SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease[1].
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
Trimetozine is an orally active sedative. Trimetozine has mild tranquilizing effects. Trimetozine can be used for the research of anxiety[1][2][3].
Traxoprodil (CP101,606) is a potent and selective NMDA antagonist and protect hippocampal neurons with an IC50 of 10 nM.
GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD)[1].
Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity[1][2].
L-Glutamic acid monosodium salt (Monosodium glutamate) is an activator of mGlu1 receptor.
YMRF-NH2 is a neuropeptide. YMRF-NH2 binds to FMRFa-R with an EC50 value of 31 nM[1][2].
IEM-1754, a dicationic adamantane derivative, is a potent blocker of open channels of native ionotropic glutamate receptors including quisqualate-sensitive receptors in insect muscles, NMDAR in cultured rat cortical neurons, and AMPAR in freshly isolated hippocampal cells. IEM-1754 shows anticonvulsant potency in vivo[1][2].
Methocarbamol-d3 is the deuterium labeled Methocarbamol. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
Votoplam is a gene splicing modulator, used to inhibit Huntington's disease[1].
Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.Target: 5HT4 Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastro-oesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).In addition to its prokinetic properties, mosapride also exerts anti-inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects. Mosapride also promotes neurogenesis in the gastrointestinal tract which may prove useful in certain bowel disorders. The neurogenesis is due to mosapride's effect on the 5-HT4 receptor where it acts as an agonist.Its common side effects include dry mouth, abdominal pain, dizziness, headache, insomnia, malaise, nausea, diarrhoea and sometimes constipation. Unlike some other prokinetic agents, mosapride has little effect on potassium channels, no effect on hERG transfected cells, and no effect on cardiovascular function that could be detected in tests on humans. Due to the pharmacokinetics of mosapride, it would take 1,000 - 3,000 times the therapeutic dose to elicit cardiovascular effects.
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.
β-Amyloid (22-35) is a 14-aa peptide, shows aggregates and induces neurotoxicity in the hippocampal cells.
7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice[1][2][3].
Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A inhibitor.
MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research[1].
SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity[1][2][3].
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research[1].
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases[1].
ST91 is a α2-adrenoceptor (α2AR) agonist. ST91 activates both α2AAR and non-α2AAR subtypes to produce spinal antinociception[1][2][3].
β-Amyloid (1-38), mouse, rat is composed of 38 aa (1-38 residues of the Aβ peptide) and is the primary component of the amyloid plaques of Alzheimer’s disease[1].
Demoxepam is a major metabolite of Chlordiazepoxide. Demoxepam exhibits cytotoxicity activity against cancer cell lines. Demoxepam has anticonvulsant and anxiolytic effects[1][2].
Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity[1].
Dimethadione is the primary metabolite of trimethadione. Dimethadione causes depression of neuromuscular transmission. Dimethadione primarily decreases transmitter release from the nerve terminal[1].
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1][2].
LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics[1].
Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system[1].
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95[1][2].