Wy 27569 is an orally active vascular selective calcium channel blocker that can effectively lower blood pressure. Wy 27569 is a thromboxane synthase inhibitor that can reshape prostaglandin balance, reduce pro thrombotic TXA2, and increase anti thrombotic PGI2. Wy 27569 can be used for research on cardiovascular diseases such as hypertension and angina.

MDL 27266 is an orally active NMDA receptor antagonist with neuroprotective effect. MDL 27266 is a broad-spectrum anticonvulsant agent.

Zocainone is an antiarrhythmic agent. Zocainone blocks sodium channels in cardiac tissue, stabilizing the cardiac action potential and reducing abnormal electrical activity. Zocainone is promising for research of cardiac arrhythmias.

T 588 is an orally active neuroprotective agent. T 588 can increase acetylcholine release from the frontal cortex and hippocampus and meliorate cognitive dysfunction. T 588 can protect cerebellar granule cells from glutamate neurotoxicity. T 588can be used for the research of neurological disease, such as Alzheimer's disease.

EVT-101 free base is a GluN2B antagonist. EVT-101 free base binds at the same GluN1/GluN2B dimer interface as Ifenprodil. EVT-101 free base inhibits calcium influx in chicken-derived cells, with an EC50 of 22 nM. EVT-101 can be used in the research of brain disorders.

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research.

AN-132 (phosphate) is an antiarrhythmic agent. AN-132 (phosphate) can inhibit Sodium Channel. AN-132 (phosphate) can prolong atrioventricular conduction time, decrease sinus rate and reduce the force of papillary muscle contraction. AN-132 (phosphate) can be used for the research of cardiovascular disease.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.

Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B.

ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.

ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders.

AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. AAG561 can be used for the study of the underlying emotion dysregulation of a mental disease or disorder.

YM 934 is a potassium channel opener. YM 934 inhibits neurogenic plasma leakage. YM 934 inhibits airway neurogenic inflammation.

(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a DHEA homolog. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide blocks the Shaker-related voltage-gated potassium channels. (S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide can inhibit the Kv1.2 K+ currents with an IC50 of 1.5 μM.

AU-1421 is a potassium ion (K⁺) site-directed regulator that specifically acts on various cation transport ATPases. AU-1421 can distinguish between two different K⁺-sensitive phosphorylation intermediate (E2P) states: for non-K⁺ transport type ATPases (such as the sarcoplasmic reticulum Ca²⁺-ATPase), after binding to AU-1421, it mimics the agonistic effect of K⁺, significantly accelerating the hydrolysis (dephosphorylation) of E2P. For K⁺ transport type ATPases (such as the gastric mucosa H⁺/K⁺-ATPase and the renal Na⁺/K⁺-ATPase), after binding to AU-1421, it inhibits the hydrolysis of E2P, stabilizing the phosphorylated intermediate, thereby blocking the ion transport cycle. AU-1421 can be used to study the mechanism of the potassium ion pump.

PD 175069 is a potent and selective N-type calcium channel antagonist with an IC50 of 0.32 μM. PD 175069 is efficacious in an audiogenic seizure model using DBA/2 mice. PD 175069 can be used for on neurological conditions such as neuropathic pain and stroke.

MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).

P-1060 is a potassium channel opener. P-1060 can be used for the research of cardiovascular disease.

Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.

4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.

Cholesteryl γ-aminobutyrate is a γ-aminobutyric acid (GABA)-mimetic prodrug. Cholesteryl γ-aminobutyrate inhibits the orthodromically-evoked discharge of pyramidal cells in the CA1 region of the hippocampus. Cholesteryl γ-aminobutyrate suppresses the open-field activity of mice and rats in a dose-dependent manner and inhibits Bicuculline-induced seizures in mice. Cholesteryl γ-aminobutyrate can be used for the study of CNS diseases related to impaired GABAergic neuronal function.

VU439 is a functionalized photoaffinity ligand of Elexacaftor). VU439 retains the activity of Elexacaftor as a CFTR corrector and can identify SCCPDH as a specific off-target of Elexacaftor through chemoproteomics.

Bastadins-5 is a potent stabilizer for the open state of RYR1. Bastadins-5 enhances Ca2+-induced Ca2+ release. Bastadins-5 can be used in research on central nuclear disease and malignant hypothermia.

Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM

CFTR Inhibitor II is a cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (< 1 min; 95% inhibition at 50 µM; Ki = 4.3 µM in CFTR-expressing FRT cells.

A novel Non-competitive AMPA/kainate antagonist.

A novel Non-competitive AMPA/kainate antagonist.

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.

Dizocilpine, a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

Ivacaftor (VX-770, Kalydeco) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively.