HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor with a ki of 2.01 μM[1].
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces Aβ1-42 accumulation.
L-Kynurenine-d4-1 is deuterium labeled L-Kynurenine. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta. 1,3,5,8-Tetrahydroxyxanthone has antispasmodic effect and anti-inflammatory activity[1].
SB 206553 is a potent and selective 5-HT2B/5-HT2C receptor antagonist with pA2 of 8.89 for rat 5-HT2B, pKi of 7.92 for human 5-HT2C, displays >80-fold selectivity over other 5-HT receptor subtypes; exhibits anxiolytic-like properties both in vitro and in vivo. Anxiety Discontinued
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile[1].
Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
Hexamethonium is a non-depolarising ganglionic blocker, a nicotinic nACh (NN) receptor antagonist.Target: nAChRHexamethonium is a non-depolarising ganglionic blocker, a nicotinic nACh receptor antagonist that acts in autonomic ganglia by binding mostly in or on the NN receptor, and not the acetylcholine binding site itself. It does not have any effect on the muscarinic acetylcholine receptors (mAChR) located on target organs of the parasympathetic nervous system but acts as antagonist at the nicotinic acetylcholine receptors located in sympathetic and parasympathetic ganglia (NN). Hexamethonium bromide is a nicotinic acetyl choline receptor antagonist. Induces apoptosis and inhibits the stimulatory effect of nicotine on endothelial cell DNA synthesis and proliferation. Hexamethonium bromide hydrate is an inhibitor of AChR α3 [1-3].
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity[1][2].
Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM)[1]. Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity[2]. Shows effect on the serotonergic system[3].
UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM[1].
Paeonol is an active extraction from the root of Paeonia suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively.
GK60 is a carboxyl nicotine hapten that can be used in the study of nicotine dependence[1].
TUG-905 is a potent GPR40 agonist with an pEC50 value of 7.03. TUG-905 increases hypothalamic cell proliferation and survival. TUG-905 reduces body mass and increases the POMC mRNA expression[1][2].
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation[1][2].
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS[1][2].
13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle[1].
Somatostatin-28 (1-12) is a somatostatin fragment that is monitored in brain tissue to track processing of somatostatin.
3-MATIDA is a metabolic glutamate 1 (mGlu1) receptor antagonist. 3-MATIDA alleviates neuronal death in cerebral ischemia models. 3-MATIDA can be used in the study of neuronal injury and epileptiform activity after ischemia [1].
Vitamin E, an essential nutrient for humans and animals reproduction, is a lipid-soluble antioxidant. Vitamin E can protect lipids against oxidative stress, and rescue the glutathione (GSH) depletion-induced hypersensitivity of cells to H2O2. Supplementation with Vitamin E increases its levels in cerebrospinal fluid and plasma, as well as reduces Aβ levels, thus beneficially influences oxidative stress in Alzheimer's disease. Vitamin E also has anti-aging effects[1][2][3][4].
Mito-apocynin (C2), an orally active mitochondria-targeted triphenylphosphonium (TPP)-based compound, is synthesized by conjugating the Apocynin moiety with a TPP + cation. Mito-apocynin (C2) exhibits antineuroinflammatory effect[1].
Somatostatin is a tetradecapeptide which can suppress the growth hormone (GH) secretion and control the pituitary hormone secretion in human CNS.
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug[1].
TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors. IC50 value: 7.5 μMTarget: serotonin 5-HT2B receptorin vitro: TG6-10-1, an analog of TG4-155 (a prostaglandin receptor EP2 antagonist, with a relatively short plasma half-life (0.6 h) and low brain:plasma ratio (0.3) after systemic administration in mice), which has a superior pharmacokinetic profile making it suitable for more extensive testing. TG6-10-1 had negligible effect on a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s > 10 μM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 μM. At a high concentration (10 μM), TG6-10-1 had little or no effect on the enzymatic activity of COX-1 (7% inhibition) and COX-2 (14% inhibition), and inhibited the leukotriene B4 (LTB4) receptor BLT1 by 1% .EP2 receptor activation by PGE2 stimulates adenylate cyclase to elevate cytoplasmic cAMP level. TG6-10-1 has a competitive mechanism of antagonism of the EP2 receptor with an equilibrium dissociation constant for the antagonist-receptor complex (KB) of 17.8 nM.in vivo: TG6-10-1 displayed a plasma half-life of 1.6 h and a brain:plasma ratio of 1.6 after systemic administration (5 mg/kg, i.p.) in mice. A significant increase in survival was observed in post-SE mice that received TG6-10-1 compared with those in the vehicle group. Administration of TG6-10-1 improved 1-wk survival from 60 to 90% after SE.
Enecadin is a neuroprotective agent extracted from patent US 8623823 B2.
Isogarciniaxanthone E (compound 1) is a natural product that can be found in Garcinia xanthochymus. Isogarciniaxanthone E enhances nerve growth factor-mediated neurite outgrowth[1].
Milnacipran (1S-cis) hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI), used in the clinical treatment of fibromyalgia.
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
MPTP hydrochloride is a brain penetrant dopamine neurotoxin, inducing Parkinson’s Disease.