Neuroscience

<p>Metoquizine is an anticholinergic compound. It is a muscarinic acetylcholine receptor antagonist that has been used to treat ulcers.</p>

<p>Pareptide monohydrochloride is a metabolically stable analog of melatonin inhibitor (MIF).</p>

<p>Beloxepin is an oral dual selective inhibitor of serotonin and norepinephrine uptake.</p>

<p>LY367385 hydrochloride: selective mGluR1a antagonist, IC50 = 8.8 μM, neuroprotective, anticonvulsant, antiepileptic.</p>

<p>AChE/BChE-IN-19 (compound 12) is a nicotinic hydrazine derivative that acts as an inhibitor of AChE (IC50=21.45 nM) and BChE (IC50=18.42 nM), and it is applicable in Alzheimer's disease research.</p>

MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 value of 1.9±0.5 nM, potentially serving as a candidate molecule for neurodegenerative disease research.

QP5020 is a QPCTL inhibitor with an IC50 value of 15 nM, demonstrating antitumor efficacy.

<p>Pomaglumetad methionil is an oral methionine prodrug of the potent specific agonist of mGlu2/3 receptor LY404039.</p>

<p>BACE1-IN-8 is a potent inhibitor of BACE1 (β-site APP lyase 1) (IC50: 3.9 μM).</p>

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

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

<p>Amyloid-β-IN-3 (EX.113) is a selective inhibitor of γ-secretase. It demonstrates inhibitory activity on Aβ42 secretion in H4 cells, with an EC50 value of 148 nM. By modulating the catalytic activity of γ-secretase, Amyloid-β-IN-3 decreases Aβ42 production, thereby alleviating neurotoxicity caused by Aβ deposition. It holds potential for Alzheimer's disease (AD) research.</p>

<p>MAO-B inhibitor 2: potent, reversible, oral, selective (IC50=1.33 nM), BBB-penetrant, with anti-oxidant and anti-inflammatory effects for Parkinson's study.</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>

SNRI-IN-1 (Compound 7a) acts as a dual inhibitor of serotonin and noradrenaline monoamine reuptake, with a P-glycoprotein Efflux Ratio of 20 [1].

<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>cSPM (Cyclic spermine) is an Aβ42 inhibitor. cSPM inhibits the aggregation of three different peptides, Aβ42, tryptophan and insulin, and reduces cytotoxicity.</p>

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

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

<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>LRRK2-IN-2: selective, potent LRRK2 inhibitor, IC50 of 0.6 nM, oral, crosses blood-brain barrier, for Parkinson's research.</p>

<p>Carlina oxide is both an AChE inhibitor and an antioxidant, effective in eliminating mosquito larvae (LC50=1.39 μg/mL). Furthermore, Carlina oxide exhibits cytotoxicity in vertebrate cells, human dermis, and HCT116 and MDA-MB231 cell lines.</p>

<p>BPN-15606 besylate is a potent oral γ-secretase regulator reducing Aβ42 and Aβ40 with good pharmacokinetics. IC50: 7 nM (Aβ42), 17 nM (Aβ40).</p>

<p>AChE-IN-10 (24r) inhibits AChE (IC50=2.4 nM), reducing amyloid buildup, tau phosphorylation, and promotes neuron health.</p>

ChEs/MAOs-IN-2 (compound a11) serves as an inhibitor for both cholinesterases and monoamine oxidases, exhibiting IC 50 values of 0.10 µM for MAO-A, 0.20 µM for MAO-B, 0.30 µM for AChE, and 0.40 µM for BChE. This compound shows promise for Alzheimer's disease research [1].

<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>BMS-901715 is an effective and selective inhibitor of adapter protein-2 associated kinase 1 (AAK1; IC50: 3.3 nM).</p>

<p>AChE-IN-8 (Compound 19), potent acetylcholinesterase blocker; IC50 = 1.95 μM; potential Alzheimer's treatment.</p>

<p>AAK1-IN-3 TFA, an AAK1 inhibitor with IC50 of 11 nM, crosses the blood-brain barrier, is a quinoline analogue, and may aid neuropathic pain research.</p>

<p>CaMKIIα-IN-1 (Compound 4d) is an orally active inhibitor of Ca 2+ /calmodulin-dependent protein kinase II α (CaMKIIα) with a Kd of 219 nM for CaMKIIα WT hub.</p>

MAO-IN-4 (Compound 2l), a monoamine oxidase (MAO) inhibitor, demonstrates IC50 values of 0.07 μM for MAO-A and 0.75 μM for MAO-B. This compound is utilized in studying depression and Parkinson's disease (PD) [1].

<p>Potent, selective MAO-B inhibitor; reversible; oral; crosses BBB; IC50=0.02 nM; potential for Parkinson's research.</p>

<p>DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.</p>

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

PF-06751979 is an inhibitor of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) (IC50 of 7.3 nM in BACE1 binding assay).

<p>Lu 26-046 is a muscarinic receptor agonist.</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>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 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 hydrobromide is a selective, competitive, non-hallucinogenic 5-HT2AR antagonist. It promotes neuronal growth in rodents and yields enduring beneficial behavioral effects.</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>

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>LRRK2-IN-4: Potent, selective LRRK2 inhibitor, oral, BBB-penetrating, IC50=2.6 nM, potential for Parkinson's.</p>

<p>Gabaculine, an irreversible GABA-T inhibitor (Ki: 2.9 μM), impacts plastid development and affects DPOR/GluTR levels.</p>

<p>SEP-363856 (SEP-856) mesylate is an orally active compound that acts as an agonist for both TAAR1 and 5-HT1A receptors. This compound exhibits antipsychotic activity in the central nervous system and has potential for the study of schizophrenia.</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>

<p>RTIOXA-43 is an OX2R/OX1R (orexin receptor) dual agonist that increases wakefulnesand is commonly used in studies related to narcolepsy and neural signaling.</p>

<p>Nafimidone hydrochloride, an antiepileptic agent, inhibits acetylcholinesterase, protects neurons, and ameliorates cognitive decline. It is utilized in epilepsy research.</p>

<p>SGE516: neuroactive steroid, enhances GABAA, lowers neuronal activity, protects from seizures.</p>

<p>DA-8031 is a selective and orally active serotonin reuptake inhibitor. It is utilized in research related to premature ejaculation (PE).</p>

<p>Sulamserod hydrochloride is a 5-HT4 receptor antagonist. It is utilized in research related to gastrointestinal disorders.</p>

<p>F 14679 is a potent 5-HT1A agonist (pKi=10.23) with a maximum Ca2t response similar to 5-HT.</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>Tipindole is a serotonin antagonist utilized in research related to depression.</p>

<p>Elzasonan hydrochloride is a serotonin 1B and serotonin 1D receptor antagonist. It is utilized in the study of depression.</p>

<p>hMAO-B-IN-10 (compound 7) is an inhibitor of MAO-A/B with IC50 values of 424.1 nM and 177.9 nM, respectively. It has demonstrated neuroprotective effects in the MPTP-induced mouse model of Parkinson's Disease (PD).</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>TP003 is a novel non-selective GABAA receptor benzodiazepine site agonist with affinity for α1β2gam2, α2β3gam2, α3β3gam2, α5β2gam2, EC50 of 20.3, 10.6, 3.24, 5.</p>

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

<p>Tiprenolol hydrochloride is a β-adrenoceptor (β-adrenoceptor) antagonist. This compound is effective in eliminating ventricular arrhythmias in dogs caused by intravenous administration of adrenaline, following inhalation of halothane.</p>

<p>(S)-Norfluoxetine, the S enantiomer of Norfluoxetine, functions as a selective serotonin reuptake inhibitor. It enhances allopregnanolone levels and reduces aggression in socially isolated mice.</p>

<p>Etoperidone is an antidepressant that acts as an orally active reuptake inhibitor for serotonin (serotonin) and noradrenaline (nor-adrenaline). It demonstrates specific binding affinities (Kd) for several receptors: 36 nM at the 5-HT2 receptor, 38 nM at the α1-adrenergic receptor (α1-adrenergic receptor), 85 nM at the 5-HT1A receptor, and 570 nM at the α2-adrenergic receptor (α2-adrenergic receptor).</p>

<p>Compound 6f is a potent, selective 5-HT1A receptor blocker (Ki: 35 nM), useful in CNS disorder research.</p>

<p>AChE/BuChE-IN-3 inhibits AChE (IC50: 0.65 μM), BuChE (IC50: 5.77 μM), crosses BBB, and hinders Aβ1-42 aggregation for Alzheimer's research.</p>

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor (IC50: 3.8 nM; Ki: 1.9 nM), more selective at BACE1 over BACE2.

<p>Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.</p>

AChE-IN-83 (compound f1) is an AChE inhibitor that suppresses nematode growth and acetylcholinesterase activity in rice seeds while being safe for the seeds. It specifically targets Aphelenchoides besseyi, with an LC50 of 19.0 μg/mL over 48 hours. AChE-IN-83 impedes nematode populations and behaviors in rice seeds, damages the nematode cuticle, and induces reactive oxygen species, lipofuscin, and lipid generation within the nematodes.

<p>MMB-4 is an oxime that can reactivate cholinesterases (cholinesterases) which have been inactivated due to exposure to organophosphates such as Sarin or Soman.</p>

<p>THRX-194556 is an agonist of the 5-HT4 receptor. It is applicable in the study of gastrointestinal functional disorders and Alzheimer's disease.</p>

<p>FCOB02 is a monoamine oxidase B (MAO-B) ligand. It can be labeled as [18F]FCOB02, serving as a 4-methylcoumarin-like targeting probe. [18F]FCOB02 demonstrates high affinity for MAO-B, with an IC50 of 10.68 nM. It is utilized for specific imaging and quantitative analysis of MAO-B in vivo.</p>

<p>Aβ-IN-2 is a peptide inhibitor of Aβ1-42.</p>

<p>LP 12 hydrochloride hydrate: potent, selective 5-HT7 agonist (Ki: 0.13 nM); less affinity for D2, 5-HT1A/2A receptors.</p>

<p>(S)-Praziquantel is the inactive isomer of R-praziquantel.</p>

<p>MAO-B-IN-5: potent, selective oral MAO-B inhibitor, IC50=0.204μM, potential for Parkinson's research.</p>

<p>25B-NBOH hydrochloride is a phenethylamine that exhibits high affinity for serotonin (5-HT) receptors 5-HT2A and 5-HT2C, with pKi values of 8.3 and 9.4, respectively.</p>

<p>D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.</p>

<p>Anti-Aβ agent 1A is a potent anti-amyloid-β agent.</p>

<p>(R)-Norfluoxetine is the (R)-enantiomer of Norfluoxetine. It functions as a potent serotonin reuptake inhibitor, with a Ki value of 13 nM. This compound is utilized in the research of depression.</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>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

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

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

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

<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>

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

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

mGlu1 receptor antagonist

group II metabotropic glutamate receptor antagonist

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

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

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

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

<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>

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>

<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>