GR3027 (Golexanolone) is a GABA-A receptor modulating steroid antagonist that selectively antagonizes the enhanced activation of GABAA receptors by neurosteroids such as allopregnanolone and THDOC.

GlyT1 inhibitor 46 is a novel potent, selective, orally available inhibitor of glycine transporter-1 (GlyT1) with IC50 of 38 and 21 nM for rat and human GlyT1, respectively.

Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog.

Flupirtine maleateis a non-opioid, centrally acting analgesia, muscle relaxation and neuroprotection. Currently under a clinical trial (recruiting phase) as a treatment for Multiple Sclerosis and has been used as an analgesic.

Flumazenil(Ro 15-1788) is a benzodiazepine antagonist, non-selective for α1, α2, α3 or α5-containing GABAA receptors.

Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 and 1,600 nM for cockroach and rat receptors, respectively).

Evans Blue is a potent inhibitor of the uptake of L-glutamate into synaptic vesicles, also an AMPA/kainate receptor antagonist

Emamectin Benzoate works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.

Dronedarone is a Class III antiarrhythmic and a multi-channel blocker for atrial fibrillation. It blocks potassium and sodium and is a calcium channel protein inhibitor.

Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.

Diltiazem HCl (Tiazac)

Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.

Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm. Dantrolene sodium is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction.

Dantrolene sodium hemiheptahydrate is a skeletal muscle relaxant which acts by blocking muscle contraction beyond the neuromuscular junction. Dantrolene sodium hemiheptahydrate is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ fro

CTDP-32476 is a potent and selective dopamine transporter (DAT) inhibitor and a competitive inhibitor of cocaine binding to the DAT with Ki of 12 nM.

CP 465022 hydrochloride is a selective GluR (AMPA) antagonist which is non-competitive.

CNS 7056 is a new short-acting sedative/anaesthetic that acts on GABAA receptors in the brain.

Citalopram hydrobromide is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has US FDA approval to treat major depression.

Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.

CGP37849 is a potent, selective and competitive NMDA receptor antagonist (Ki = 35 nM). Anticonvulsive following oral administration in vivo.

CFM-2 is a selective non-competitive AMPAR antagonist.

Cariporide is a selective Na+/H+ exchanger isoform 1 (NHE1) inhibitor (IC50 values are 0.05, 3 and 1000 μM for NHE1, NHE3 and NHE2 respectively).

BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.

Bamaquimast is an inhibitor of proton pump extracted from patent US2005165041, example 138.

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.

Azosemide (Azosemidum) is a potent Na-K-Cl Cotransporter NKCC1 with IC50 of 0.246 and 0.197 uM for hNKCC1A and NKCC1B, being about 4-times more potent than bumetanide.

Azimilide 2Hcl(NE-10064 2Hcl) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.

AZD9056 is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.

Atomoxetine Hcl(LY 139603; Tomoxetine Hcl) is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).