Neuroscience

<p>Aβ aggregation-IN-1 (Compound 1b) is an inhibitor of amyloid-beta precursor protein. It suppresses the aggregation and disaggregation of amyloid-beta fibrils with IC50 values of 3.92 and 7.19 M, respectively. Additionally, Aβ aggregation-IN-1 reduces malondialdehyde formation in neuronal cells, increases intracellular levels of reduced glutathione (GSH), and inhibits caspase 3.</p>

<p>(E)-CHBO4 is an MAO-B inhibitor with an IC50 value of 0.023 μM, making it a potential candidate for research into Parkinson's disease treatment.</p>

Designed anti-Alzheimer’s compound; potent Glutaminyl Cyclase inhibitor; IC50 at 4.5 nM; reduces brain Aβ; improves cognition.

SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It

<p>Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM).</p>

LY2794193, a potent and selective mGlu3 receptor agonist, reduces akathisia seizures and increases GAT1, GLAST and GLT-1 protein levels in rats.

CPPG: potent group II/III mGlu receptor antagonist, 20x more selective for group III (IC50: 2.2 nM) than II (46.2 nM) in rat cortex.

<p>Serotonin hydrogen maleate serves as a monoaminergic neurotransmitter and an endogenous 5-HT receptor agonist within the central nervous system (CNS). It also functions as an inhibitor of catechol O-methyltransferase (COMT), exhibiting a Ki value of 44 μM.</p>

<p>5-IAI hydrochloride is a psychoactive analog of para-iodoamphetamine. 5-IAI hydrochloride significantly reduces serotonin uptake sites and hippocampal serotonin levels in rats.</p>

<p>BF-168 is a candidate probe for PET and specifically recognizes both neuritic and diffuse plaques (Ki: 6.4 nM for Aβ1-42).</p>

<p>LRRK2-IN-16 (compound 25) is an inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. It is applicable for research in neurodegenerative and autoimmune diseases.</p>

<p>DL-Thyroxine is a thyroid hormone that acts as a monoamine oxidase (monoamine oxidase) inhibitor.</p>

<p>AAZ-A 154 hydrobromide is a selective, competitive, non-hallucinogenic 5-HT2AR antagonist. It promotes neuronal growth in rodents and yields enduring beneficial behavioral effects.</p>

<p>AAZ-A 154 benzoate is a selective, competitive, and non-hallucinogenic 5-HT2AR antagonist. This compound facilitates neuronal growth in rodents and produces lasting beneficial behavioral effects.</p>

<p>AAZ-A 154 hydrochloride is a selective, competitive, non-hallucinogenic antagonist of 5-HT2AR. It promotes neuronal growth in rodents and results in enduring beneficial behavioral effects.</p>

<p>AAZ-A 154 mesylate mesylate is a selective, competitive, and non-hallucinogenic antagonist of 5-HT2AR. It enhances neuronal growth in rodents and produces enduring beneficial behavioral effects.</p>

<p>GABA-IN-4 (Compound 17) is a derivative of N-(indol-3-ylglyoxylyl)benzylamine. It exhibits high affinity for the benzodiazepine receptor (BzR), the binding site within the GABAA receptor complex, with a Ki value of 67 nM. Benzodiazepines are widely used as anxiolytic, sedative-hypnotic, and anticonvulsant agents.</p>

<p>YNT-3708 is an orexin receptor (OXR) agonist, exhibiting EC50 values of 14.6 nM for OX1R and 277 nM for OX2R.</p>

<p>Ro4368554 is a selective 5-HT6 antagonist capable of crossing the blood-brain barrier. It can reverse memory deficits caused by scopolamine and tryptophan depletion. Ro4368554 is applicable for research related to memory impairments.</p>

hAChE-IN-10 (Compound ET11) is an inhibitor of human acetylcholinesterase (AChE) with an IC50 of 6.34 nM. This compound is capable of scavenging free radicals and exhibits antioxidant activity. Additionally, hAChE-IN-10 demonstrates metal-chelating properties, inhibiting Cu2+-induced Aβ1-42 aggregation, reducing amyloid plaque formation, and offering neuroprotective effects. It also ameliorates cognitive impairment in mice induced by Scopolamine.

<p>MAO-A inhibitor3 (Compound 360) is an MAO-A inhibitor with an IC50 greater than 100 μM. It is utilized in the investigation of neurological disorders.</p>

<p>LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.</p>

<p>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</p>

<p>(RS)-AMPA ((±)-AMPA) hydrochloride is a glutamate analog and serves as an efficient selective agonist for the excitatory neurotransmitter L-glutamic acid (L-glutamic acid). It does not interfere with the binding sites of alginate or NMDA receptors.</p>

<p>AAZ-A 154 is a selective, competitive, and non-hallucinogenic antagonist of the 5-HT2AR. It promotes neuronal growth in rodents and results in lasting beneficial behavioral effects.</p>

<p>Lu 26-046 is a muscarinic receptor agonist.</p>

<p>AChE-IN-11 aids Alzheimer's research, has neuroprotection/antioxidant properties (ORAC=2.5), and acts on AChE, MAO-B, BACE1 with IC50 values of 7.9-9.9 μM.</p>

BGT1-IN-1 (compound 9) is an effective inhibitor of BGT1, demonstrating IC50 values of 13.9 µM for hBGT1 and 58.3 µM for GAT3. It exhibits no cytotoxic effects and possesses neuroprotective activity.

<p>Nedemelteon is an agonist of the melatonin receptor (melatonin receptor).</p>

<p>DAPM (gamma-Secretase Inhibitor XVI) is a Notch pathway inhibitor with anticancer activity and antiproliferative effects.</p>

<p>Cyproflanilide is a GABAR antagonist that exhibits high activity against a variety of pests, including those from the Lepidoptera, Coleoptera, and Thysanoptera orders.</p>

<p>P2X7 receptor antagonist-5 (compound 13a) is a potent, orally active, and long-lasting antagonist of the P2X7 receptor.</p>

<p>Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.</p>

<p>Compound 16 (hAChE/Aβ1-42-IN-1) is a potent inhibitor targeting both hAChE and Aβ1-42 aggregation, demonstrating considerable safety in hepG2 cell lines and</p>

<p>SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for</p>

<p>(+)-sparteine (sulfate pentahydrate) is a ganglion blocker that competitively blocks nicotinic acetylcholine receptors in neurons.</p>

<p>Compound B15, a potent α7 nAChR antagonist, IC50 = 3.3 μM, promising for research on schizophrenia, Alzheimer's, and inflammation.</p>

<p>Compound 4c, a potent GABAA agonist with anti-depressive effects in mouse FST/TST, shows promise in depression research.</p>

<p>BChE-IN-3: Selective, pseudo-irreversible BChE inhibitor (IC50: 56.9 nM); borderline reversible AChE inhibitor.</p>

<p>(S)-YNT-3708 is the S-isomer of YNT-3708, demonstrating relatively low activity against OX1R and OX2R receptors, with EC50 values of 3595 nM and 1661 nM, respectively.</p>

<p>Terguride: treats hyperprolactinemia, blocks 5-HT2A/B, activates dopamine receptors, studied for PAH.</p>

<p>AAK1-IN-2 TFA (compound (S)-31) is a selective and potent AAK1 inhibitor (IC50: 5.8 nM) that can cross the blood-brain barrier.</p>

<p>U92016A hydrochloride: potent, orally active 5-HT1A agonist, metabolically stable, high intrinsic activity, Ki=0.2 nM.</p>

<p>LB-102 is an orally active inhibitor of dopamine D2, D3, and serotonin 5-HT7 receptors, utilized in the study of schizophrenia and other psychiatric disorders.</p>

<p>Zanapezil is an acetylcholinesterase (AChE) inhibitor. Zanapezil increases choline acetyltransferase activity in cultured rat septal cholinergic neurons.</p>

<p>BChE-IN-2, a pyrimidine/pyridine derivative, potently inhibits BChE (Ki 0.099 μM) and shows promise in AD research.</p>

<p>CEase-IN-1 (A1H3), potent CEase inhibitor, IC50 0.36μM, for hypercholesterolemia study.</p>

<p>Geissoschizoline inhibits human AChE/BChE (IC50: 20.40/10.21 µM) and has anti-inflammatory properties.</p>

<p>LRRK2-IN-6 is an oral, selective LRRK2 inhibitor crossing the blood-brain barrier, targeting GS (IC50: 4.6μM) and WT LRRK2 (IC50: 49μM).</p>

<p>Aβ42 agonist-1 is a small molecule compound with anti-cancer activity and NF-κB inhibitory properties, inducing Aβ42 aggregation.</p>

<p>ChE/Aβ1-42-IN-1 (compound 28) is a potent aggregation inhibitor of ChE and Aβ 1-42 with excellent BBB permeability.</p>

<p>YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.</p>

<p>Desmethylflunitrazepam (Norflunitrazepam) is a benzodiazepine derivative and an active metabolite of Flunitrazepam.</p>

<p>Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels &amp; lowering PAH at low doses.</p>

<p>F 14679 is a potent 5-HT1A agonist (pKi=10.23) with a maximum Ca2t response similar to 5-HT.</p>

<p>The compound is an inactive analog of forskolin(an adenylyl cyclase activator).</p>

<p>AM9405: peripheral CB1/5-HT3 agonist, suppresses gut motility, relieves GI disorder symptoms in mice.</p>

<p>LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human</p>

<p>Gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. It inhibits Aβ42 secretion in HEK cell lines stably expressing APP (Aβ amyloid precursor protein) with a pIC50 of 8.1. This compound is applicable in Alzheimer's disease research.</p>

<p>Compound 2o, also known as CB2R/5-HT1AR agonist 1, serves as a partial orally active agonist for the CB2 receptor (EC50 = 479.6 nM) and a full agonist for the 5-HT1A receptor (EC50 = 2.7 μM). This compound demonstrates both anti-anxiety and anti-depressive effects and has favorable pharmacokinetic properties [1].</p>

<p>Tebideutorexant, an orexin-1 receptor antagonist, shows anti-panic effects in rodents and humans, providing a tool for stress response and psychiatric research.</p>

<p>DL-AP5 (2-APV) lithium is a competitive antagonist of the NMDA (N-Methyl-D-aspartate) receptor. It exhibits notable analgesic activity and specifically blocks channels in the rabbit retina.</p>

<p>BACE1-IN-5 inhibits BACE1 (IC50: 9.1 nM) &amp; Aβ production (IC50: 0.82 nM), enhances hERG inhibition &amp; P-gp efflux.</p>

Remlifanserin is a potent inverse agonist of the serotonin receptor (5-HT2A).

<p>Relicpixant is a potent purine receptor (P2X) antagonist.</p>

<p>SZ1676 is a derivative of SZ1677, which is an agent of neuromuscular blocking.</p>

<p>HDAC6-IN-9 is a γ-secretase modulator that can significantly reduce the level of Aβ42 in mouse brain and can be used to study neurological diseases.</p>

<p>PXS-4787 hydrochloride is a specific and potent pan-lysyl oxidase inhibitor that effectively eliminates the activity of lysyl oxidase. It exhibits varying IC50 values against different forms of the enzyme, including 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4). In addition, PXS-4787 hydrochloride reduces the deposition and cross-linking of collagen I secreted by human fibroblasts.</p>

<p>benzodiazepine receptor antagonist,competitive</p>

<p>Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.</p>

<p>AChE-IN-47 (compound g17) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 0.24 μM. It prevents the self-aggregation of β-amyloid peptides and exhibits neuroprotective properties by effectively reducing the accumulation of intracellular reactive oxygen species (ROS).</p>

<p>AM-6494 is a potent and orally active BACE1 inhibitor (IC50: 0.4 nM) with in vivo selectivity over BACE2 (IC50: 18.6 nM).</p>

<p>Tuclazepam (KC 1956) is a derivative of the benzodiazepine class of drugs, exhibiting anti-anxiety and sedative properties.</p>

<p>AChE-IN-79 (compound 3i) is an acetylcholinesterase inhibitor with an IC50 of 2.7 µM, suitable for studies related to Alzheimer's disease.</p>

<p>PF470 (PF-06297470) is a negative allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5), which demonstrated significant therapeutic effects in Parkinson's disease models. However, its clinical development was halted due to potential issues identified in toxicological studies.</p>

<p>AChE/BChE-IN-24 (compound 5k) functions as a neuroprotective agent by inhibiting acetylcholinesterase. It targets both AChE and BChE, demonstrating IC50 values of 16.38 μM and 10.44 μM, respectively.</p>

<p>CL-13 is an inhibitor of butyrylcholinesterase (BChE), exhibiting an IC50 of 1.15 μM and a selectivity index (SI) of 9.2 for acetylcholinesterase. It demonstrates antioxidative activity in SH-SY5Y cells with a DPPHEC50 of 47.01 μM and has the capacity to chelate metals involved in Aβ aggregation and/or oxidative stress, showing no neurotoxicity at concentrations up to 50 μM. CL-13 can also reverse scopolamine-induced cognitive impairments without affecting motor abilities in mice.</p>

<p>AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.</p>

<p>Tipindole is a serotonin antagonist utilized in research related to depression.</p>

<p>Buntanetap (L-Tartrate) functions as an oral small molecule inhibitor targeting multiple neurotoxic proteins. It decreases the production of amyloid precursor protein (APP) by inhibiting the translation of its mRNA [1].</p>

<p>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

<p>AChE/BChE-IN-10 inhibits AChE/BChE (IC50: 0.176/0.47 μM), crosses the blood-brain barrier, and prevents Aβ-aggregation.</p>

BDZ-g: potent, selective AMPA receptor antagonist; useful for researching neurological disorders.

<p>Umibecestat inhibits human and mouse BACE-1 (IC50: 11 nM &amp; 10 nM), potentially for Alzheimer's research.</p>

<p>BMS 299897, a sulfonamide γ-secretase inhibitor, inhibits Aβ production with an IC50 of 7 nM in HEK293 cells overexpressing APP.</p>

<p>LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</p>

<p>Iclepertin (BI-425809) is a GlyT1 inhibitor.Iclepertin is used for the treatment of Alzheimer;s disease and other CNS disorders.</p>

<p>AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor (IC50: 0.42 μM).</p>

Xanthocillin X permethyl ether, a natural product extracted from fungal sources, exhibits Aβ-42 lowering activity.

neuronal α7 nAChR antagonist

<p>BF 227 is a candidate for an amyloid imaging probe for PET [Ki: 4.3 nM for Aβ1-42 fibrils].</p>

<p>Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.</p>

(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .

Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).

<p>(S)-Rasagiline is rasagiline S-isomer, and is an agent of anti-Parkinson.</p>

group II metabotropic glutamate receptor antagonist

mGlu1 receptor antagonist

<p>7-Desmethyl-agomelatine, a metabolite of Agomelatine, exhibits lower activity than Agomelatine, which functions as a melatonergic (MT1 and MT2) agonist and 5-HT2C antagonist.</p>

<p>(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial the 5-HT1A receptor agonist.</p>

SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.

<p>Pumosetrag Hydrochloride is an orally available 5-HT3 partial agonist. It is developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.</p>

<p>The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat NT3. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat NT3. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat NT3, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat NT3 in the samples is then determined by comparing the OD of the samples to the standard curve.</p>