Neurociência

8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that enhances the spontaneous release of histamine by promoting the degranulation of mast cells in guinea pig and human intestinal preparations. By activating the serotonin signaling pathway, this compound demonstrates potential in regulating gastrointestinal functions and offers insight into the management and suppression of functional gastrointestinal disorders such as irritable bowel syndrome. Its effects in increasing histamine release could play a crucial role in gastrointestinal regulation.

<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>MAO-B-IN-34 (compound 3d) is an inhibitor of monoamine oxidase B.</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>LRRK2-IN-5 is an oral, BBB-penetrating selective inhibitor for LRRK2 with IC50s: 1.2μM (GS) and 16μM (WT); halts LRRK2 autophosphorylation.</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>LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor.</p>

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

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

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

<p>SB 224289: selective 5-HT1B antagonist, pKi 8.2, 60x selectivity, effective orally.</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>SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].</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>(S)-Praziquantel is the inactive isomer of R-praziquantel.</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>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>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>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 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>AChE/BChE-IN-3 (BMC-1) HCl is a dual inhibitor with IC50s: eqBChE 0.383 μM, elAChE 6.08 μM.</p>

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

<p>5-HT2/5-HT7 receptor antagonist</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>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>Notch inhibitor 1 blocks Notch 1/3 (IC50: 7.8/8.5 nM) and aids cancer research.</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>AZD 2066 hydrate is a selective, orally active, and brain-penetrant antagonist of mGluR5. It exhibits antinociceptive effects [1].</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>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>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>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>BChE-IN-3: Selective, pseudo-irreversible BChE inhibitor (IC50: 56.9 nM); borderline reversible AChE inhibitor.</p>

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

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

<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>

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>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>Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM).</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>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>Anti-Aβ agent 1A is a potent anti-amyloid-β agent.</p>

S-8510 phosphate is an agonist of inverse Benzodiazepine (BDZ) receptor(Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively).

<p>BACE1-IN-2 is a BACE1 inhibitor (IC50: 22 nM).</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>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>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>LRRK2-IN-4: Potent, selective LRRK2 inhibitor, oral, BBB-penetrating, IC50=2.6 nM, potential for Parkinson's.</p>

<p>MAO-B-IN-10: Potent, selective MAO-B inhibitor; crosses blood-brain barrier; IC50 5.3 μM; reduces Aβ aggregation 58.2%, disaggregates 43.3%.</p>

FP0429 is an agonist of mGlu4.

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

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

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

<p>AChE/BACE1/GSK3β-IN-1 is an orally active, blood-brain barrier-transparent, moderately bioavailable triple inhibitor of AChE/BACE1/GSK3β.</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>(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>Gabaculine, an irreversible GABA-T inhibitor (Ki: 2.9 μM), impacts plastid development and affects DPOR/GluTR levels.</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>PXS-5153A is an oral, fast-acting LOXL2/3 inhibitor with IC50 &lt;40 nM for LOXL2 and 63 nM for LOXL3, potentially treating fibrosis.</p>

<p>5-HT2 receptor antagonist</p>

<p>DAPM (gamma-Secretase Inhibitor XVI) is a Notch pathway inhibitor with anticancer activity and antiproliferative effects.</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>Relicpixant is a potent purine receptor (P2X) antagonist.</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>cSPM (Cyclic spermine) is an Aβ42 inhibitor. cSPM inhibits the aggregation of three different peptides, Aβ42, tryptophan and insulin, and reduces cytotoxicity.</p>

<p>Befiradol HCl (NLX-112) is a selective 5-HT1A receptor agonist with anxiolytic effects and prevents ATXN3 aggregation.</p>

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

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

<p>LRRK2-IN-3: potent, selective oral LRRK2 blocker, BBB-penetrant, IC50 of 0.6 nM in hPBMCs, for Parkinson's research.</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>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>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>LY2979165 (mGlu2 agonist) is an orthosteric agonist of mGluR2 and can be used in studies about serving as an anti-depressant.</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/BChE-IN-10 inhibits AChE/BChE (IC50: 0.176/0.47 μM), crosses the blood-brain barrier, and prevents Aβ-aggregation.</p>

<p>SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.</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>AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor (IC50: 0.42 μM).</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>NB-360: potent, brain-penetrant BACE1/2 inhibitor; IC50s: 5-6 nM; high selectivity vs pepsin, cathepsin E/D.</p>

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

neuronal α7 nAChR antagonist

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

group II metabotropic glutamate 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).

<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>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>

mGlu1 receptor antagonist

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