Neurociência

<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>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>

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>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>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>P2X4 antagonist-1 is a potent P2X4 receptor antagonist used in the study of neurological, cardiovascular, and immune system diseases.</p>

<p>5-HT2A and 2C receptor antagonist</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>

<p>LP 12 hydrochloride hydrate: potent, selective 5-HT7 agonist (Ki: 0.13 nM); less affinity for D2, 5-HT1A/2A receptors.</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>Alixorexton is an agonist of the orexin-2 receptor (orexin-2 receptor) and is utilized in obesity research.</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>K027 is a potent organophosphate (OP) inhibitor of acetylcholinesterase (AChE) reactivation. k027 can be used to study Alzheimer's disease.</p>

<p>Potent 5-HT6/5-HT2A receptors dual antagonist with K i of 11 nM &amp; 39 nM.</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>AChE-IN-10 (24r) inhibits AChE (IC50=2.4 nM), reducing amyloid buildup, tau phosphorylation, and promotes neuron health.</p>

<p>CVN636, a potent and selective allosteric agonist for the mGluR7 receptor, exhibits oral activity and CNS permeability [1], with an EC50 of 7 nM for human</p>

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

<p>BACE-1 Inhibitor 2 is a potent, CNS-permeable inhibitor of BACE-1, exhibiting an IC50 value of 1.5 nM in enzymatic assays [1].</p>

<p>γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM).</p>

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

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

<p>Rodatristat is an effective tryptophan hydroxylase 1 and TPH2 inhibitor (IC50s: 33 nM and 7 nM, respectively).</p>

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

<p>CaMKK2-IN-1 is a selective and potent inhibitor of CaMKK2, exhibiting an IC50 of 7 nM.</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>

<p>2,6-Dimethoxybenzylamine hydrochloride (Compound 5) exhibits reversible inhibitory activity against copper amine oxidase (CAO) and inhibits benzylamine oxidase (BAO) and monoamine oxidase B (MAO B) with IC50 values of 120 μM and 190 μM, respectively.</p>

<p>VU6007496 is a highly selective and CNS-penetrating M1 positive allosteric modulator (PAM) that exhibits good pharmacokinetics (PK).</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

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

<p>Sulamserod hydrochloride is a 5-HT4 receptor antagonist. It is utilized in research related to gastrointestinal disorders.</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>Nafimidone hydrochloride, an antiepileptic agent, inhibits acetylcholinesterase, protects neurons, and ameliorates cognitive decline. It is utilized in epilepsy research.</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>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>BChE-IN-38 (compound 13) is a potent BChE inhibitor, with Ki values of 62.05, 28.78, 14.09, and 1.15 nM for hCAI, hCAII, AChE, and BChE, respectively. BChE-IN-38 also demonstrates cytotoxic activity.</p>

<p>K203 is a potent tabun-inhibited AChE reactivator and is an important antidote to organophosphorus poisoning.</p>

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

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

<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>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>

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.

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

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

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

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

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

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

<p>LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor.</p>

<p>AChE/BChE/MAO-B-IN-5 is a multi-target inhibitor capable of crossing the blood-brain barrier, targeting cholinesterases (AChE and BChE) and monoamine oxidase MAO-B. It exhibits IC50 values of 0.24 µM for AChE, 6.29 µM for BChE, and 0.11 µM for MAO-B. AChE/BChE/MAO-B-IN-5 holds potential for research in neurodegenerative diseases such as Alzheimer's disease.</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>

<p>AChE-IN-8 (Compound 19), potent acetylcholinesterase blocker; IC50 = 1.95 μM; potential Alzheimer's treatment.</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>AChE-IN-5: oral, crosses blood-brain barrier, targets AChE/5-HT1A/SERT, potent with 2.29 nM IC50.</p>

<p>BChE-IN-5: potent, selective BChE inhibitor (IC50: 2.8 nM), more effective on hBChE, potential in Alzheimer's research.</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>AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-transparent, moderately bioavailable triple inhibitor of AChE/BACE1/GSK3β.</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>AChE-IN-63 (Compound 5AD) serves as a selective inhibitor of hAChE, exhibiting an IC 50 value of 0.103 μM. Moreover, it inhibits hBChE and hBACE-1 with IC 50 values of 10 μM and 1.342 μM, respectively. AChE-IN-63 is effective in inhibiting Aβ aggregation and preventing the formation and deposition of Aβ1-42. It can effectively penetrate the blood-brain barrier and is orally bioavailable. This compound is primarily utilized in research related to Alzheimer's disease [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>eeAChE-IN-1 is a strong inhibitor of eeAChE (IC50: 23 nM).</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>(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>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>Compound 22d is a GSM that crosses the blood-brain barrier, inhibits Aβ42 production (IC50: 60 nM), and may help study Alzheimer's.</p>

<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>TDI-11861 is a second-gen sAC (ADCY10) inhibitor with an IC50 of 5.5 nM and slow dissociation.</p>

<p>Relicpixant is a potent purine receptor (P2X) antagonist.</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>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>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>(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>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>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>MAO-B-IN-5: potent, selective oral MAO-B inhibitor, IC50=0.204μM, potential for Parkinson's research.</p>

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

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

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

<p>LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.</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>Umibecestat inhibits human and mouse BACE-1 (IC50: 11 nM &amp; 10 nM), potentially for Alzheimer's research.</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>BMS 299897, a sulfonamide γ-secretase inhibitor, inhibits Aβ production with an IC50 of 7 nM in HEK293 cells overexpressing APP.</p>

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

<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>

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).

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

group II metabotropic glutamate receptor antagonist

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

neuronal α7 nAChR antagonist

<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>

mGlu1 receptor antagonist

<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>

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

(-)-Bicuculline methobromide is a potent antagonist of GABAA 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>