Traxoprodil mesylate (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
Org 25543 hydrochloride is a selective and irreversible GlyT2 inhibitor (IC50: 16 nM). Org 25543 hydrochloride has analgesia effect. Org 25543 hydrochloride ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice[1][2][3].
NHE3-IN-3 (Compound 1) is a Na+/H+ exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats[1].
FCPT is an ATP competitive kinesin-5 inhibitor.
Isopimaric acid is a potent opener of large conductance calcium activated K+ (BK) channels.
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.IC50 Value: 7.1 nM at V(H) = -40 mV [1]Target: calcium channelin vitro: Both clevidipine and nitroglycerin completely reversed U46619-induced contraction (clevidipine (50% effective concentration [EC50] = 3.88 +/- 0.84 x 10(-6) mol/L, nitroglycerin EC50 = 4.84 +/- 2.76 x 10(-8) mol/L) [2]. A decrease in temperature increased the half-life of clevidipine in blood, whereas dilution of the blood did not affect the in vitro half-life of clevidipine. The albumin concentration affected the hydrolysis rate of clevidipine in RBC suspended with saline [3].in vivo: Clevidipine is a high-clearance drug with a relatively small volume of distribution, resulting in an extremely short half-life in all species studied. The median initial half-life of the individual value (Bayesian estimates) is 12, 20, and 22 s in the rabbit, rat, and dog, respectively [4]. The extremely high clearance value and the small volume of distribution resulted in short half-lives of clevidipine, 2.2 and 16.8 min, respectively. The blood concentration and dose rate producing half the maximal effect (i.e. EC50 and ED50) were approximately 25 nM and 1.5 microg/kg/min, respectively [5].Clinical trial: CARVE: Clevidipine for Vasoreactivity Evaluation of the Pulmonary Arterial Bed. Phase 4
CXL-1020 is a hydroxylamine-based nitroxyl (HNO) donor. CXL-1020 improves cardiac inotropy/lusitropy and Ca2+ cycling in rats with abnormal relaxation. CXL-1020 induces vasorelaxation and improves cardiac function in canine models. CXL-1020 has been used to research systolic heart failure and stable heart failure[1].
Propoxycaine hydrochloride is the hydrochloride salt form of Propoxycaine, a para-aminobenzoic acid ester with local anesthetic activity.Target: sodium channelPropoxycaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. This results in a loss of sensation.
Carboxyamidotriazole (L 651582; CAI) is a blocker of non-voltage dependent calcium channel[1]. Carboxyamidotriazole (L 651582; CAI) is a non-cytotoxic anti-tumor drug, which also shows anti-inflammatory activity[2].
Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria[1].
Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain[1][2][3].
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection[1]. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling[2].
Mephenesin is an NMDA receptor antagonist, is a centrally acting muscle relaxant.Target: NMDA receptor
Fengabine is a GABAergic antidepressant drug. Fengabine can be used for the research of depression[1].
V-116517 is a novel potent, selective, oral bioavailable TRPV1 antagonist with IC50 of 35.1 nM; shows high selectivity for TRPV1 over TRPV3 and TRPV4 (>10 uM) in a panel of 66 ion channels, receptors, transporters; dose-dependently reverses thermal hyperalgesia with ED50 of 2 mg/kg (p.o.) in acute inflammatory CFA model; shows excellent aqueous solubility, metabolic stability, oral bioavailability in multiple species, and excellent efficacy in a variety of animal pain models. Pain Phase 2 Clinical
TRPV1 antagonist 5 (compound 1) is a potent TRPV1 antagonist[1].
PD0176078 is a newly found N-type Calcium channel blocker.
α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases[1].
L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.Target: NMDA ReceptorL-701324 is a potent, active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents. L-701324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia. L-701324 (2.5-40 mg/kg, i.p.) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg, i.p.).
Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
Glycine-1-13C 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.
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively[1].
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily. PF-05105679 is used for clinical efficacy in cold-related pain[1].
CNQX (FG9065) is a potent AMPA/kainate receptor antagonist.
A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
(+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.
Lubiprostone(SPI-0211;RU0211) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation.Target: OthersLubiprostone is a bicyclic fatty acid derived from prostaglandin E1 that acts by specifically activating ClC-2 chloride channels on the apical aspect of gastrointestinal epithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase motility, and promote spontaneous bowel movements (SBM). From Wikipedia.
ADCI, a noncompetitive NMDA antagonist, is a broad-spectrum anticonvulsant agent[1].
Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD+) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy[1][2].