RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect[1][2][3].
RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research[1][2][3][4].
Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs[1].
GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease[1].
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.IC50 value:Target: α4β2 nAChRVarenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms Varenicline(CP 526555; Champix; Chantix) can assist some patients to quit smoking.
Agalloside is a neural stem cell differentiation activator that can be found in Aquilaria agallocha[1].
4-O-Methylbutein is a phenolic glucoside that can be isolated from Elsholtzia ciliata.4-O-Methylbutein exhibits neuroprotective effects against glutamate-induced HT22 cell death with an EC50 of 35.2 μM[1].
Tetraethylammonium chloride is a non-selective potassium channel blocker. Tetraethylammonium chloride is a good substrate for organic cation transporter (OCTN1). Tetraethylammonium chloride antitumor properties[1][2].
Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR)[1][2].
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively[1][2].
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research[1].
L-Stepholidine (Stepholidine), an alkaloid extract of the Chinese herb Stephania intermedia, is the first compound known to exhibit mixed dopamine D1 receptor agonist/D2 antagonist properties. L-Stepholidine (Stepholidine) has neuroprotective effect and inhibits heroin-induced reinstatement. L-Stepholidine (Stepholidine) is a potential medication for the treatment of opiate addiction[1][2][3].
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist[1]. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment[2][3][4].
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05)[1][2].
Danshenxinkun D is an anti-Alzheimer's disease (AD) candidate. Danshenxinkun D can significantly reverse the expression of PSEN1 and DRD2 mRNA in H2O2 treated PC12 cells. Danshenxinkun D can be used in the study of anti-Alzheimer's disease product candidate [1].
DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system[1][2][3].
c-ABL-IN-2 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-2 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2020260871A1, compound 25)[1].
PF-4778574 is a positive allosteric modulation of AMPA receptor with EC50 of 45 to 919 nM in differenct cells.
(3S,4R)-PF-6683324 is a tropomyosin-related kinase (Trk) inhibitor extracted from patent WO2015092610A1 example 9. (3S,4R)-PF-6683324 has the potential for the research of pain and cancer[1].
WT-TTR inhibitor 1 (Compound 21) is a wild-type Transthyretin (WT-TTR) inhibitor with 29.05% inhibition at 100 μM[1].
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer's disease and Parkinson's disease[1].
CZC-25146 Hcl is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases(PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.
Sunifiram (DM-235) is a piperazine derived ampakine-like drug which has nootropic effects in animal studies with significantly higher potency than piracetam.IC50 value: Target: in vitro: DM 232 and DM 235 are novel antiamnesic compounds structurally related to ampakines. The involvement of AMPA receptors in the mechanism of action of DM 232 and DM 235 was, therefore, investigated in vivo and in vitro. Both compounds (0.1 mg/kg i.p.) were able to reverse the amnesia induced by the AMPA receptor antagonist NBQX (30 mg/kg i.p.) in the mouse passive avoidance test. At the effective doses, the investigated compounds did not impair motor coordination, as revealed by the rota rod test, nor modify spontaneous motility and inspection activity, as revealed by the hole board test [1]. In mouse hippocampal slices, sunifiram at 10-100 nM significantly enhanced LTP in a bell-shaped dose-response relationship which peaked at 10 nM. The enhancement of LTP by sunifiram treatment was inhibited by 7-chloro-kynurenic acid (7-ClKN), an antagonist for glycine-binding site of NMDAR, but not by ifenprodil, an inhibitor for polyamine site of NMDAR [2].in vivo: OBX mice were administered once a day for 7-12 days with sunifiram (0.01-1.0 mg/kg p.o.) from 10 days after operation with or without gavestinel (10 mg/kg i.p.), which is glycine-binding site inhibitor of N-methyl-d-aspartate receptor (NMDAR) [3].
HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research[1].
(RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
Carbamazepine-d8 is the deuterium labeled Carbamazepine. Carbamazepine, a sodium channel blocker, is an anticonvulsant drug, with an IC50 of 131 μM[1][2].
C-DIM12 is a synthetic Nurr1 activaor induces Nurr1 and DA gene expression in cell lines and primary neurons.Target: Nurr1in vitro: C-DIM12 as a modulator of Nurr1 activity that results in inhibition of NF-κB-dependent gene expression in glial cells by stabilizing nuclear corepressor proteins, which reduces binding of p65 to inflammatory gene promoters. C-DIM12 Decreases Inflammatory Gene Expression in BV-2 Microglia. C-DIM12 Decreases Expression of NF-κB-Enhanced GFP Expression in Human Embryonic Kidney 293 Reporter Cells.[1] C-DIM12 increases protein levels of exogenously expressed human Nurr1 in transfected neurons.C-DIM12 protects neurons from 6-hydroxydopamine toxicity. [2]
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels[1].
α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR[1].