Neuroscience

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

<p>MAO-B-IN-34 (compound 3d) is an inhibitor of monoamine oxidase B.</p>

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

<p>metabotropic glutamate receptor type 1 (mGlu1) antagonist</p>

Fletazepam, a benzodiazepine derivative, exhibits sedative, anti-anxiety, and muscle-relaxant properties. It is utilized in neurological research.

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

<p>Rodatristat ethyl is an oral TPH1 inhibitor reducing 5-HT levels &amp; lowering PAH at low doses.</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>SZ1676 is a derivative of SZ1677, which is an agent of neuromuscular blocking.</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>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>

<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>AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1].</p>

<p>AChE/BChE-IN-3 (BMC-1) HCl is a dual inhibitor with IC50s: eqBChE 0.383 μM, elAChE 6.08 μM.</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>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>(+)-sparteine (sulfate pentahydrate) is a ganglion blocker that competitively blocks nicotinic acetylcholine receptors in neurons.</p>

<p>Dihydro-β-erythroidine hydrobromide(DHβE) is a potent, oral active and competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs).</p>

<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>

<p>eeAChE-IN-1 is a strong inhibitor of eeAChE (IC50: 23 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>

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

<p>AChE/BChE-IN-1: dual AChE/BChE inhibitor, IC50 of 1.06 nM/7.3 nM, crosses blood-brain barrier, with antioxidant properties for Alzheimer's research.</p>

<p>MAO-B-IN-42 (Compound 4f) is a selective and reversible monoamine oxidase-B (MAO-B) inhibitor, with an IC50 value of 0.184 μM. By blocking the oxidative deamination of monoamines catalyzed by MAO-B, it helps maintain neurotransmitter levels. MAO-B-IN-42 shows potential for research into Parkinson's disease.</p>

<p>BChE-IN-5: potent, selective BChE inhibitor (IC50: 2.8 nM), more effective on hBChE, potential in Alzheimer's 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>F 14679 is a potent 5-HT1A agonist (pKi=10.23) with a maximum Ca2t response similar to 5-HT.</p>

<p>BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).</p>

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

<p>DL-Thyroxine is a thyroid hormone that acts as a monoamine oxidase (monoamine oxidase) inhibitor.</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>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>(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>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>γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM).</p>

<p>VU6005806 is a potent M4 PAM with EC50s: 94 nM (human), 28 nM (rat), 87 nM (dog), 68 nM (cyno); studied for neuropsychiatric disorders.</p>

<p>ASP-2205, a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM), enhances the urethral closure reflex mediated by the genital nerve, thereby preventing urinary incontinence.</p>

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

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

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

<p>Rocavorexant is an antagonist of the orexin-1 receptor (orexin-1 receptor), exhibiting a pIC50 value of 9.1 for human OX1 and a pIC50 of 6.0 for human OX2.</p>

<p>DSP-1053: Benzylpiperidine-based, potent SERT inhibitor (Ki=1.02nM), partial 5-HT1A receptor agonist (Ki=5.05nM), antidepressant.</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>(9R)-RO7185876 (Compound example 16) is a γ-secretase inhibitor. It reduces the secretion of Αβ42. This compound can be employed in the research of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, senile dementia, or Down syndrome.</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>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>5-HT2 receptor antagonist</p>

<p>AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.</p>

<p>5-HT6R/MAO-B modulator 1 blocks 5-HT6R and permanently inhibits MAO-B, protects glial cells, and reverses memory loss.</p>

<p>MADAM demonstrates high affinity and selectivity for 5-HTT, with a Ki value of 1.6 nM. It is utilized as a PET radiotracer for visualizing serotonin transporters.</p>

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

<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>

<p>PF-06648671 is a γ-secretase modulator for the treatment of neurodegenerative and/or neurological disorders.</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>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>5-HT1A modulator 4 (Compound 1) is a ligand for the 5-HT receptor, with Ki values of 2.18 μM for 5-HT1A and 19.7 μM for 5-HT2A.</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>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>MAO-B-IN-40 (3a) is an inhibitor of MAOB, exhibiting an IC50 value of 0.493 μM against hMAOB, and demonstrates significant neuroprotective and antioxidant effects. MAO-B-IN-40 (3a) is applicable in Parkinson's disease research.</p>

<p>EF1502 is a potent and selective GABA transporter inhibitor.</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>MAO-B-IN-6 is a selective, potent, orally active MAO-B inhibitor (IC50: 0.019 μM). MAO-B-IN-6 is superior to Safinamide both in vitro and in vivo.</p>

<p>(+)-Cevimeline HCl hemihydrate is a muscarinic agonist for dry mouth in Sjogren's with rapid absorption, differing metabolism in species.</p>

LY3020371 HCl: potent mGlu2/3 antagonist, antidepressant-like; Ki: 5.3/2.5 nM, IC50: 16.2 nM for cAMP inhibition.

<p>BRD0418 acts as an upregulator of TRIB1 expression by leading to reprogramming of hepatic lipoprotein metabolism from adipogenesis to clearance it.</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>

<p>Zanapezil is an acetylcholinesterase (AChE) inhibitor. Zanapezil increases choline acetyltransferase activity in cultured rat septal cholinergic neurons.</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>Revexepride, a 5-HT4 agonist, may boost CYP3A4, used for treating GERD.</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>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>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>

<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>Compound AV-2, also known as AChE/Aβ-IN-5, is a bifunctional inhibitor that acts on AChE and auto-induced Aβ (Amyloid-β) aggregation. This compound has demonstrated significant efficacy in mitigating cognitive impairment in mice induced by scopolamine and Aβ [1].</p>

<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>

<p>Notch inhibitor 1 blocks Notch 1/3 (IC50: 7.8/8.5 nM) and aids cancer research.</p>

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

<p>P2X7 receptor antagonist-5 (compound 13a) is a potent, orally active, and long-lasting antagonist of the P2X7 receptor.</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>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

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

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

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

<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>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>(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>

neuronal α7 nAChR antagonist

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

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

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

mGlu1 receptor antagonist

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).

group II metabotropic glutamate 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>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>(-)-Bicuculline methobromide is a potent antagonist of GABAA receptor .</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>