADP-ribose ammonium (cADPR ammonium) is a potent second messenger for calcium mobilization that is synthesized from NAD+ by an ADP-ribosyl cyclase. Cyclic ADP-ribose ammonium increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.

sFTX-3.3 is a Ca2+ channel antagonist with IC50s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.

SSD114 is a novel GABAB positive allosteric modulator.

Pregabalin

Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.