Search Result
Results for "
striatal
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-160019
-
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Deubiquitinase
Mitophagy
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Neurological Disease
|
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MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
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- HY-B0590
-
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Ro 1-9569
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Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-12472
-
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TAK-063
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Phosphodiesterase (PDE)
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Infection
Neurological Disease
Cancer
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Balipodect (TAK-063) is a selective, brain-penetrant and orally active PDE10A inhibitor with an IC50 of 0.30 nM. Balipodect shows >15000-fold selectivity over other PDEs. Balipodect elevates striatal cAMP and cGMP levels in mice. Balipodect can be used for the study of schizophrenia[1].
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- HY-10435A
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(±)-SKF-82958 hydrobromide; Chloro-APB hydrobromide
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Dopamine Receptor
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Neurological Disease
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SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
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- HY-B0590S
-
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Ro 1-9569-d6
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Monoamine Transporter
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Neurological Disease
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Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-B1124
-
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Adenylate Cyclase
Dopamine Transporter
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Neurological Disease
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Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection .
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- HY-B0344
-
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(-)-Scopolamine methyl bromide; Hyoscine methyl bromide
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mAChR
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Neurological Disease
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Methscopolamine bromide ((-)-Scopolamine methyl bromide; Hyoscine methyl bromide) is a peripherally acting muscarinic receptor (mAChR) antagonist that cannot cross the blood-brain barrier. Methscopolamine bromide blocks the muscarinic negative feedback regulation of acetylcholine release from striatal cholinergic terminals, thereby increasing acetylcholine release in the striatum of freely moving rats. Methscopolamine bromide does not induce motor excitation in freely moving rats, nor does it alter the duration of ethanol-induced loss of righting reflex in mice. Methscopolamine bromide fails to antagonize the arecoline-mediated reduction in the duration of ethanol-induced loss of righting reflex in mice .
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- HY-B1382
-
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1,2,2,6,6-Pentamethylpiperidine
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nAChR
|
Cardiovascular Disease
Neurological Disease
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Pempidine (1,2,2,6,6-Pentamethylpiperidine) is an orally active ganglionic blocking agent used in hypertension-related conditions. Pempidine is a nicotinic receptor blocker. Pempidine can antagonize the nicotine-induced increase of the striatal dopamine (DA) in vitro .
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- HY-145468
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GPR52
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Neurological Disease
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GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons .
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- HY-124591
-
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5-HT Receptor
Monoamine Oxidase
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Neurological Disease
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TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling .
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- HY-B0188
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Mianserine
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Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
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Neurological Disease
|
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Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-145512
-
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NLT
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Dopamine Receptor
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Neurological Disease
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N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
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- HY-Z0283
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Benzenecarboxamide; Phenylamide
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Endogenous Metabolite
PARP
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Others
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Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-107969
-
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Dopamine Receptor
COX
NO Synthase
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Neurological Disease
Cancer
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Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
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- HY-167856
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GPR88
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Neurological Disease
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RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
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- HY-159829
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NBI-1117568; HTL-0016878
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mAChR
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Neurological Disease
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
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- HY-B1752
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LY 171555; (-)-LY 141865
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Dopamine Receptor
Calcium Channel
Bcl-2 Family
iGluR
Apoptosis
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Neurological Disease
|
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Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3 dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia .
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- HY-120017
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MD-370503
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Monoamine Oxidase
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Neurological Disease
|
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Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential .
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- HY-P1206
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CH 275
1 Publications Verification
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Somatostatin Receptor
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Neurological Disease
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CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
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- HY-B0590A
-
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Ro 1-9569 Racemate
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Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-B0884A
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Monoamine Oxidase
Cholinesterase (ChE)
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Neurological Disease
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Minaprine dihydrochloride is a brain-penetrant monoamine oxidase inhibitor. Minaprine dihydrochloride also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine dihydrochloride reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine dihydrochloride exhibits convulsant, antidepressant properties .
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- HY-125339
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COMT
Apoptosis
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Neurological Disease
Cancer
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Ro 41-0960 is a CNS-penetrant, orally active catechol-O-methyl transferase (COMT) inhibitor. Ro 41-0960 reduces dopamine catabolism, increases striatal dopamine and DOPAC levels, decreases striatal HVA levels, induces apoptosis, inhibits proliferation and extracellular matrix formation in uterine fibroid cells. Ro 41-0960 arrests or shrinks uterine fibroid lesions in rats. Ro 41-0960 can be used for the research of Parkinson’s disease, uterine leiomyomas, and breast cancer .
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- HY-B1124A
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Adenylate Cyclase
Dopamine Transporter
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Neurological Disease
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Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research. Fipexide hydrochloride acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection .
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- HY-12294A
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NVP-AAM077 tetrasodium hydrate
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Apoptosis
Caspase
iGluR
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Neurological Disease
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PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a tetrasodium hydrate of PEAQX (HY-12294). PEAQX tetrasodium hydrate is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX tetrasodium hydrate can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
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- HY-106584
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Clospipramine
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Drug Derivative
Dopamine Receptor
5-HT Receptor
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Neurological Disease
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Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia .
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- HY-100968
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Dopamine Receptor
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Neurological Disease
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GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats .
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- HY-156331
-
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mGluR
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Neurological Disease
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VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
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- HY-12294
-
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NVP-AAM077
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Caspase
Apoptosis
iGluR
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Neurological Disease
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PEAQX (NVP-AAM077) is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
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- HY-P4532
-
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Cathepsin
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Neurological Disease
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Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II .
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- HY-110302
-
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Opioid Receptor
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Neurological Disease
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6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
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- HY-N2326
-
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nAChR
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Neurological Disease
Metabolic Disease
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(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to α4β2- and α7-type nicotinic receptors in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM). (±)-Anatoxin A fumarate has toxic effect on fish .
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- HY-156772
-
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GPR88
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Others
Neurological Disease
|
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GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC50 value of 14 µM in GPR88 cAMP functional assay .
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- HY-152170
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bPiDI
1 Publications Verification
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nAChR
|
Neurological Disease
|
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bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
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- HY-P1303
-
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-119468
-
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Dopamine Transporter
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Neurological Disease
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Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression .
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- HY-B0884
-
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Monoamine Oxidase
Cholinesterase (ChE)
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Neurological Disease
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Minaprine is a brain-penetrant monoamine oxidase inhibitor. Minaprine also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine exhibits convulsant, antidepressant properties .
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- HY-107674
-
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nAChR
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Neurological Disease
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bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
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- HY-105328
-
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5-HT Receptor
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Neurological Disease
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S-14489 is an orally active selective postsynaptic 5-HT1A receptor antagonist with a pKi of 9.2. S-14489 can act as a 5-HT1A autoreceptor agonist and inhibit striatal 5-hydroxytryptophan accumulation. S-14489 can be used for the research of neurological disease .
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- HY-10435
-
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(±)-SKF-82958; Chloro-APB
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Dopamine Receptor
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Neurological Disease
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SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
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- HY-W711852
-
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Benzenecarboxamide-d5; Phenylamide-d5
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Isotope-Labeled Compounds
PARP
Endogenous Metabolite
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Others
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Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-118706
-
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Dopamine Receptor
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Neurological Disease
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PD 118440 is an orally active dopamine (DA) agonist. PD 118440 has significant central nervous system effects, including inhibition of striatal DA synthesis, suppression of DA neuron firing, and reversal of Reserpine (HY-N0480)-induced depression in rats .
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-
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- HY-12294B
-
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(Rac)-NVP-AAM077
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iGluR
Caspase
Apoptosis
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Neurological Disease
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(Rac)-PEAQX is a NMDA receptor agonist. (Rac)-PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
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- HY-116550
-
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Dopamine Transporter
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Neurological Disease
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Piroheptine hydrochloride is an anticholinergic agent to inhibit dopamine uptake. Piroheptine hydrochloride prevents loss of striatal dopamine induced by MPTP (HY-15608). Piroheptine hydrochloride can be used for research in Parkinson .
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- HY-118461
-
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Dopamine Receptor
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Neurological Disease
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PD 120697 is an orally active dopamine (DA) agonist. PD 120697 inhibits striatal DA synthesis, DA neuronal firing, spontaneous locomotor activity, and reverses Reserpine (HY-N0480)-induced depression .
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- HY-129682
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-
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- HY-117838
-
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Phosphodiesterase (PDE)
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Neurological Disease
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Phosphodiesterase 10-IN-2 (THPP-4) is an oral active phosphodiesterase 10A (PDE10A) inhibitor with the Ki of 4.5 nM. Phosphodiesterase 10-IN-2 can be used for study of schizophrenia .
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- HY-W008610
-
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Dopamine Receptor
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Neurological Disease
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GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats .
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- HY-P1303A
-
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-105793
-
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mAChR
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Neurological Disease
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Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
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- HY-B1124AR
-
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Adenylate Cyclase
Dopamine Transporter
Reference Standards
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Neurological Disease
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Fipexide (hydrochloride) (Standard) is the analytical standard of Fipexide (hydrochloride). This product is intended for research and analytical applications. Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research. Fipexide hydrochloride acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection .
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- HY-B1124R
-
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Reference Standards
Adenylate Cyclase
Dopamine Transporter
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Neurological Disease
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Fipexide (Standard) is the analytical standard of Fipexide. This product is intended for research and analytical applications. Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection .
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- HY-W686216
-
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Dopamine Receptor
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Neurological Disease
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VK-28 is a blood-brain barrier-permeable iron chelator. VK-28 inhibits mitochondrial membrane lipid peroxidation and the iron-dependent generation of reactive hydroxyl radicals. VK-28 exhibits neuroprotective activity and protects rats against 6-OHDA-induced striatal dopaminergic damage. VK-28 can be used in studies related to Parkinson's disease .
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- HY-Z0283R
-
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Benzenecarboxamide (Standard); Phenylamide (Standard)
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Reference Standards
Endogenous Metabolite
PARP
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Others
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Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-10435AR
-
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(±)-SKF-82958 hydrobromide (Standard); Chloro-APB hydrobromide (Standard)
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Reference Standards
Dopamine Receptor
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Neurological Disease
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SKF-82958 (hydrobromide) (Standard) is the analytical standard of SKF-82958 (hydrobromide). This product is intended for research and analytical applications. SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM) .
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- HY-107969R
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Dopamine Receptor
Reference Standards
COX
NO Synthase
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Neurological Disease
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Haloperidol decanoate (Standard) is the analytical standard of Haloperidol decanoate. This product is intended for research and analytical applications. Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
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- HY-131885
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GABA Receptor
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Neurological Disease
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RuBi-Glutamate hexafluorophosphate sodium is a neuronal activator. RuBi-Glutamate hexafluorophosphate sodium photocleaves to release glutamate upon one- or two-photon excitation, activating glutamate receptors in cortical pyramidal neurons. RuBi-Glutamate hexafluorophosphate sodium reduces peak amplitude of evoked GABAergic inhibitory postsynaptic currents in its caged form. RuBi-Glutamate hexafluorophosphate sodium can be used for the research of Huntington's disease .
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- HY-116450
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Dopamine Receptor
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Neurological Disease
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TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
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- HY-171328
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Dopamine Receptor
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Neurological Disease
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RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [ 35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity .
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- HY-101343
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5-HT Receptor
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Neurological Disease
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RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
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- HY-138232
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LTNAM
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Aminopeptidase
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Neurological Disease
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Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
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- HY-B0590E
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Ro 1-9569 mesylate
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Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-B0590R
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Ro 1-9569 (Standard)
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Reference Standards
Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-B0590S3
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TBZ-d7-d7; Ro 1-9569-d7
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Isotope-Labeled Compounds
Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-182484
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GlyT
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Neurological Disease
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Org 24461 is a selective and brain-penetrant GlyT-1 inhibitor. Org 24461 blocks glycine uptake, reuptake, reverse operation, [ 3H]glycine efflux and release. Org 24461 enhances NMDA receptor function, modulates striatal monoamine/glutamate levels, and reverses PCP-induced behavioral and electrographic abnormalities. Org 24461 can be used for the research of retinal hypoxia/ischemia, and schizophrenia .
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- HY-B0884AR
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Reference Standards
Monoamine Oxidase
Cholinesterase (ChE)
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Neurological Disease
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Minaprine dihydrochloride (Standard) is the analytical standard of Minaprine dihydrochloride (HY-B0884A). This product is intended for research and analytical applications. Minaprine dihydrochloride is a brain-penetrant monoamine oxidase inhibitor. Minaprine dihydrochloride also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine dihydrochloride reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine dihydrochloride exhibits convulsant, antidepressant properties .
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- HY-106366
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Drug Derivative
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Neurological Disease
Inflammation/Immunology
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Siagoside is an inner ester of Ganglioside GM1 (HY-N10546). Siagoside selectively attenuates morphological and functional striatal impairments induced by transient forebrain ischemia in rats. Siagoside can be used for the research of neurological disease, such as acute cerebral ischemia .
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- HY-180422
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Dopamine Receptor
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Neurological Disease
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(-)-UH 232 is a central dopamine (DA) receptor agonist. (-)-UH 232 weakly decreases 3, 4-dihydroxyphenylalanine (DOPA) formation in striatal and limbic brain regions in rats. (-)-UH 232 can be used for the research of neurological diseases including parkinson's disease and schizophrenia .
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- HY-107674R
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Reference Standards
nAChR
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Neurological Disease
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bPiDDB (Standard) is the analytical standard of bPiDDB (HY-107674). This product is intended for research and analytical applications. bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
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- HY-108942
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Adenosine Receptor
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Cardiovascular Disease
Neurological Disease
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ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease .
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- HY-183665
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Dopamine Receptor
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Neurological Disease
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GBR-13119 is a blood-brain barrier-permeable inhibitor of the presynaptic dopamine uptake system. GBR-13119 binds to dopamine uptake sites with high selectivity, without being affected by other neurotransmitter reuptake inhibitors. GBR-13119 exhibits a lipophilic systemic distribution profile with extremely low defluorination in rats, while it shows a differential characteristic of slow striatal washout in the brain of primates. GBR-13119 can serve as a PET tracer to achieve visualized imaging of the striatum in primates, and can reflect MPTP-induced dopaminergic neuron degeneration through reduced uptake. GBR-13119 can be widely applied to studies related to Parkinson's disease and dopaminergic neuron degeneration .
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- HY-W700204
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Dopamine Receptor
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Neurological Disease
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N-(p-Aminophenethyl) spiperone is a selective D2-like dopamine receptor antagonist. N-(p-Aminophenethyl) spiperone binds to the ligand recognition sites of functional D2 and D3 dopamine receptors. N-(p-Aminophenethyl) spiperone serves as a research tool compound for labeling, localizing and identifying D2 and D3 dopamine receptors .
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- HY-124186
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Dopamine Receptor
5-HT Receptor
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Neurological Disease
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LR1143 is a dopamine transporter (DAT) and 5-HT uptake inhibitor, with IC50 values of 3.4 nM and 112 nM in rats, respectively. LR1143 binds to DAT labeled with the dopamine reuptake inhibitor GBR 12935 (HY-12242A), with an IC50 of 4.4 nM. LR1143 shows lower selectivity for DAT than for serotonin reuptake sites. LR1143 can be used in studies related to cocaine abuse .
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- HY-182381
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Dopamine Receptor
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Neurological Disease
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FLA-797 is a brain-penetrant dopamine D2 receptor blocker and very low affinity for dopamine D1 receptors. FLA-797 selectively binds to and blocks postsynaptic dopamine D2 receptors. FLA-797 induces catalepsy in male rats. FLA-797 blocks dopamine agonist-induced hypothermia in male rats. FLA-797 contributes marginally to the dopamine D2 receptor-blocking activity of Remoxipride (HY-101313) in male rats. FLA-797 does not mimic the atypical antipsychotic profile of Remoxipride. FLA-797 can be used for research on mental disorders .
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- HY-186130
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Calpain
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Neurological Disease
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CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies .
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- HY-182600
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Kallikrein
Plasminogen/Plasmin
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Neurological Disease
Inflammation/Immunology
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KLK6-IN-1 is a reversible small‑molecule inhibitor of KLK6, KLK1, and plasmin. KLK6-IN-1 shows IC50 values of 1.57 μM (KLK6), 5.1 μM (KLK1), 7.4 μM (plasmin), and Ki values of 0.8 μM (KLK6), 2.4 μM (KLK1), 1.3 μM (plasmin). KLK6-IN-1 is highly selective for KLK6 and its proteolytic network. KLK6-IN-1 induces oligodendrocyte differentiation by promoting oligodendrocyte precursor cell maturation. KLK6-IN-1 can be used for the research of multiple sclerosis .
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- HY-183927
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Dopamine Receptor
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Neurological Disease
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Spectramide is a blood-brain barrier-permeable, reversible, and selective dopamine D2 receptor ligand. Spectramide shows no strong interactions with dopamine D1 receptors, dopamine uptake sites, adrenergic receptor systems, cholinergic receptor systems, or 5-HTR systems. Spectramide can be labeled with 11C or 123I isotopes for use in PET or SPECT. Spectramide preferentially accumulates in the striatum with low uptake in other brain regions, and its accumulation can be blocked by pre-administration of Haloperidol (HY-14538) .
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- HY-182456
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KMO
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Neurological Disease
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CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease .
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Product Name |
Target |
Research Area |
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- HY-145512
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NLT
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Dopamine Receptor
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Neurological Disease
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N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
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- HY-P1206
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CH 275
1 Publications Verification
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Somatostatin Receptor
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Neurological Disease
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CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
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- HY-P4532
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Cathepsin
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Neurological Disease
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Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II .
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- HY-P1303
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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- HY-P1303A
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5-HT Receptor
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Neurological Disease
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CART(62-76)(human,rat) TFA is a neuropeptide (62-76 residues of the CART peptide) with neurotransmitter-like effects. CART(62-76)(human,rat) TFA can modulate the activity of striatal noradrenergic and corticostriatal and hypothalamic serotoninergic (5-HT) system in the rat brain .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0590S
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Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-W711852
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Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-B0590S3
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Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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