S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the treatment of aging-related memory disturbances.

PPPA is a competitive NMDA receptor antagonist that displays moderate selectivity for NR2A-containing receptors.

PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin.

Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM.

GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates.

FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception.

CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABAAreceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo.

A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.

17-PA is a selective antagonist of neurosteroid potentiation and direct gating of GABAA receptors.

(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist.

IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo.

Fenoverine is an antispasmodic drug and inhibits calcium channel currents. Fenoverine induces rhabdomyolysis.

MRS4738 is a potent and high affinity P2Y14R antagonist. MRS4738 exhibits anti-hyperallodynic and antiasthmatic activity in vivo.

QNZ is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).

Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).

Rapastinel(GLYX-13) is a NMDA receptor partial agonist that acts at the glycine site.

Retigabine 2Hcl (Ezogabine; D23129) is a Kv7.2-7.5 (KCNQ2-5) neuronal potassium channel opener witrh anticonvulsant activity.

Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension.

RQ-00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively).

SKF96365 is blocker of TRP cation channels. Inhibits capacitative Ca2+ entry.

STF-31 is an inhibitor of GLUT1 (IC50 = ~1 µM) that blocks glucose uptake.

TAK-438 is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion.

Traxoprodil is an NMDA ε 2 (NR2B) antagonist that has been studied as an alternative to serotonin selective reuptake inhibitors.

TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

Valspodar(PSC833) is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR).

Verinurad is an urate transporter inhibitor with EC50 value of 0.05 μM.Verinurad is useful in the modulation of blood or serum uric acid levels, reducing serum uric acid levels in a human.

VX-809 is a CFTR modulator with EC50 of 0.1 μM.

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.