Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current[1][2].
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].
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].
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].
UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM[1].
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].
Somatostatin-28 (1-12) is a somatostatin fragment that is monitored in brain tissue to track processing of somatostatin.
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].
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.
Nialamide is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class that was used as an antidepressant.
A2A receptor antagonist 1 is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively[1]. 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage[2].
(E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model[1].
Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].
Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
A Zn2+-dependent pan-inhibitor of class I and class II HDACs with a long half-life (12h) in vivo; significantly enhances the migration of astrocytes and accelerates wound repair more effectively than SAHA and VPA; up-regulates the expression of NGF, phospho-TrkA, p-AKT, NF-κB, and Bcl-2, while down-regulates the expression of p75 NTR, phospho-JNK, and Bax.
6-Epiagarotetrol is a neuroprotective agent can be extracted from Aquilaria sinensis. 6-Epiagarotetrol has a protective effect on corticosterone-induced PC12 cell damage[1].
ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation[1][2].
Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia[1].
MDA 19 is a selective human CB2 receptor agonist with Ki of 43.3 nM. IC50 Value: 43.3 nM(Ki)Target: CB2 receptorin vitro: MDA19 displayed 4-fold-higher affinity at the human CB(2) than at the human CB1 receptor (K(i) = 43.3 +/- 10.3 vs 162.4 +/- 7.6 nM) and nearly 70-fold-higher affinity at the rat CB2 than at the rat CB1 receptor (K(i) = 16.3 +/- 2.1 vs 1130 +/- 574 nM). In guanosine triphosphate (GTP)gamma[(35)S] functional assays, MDA19 behaved as an agonist at the human CB1 and CB2 receptors and at the rat CB1 receptor but as an inverse agonist at the rat CB2 receptor. In 3',5'-cyclic adenosine monophosphate (cAMP) assays, MDA19 behaved as an agonist at the rat CB1 receptor and exhibited no functional activity at the rat CB(2) receptor. In extracellular signal-regulated kinases 1 and 2 activation assays, in vivo: MDA19 behaved as an agonist at the rat CB2 receptor. MDA19 attenuated tactile allodynia produced by spinal nerve ligation or paclitaxel in a dose-related manner in rats and CB2(+/+) mice but not in CB2(-/-) mice, indicating that CB2 receptors mediated the effects of MDA19. MDA19 did not affect rat locomotor activity.
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2)[1][2].
Neuromedin B (NMB) is a member of Bombesin (BN)-like peptide family in mammals.
Celaphanol A is a diterpene that can be isolated from the root bark of Celastrus orbiculatus. Celaphanol A shows neuroprotective effect against a hydrogen peroxide-induced cytotoxicity in PC12 cells[1].
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.