Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions[1].
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats[1].
NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity[1].
Neomycin sulfate is an aminoglycoside antibiotic used for preventing or treating bacterial infections.
Ethyl dirazepate is a drug which is a benzodiazepine derivative. It has anxiolytic and hypnotic and possibly other characteristic benzodiazepine properties.
Glycine-1-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
Propofol-d17 (2,6-Diisopropylphenol-d17) is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic[1].
Vm24-toxin is a toxin peptide that can be isolated from the Mexican scorpion Vaejovis mexicanus smithy. Vm24-toxin is an inhibitor of Kv1.3 potassium channel[1].
Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide[1].
CyPPA is a positive modulator of hSK3 and hSK2, with EC50 values of 14 μM and 5.6 μM, repectively. CyPPA is inactive on both hSK1 and hIK channels[1][2].
AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively[1]. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response[2].
ASP 2905 (ASP2905) is a novel potent, selective, orally bioavailable inhibitor of voltage-gated potassium channel KCNH3 with IC50 of 9.0 nM; displays minimally bound with low affinities to 55 transmembrane proteins; decreases the frequency of spontaneous inhibitory postsynaptic currents in cultured rat hippocampal neurons at 0.1-1 uM; reverses the disruption of spontaneous alternation behavior induced by MK-801 and scopolamine in mice, and ameliorates the cognitive deficits of aged rats. Alzheimer Disease Phase 1 Discontinued
Uldazepam is a benzodiazepine derivative and can be used to treat patients with anxiety syndromes as tranquilizer.
Epoxylathyrol, an epoxylathyrane derivative isolated from the Euphorbia boetica, is a P-glycoprotein (P-gp) inhibitor. Epoxylathyrol is a P-gp-mediated multidrug resistance (MDR) reverser[1][2].
Bullatine A (BLA), a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A (BLA) is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses[1].Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed[2].
XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.IC50 value: 3 nMTarget: NaV1.7in vitro: XEN907 shows a further 10-fold increase in potency, represents a promising structure for further optimization efforts. XEN907 shows no significant activity at 10 μM against a broad panel of 63 receptors and transporters. Determination of the ADME properties of XEN907 reveals that XEN907 is not cytotoxic and has favourable hepatocyte metabolic stability for both human and dog, although inhibition of CYP3A4 is observed in a recombinant human enzyme assay.[1]in vivo: Pharmacokinetic analysis in rats of XEN907 demonstrates that, consistent with the compound's ADME parameters, the compound is modestly bioavailable. Following an initial rapid absorption phase (oral Tmax = 20 min), XEN907 is extensively distributed (Vss 600-fold higher than the plasma volume in rats) and rapidly cleared. [1]
Glycine-13C2 is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
SR33805 is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca2+ channels. SR33805 can be used for the research of acute or chronic failing hearts[1][2].
Luseogliflozin (TS 071) hydrate is a selective potent and orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor with an IC50 of 2.26 nM. Luseogliflozin hydrate can be used for the research of type 2 diabetes mellitus (T2DM)[1][2].
TWIK-1/TREK-1-IN-1 (compound 2a) is an inhibitor of the TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.36 μM and 14.6 μM, respectively, and has antidepressant-like effects[1].
Chlormethiazole is an potent and orally active GABAA agonist[1]. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus[2].
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist[1]. CNQX disodium blocks the expression of fear-potentiated startle in rats[5].
Ethacizine hydrochloride (Ethacizin; NIK-244) is a longer-lasting Class Ic antiarrhythmic agent than Flecainide[1]. Ethacizine hydrochloride (Ethacizin; NIK-244) inhibits the depolarizing current responsible for the intraatrial and His-Purkinje-ventricular conduction[2].
LOE 908 hydrochloride is a non-selective cation channel (NSCC) inhibitor[1].
Lercanidipine. (R)- is an enantiomer of antihypertensive drugs Lercanidipine. Lercanidipine acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels.
Tracazolate hydrochloride (ICI 136753 hydrochloride) is a potent GABAA receptor modulator. Tracazolate hydrochloride potentiates α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) in a concentration-dependent manner. Tracazolate hydrochloride has the potency (EC50) is determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2].
Ertugliflozin (PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[1]. A drug for the treatment of type 2 diabetes mellitus[2].
Dalazatide (ShK-186) is a Kv1. 3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease[1][2].