Neuroscienza

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

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>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>

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.

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.

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.

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].

Potent 5-HT6/5-HT2A receptors dual antagonist with K i of 11 nM & 39 nM.

(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.

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.

Lu 26-046 is a muscarinic receptor agonist.

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

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

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

eeAChE-IN-1 is a strong inhibitor of eeAChE (IC50: 23 nM).

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

VA012 (compound 11) acts as a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. It has been shown to reduce food intake and prevent weight gain during subchronic administration without causing central nervous system-related discomfort. VA012 is applicable in obesity research.

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

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

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.

R-137696 is an orally active 5-HT1A receptor agonist that facilitates the relaxation of the proximal stomach. It is utilized in research related to functional dyspepsia.

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

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>(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>

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.

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.

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

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

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

MAO-A/SERT-IN-1 acts as an inhibitor for both MAO-A and the serotonin transporter (SERT). It decreases the SERT-mediated reuptake of 5-HT and demonstrates neuroprotective properties in cellular inhibition models. Additionally, this compound has shown to alleviate depressive behaviors in both zebrafish and mice.

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].

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.

AChE-IN-24: Strong AChE blocker, crosses blood-brain barrier, IC50=0.053 μM, useful for AD research.

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.

AChE-IN-22 (10q) selectively inhibits AChE (IC50: 0.88 μM), less on BuChE (IC50: 10 μM), targets CAS and PAS, useful in Alzheimer's research.

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>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>

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

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

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

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

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

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

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

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

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

mGlu1 receptor antagonist

group II metabotropic glutamate receptor antagonist

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

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.

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.

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

neuronal α7 nAChR antagonist

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>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>

Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist that effectively inhibits calmodulin-activated Ca 2+ -phosphodiesterase (PDE) with an IC 50 of 28 μM. This compound also competitively inhibits trypsin-treated Ca 2+ -PDE with respect to cyclic GMP, exhibiting an IC 50 of 375 μM and a K i value of 300 μM.

Desmethyl cariprazine is a Cariprazine active metabolite. Cariprazine, an antipsychotic drug candidate, shows a high affinity for the D3 (Ki: 0.085 nM) and D2 (Ki: 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).

Ebeiedinone, a steroidal alkaloid derived from Fritillaria species, effectively inhibits the activity of human whole blood cholinesterase (ChE) at a concentration of 0.1 mM, resulting in a significant inhibitory effect of 69.0%.

VU0080241 is a positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4).

2-AEMP TFA is a potent and rapidly acting antagonist of GABA(A)-ρ1 receptors. 2-AEMP is an analog of GABA.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.

Physostigmine is a potent and reversible inhibitor of cholinesterase. It is also reported to form a slowly degrading carbamylated enzyme complex with acetylcholinesterase (AChE).

Acridine-9-carboxylic acid is a useful organic compound for research related to life sciences. The catalog number is T65511 and the CAS number is 5336-90-3.

Eglumegad (LY354740) hydrochloride is a potent, selective agonist for group II (mGlu2/3) receptors, showing IC50 values of 5 nM for mGlu2 and 24 nM for mGlu3 receptors in transfected human cells. This compound provides neuroprotection against NMDA-induced toxicity and exhibits anxiolytic- and antipsychotic-like properties [1].

BRL 15572 is a useful organic compound for research related to life sciences. The catalog number is T64501 and the CAS number is 734517-40-9.

VU6000918 is a positive allosteric modulator that targets the muscarinic acetylcholine receptor subtype M4. It exhibits a half maximal effective concentration (EC50) of 19 nM for the human M4 receptor.

Alfadolone acetate is a gamma-aminobutyric acid (GABA) receptor agonist.

3-Methylglutaconic acid, a primary metabolite accumulating in 3-Methylglutaconic aciduria (MGTA), induces lipid and protein oxidation, while diminishing non-enzymatic antioxidant defenses in cerebral cortex supernatants, thereby promoting oxidative stress in the cerebral cortex. This compound is utilized in research concerning brain damage diseases [1].

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IL-6. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IL-6. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IL-6, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IL-6. You can calculate the concentration of Mouse IL-6 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse TNF-α. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse TNF-α. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse TNF-α, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse TNF-α. You can calculate the concentration of Mouse TNF-α in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human IL-6. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human IL-6. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human IL-6, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human IL-6. You can calculate the concentration of Human IL-6 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse GROα/CXCL1. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse GROα/CXCL1. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse GROα/CXCL1, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse GROα/CXCL1. You can calculate the concentration of Mouse GROα/CXCL1 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IL-17A. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IL-17A. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IL-17A, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IL-17A. You can calculate the concentration of Mouse IL-17A in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IL-9. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IL-9. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IL-9, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IL-9. You can calculate the concentration of Mouse IL-9 in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Mouse IFN-γ. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Mouse IFN-γ. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Mouse IFN-γ, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Mouse IFN-γ. You can calculate the concentration of Mouse IFN-γ in the samples by comparing the OD of the samples to the standard curve.

This ELISA kit uses the Sandwich-ELISA principle. The micro ELISA plate provided in this kit has been pre-coated with an antibody specific to Human IFN-α. Samples (or Standards) are added to the micro ELISA plate wells and combined with the specific antibody and biotinylated detection antibody specific for Human IFN-α. Then Avidin-Horseradish Peroxidase (HRP) conjugate are added successively to each micro plate well and incubated. Free components are washed away. The substrate solution is added to each well. Only those wells that contain Human IFN-α, biotinylated detection antibody and Avidin-HRP conjugate will appear blue in color. The enzyme-substrate reaction is terminated by the addition of stop solution and the color turns yellow. The optical density (OD) is measured spectrophotometrically at a wavelength of 450 nm. The OD value is proportional to the concentration of Human IFN-α. You can calculate the concentration of Human IFN-α in the samples by comparing the OD of the samples to the standard curve.

<p>Coumaran (2,3-Dihydrobenzofuran) is an acetylcholinesterase (AChE) inhibitor isolated from leaves of L. camara. Coumaran(2,3-Dihydrobenzofuran) can be used as a biopesticide. 2,3-dihydrobenzofuran is a member of the class of 1-benzofurans that is the 2,3-dihydroderivative of benzofuran. It has a role as a metabolite.</p>

2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist with anti-depressive-like effects.

<p>RU 24969 succinate, a 5-HT receptor agonist, exhibits K i values of 0.38 nM for 5-HT 1B and 2.5 nM for 5-HT 1A, indicating its affinity towards these receptors. It reduces fluid consumption and enhances forward locomotion. This compound is utilized in neurological disease research.</p>

<p>Lupinine is an alkaloid capable of counteracting ethanol anesthesia. Lupinine is an AChE and BChE inhibitor and potential CD69 activator found in species of Loranthus, Calia, and Lupinus. It may also inhibit heparin.</p>