54 Results for "

synaptic blocking

" in MedChemExpress (MCE) Product Catalog:
Products (54)

54 Results for "synaptic blocking" in MCE Product Catalog:

Art. -Nr.: HY-A0022
CAS. Nr.: 24853-80-3
Synonyms: Azafen; Pipofezin hydrochloride; Pipofezine hydrochloride
Azaphen (Azafen) is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen can be used in studies related to depression .
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Art. -Nr.: HY-W004464
CAS. Nr.: 20980-22-7
2-(1-Piperazinyl)pyrimidine is an orally effective α2-adrenoceptor antagonist and 5-HT1A receptor agonist. 2-(1-Piperazinyl)pyrimidine is an in vivo metabolite related to buspirone. 2-(1-Piperazinyl)pyrimidine modulates excitatory synaptic transmission in the hippocampus and the release of monoamine transmitters such as norepinephrine and 5-HT by blocking α2-adrenoceptor and activating 5-HT1A Receptor. 2-(1-Piperazinyl)pyrimidine is used in research on psychiatric disorders such as anxiety and depression .
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Art. -Nr.: HY-100714B
CAS. Nr.: 79055-67-7
Synonyms: L-APV; L-2-Amino-5-phosphonovaleric acid
Target:  

iGluR

Forschungsgebiete:  

Neurological Disease

L-AP5 (L-APV; L-2-Amino-5-phosphonovaleric acid) is an NMDA antagonist and is the isomer of D-AP5 (HY-100714A). L-AP5 shows a relatively weak amino acid and synaptic blocking activity .
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Art. -Nr.: HY-107605
CAS. Nr.: 745055-86-1
Target:  

iGluR

Forschungsgebiete:  

Neurological Disease

UBP296 is a potent and selective antagonist of GLUK5-containing kainate receptor in the spinal cord. UBP296 reversibly blocks ATPA-induced depressions of synaptic transmission, and affects AMPA receptor-mediated synaptic transmission directly in rat hippocampal slices .
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Art. -Nr.: HY-P1054
CAS. Nr.: 1315378-67-6
Synonyms: YNVYGIEEVKI
Target:  

PKC

Forschungsgebiete:  

Neurological Disease

pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively blocks PICK1 interactions, caused the opposite effects on synaptic AMPAR function to PICK1 expression .
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Art. -Nr.: HY-100785A
CAS. Nr.: 2935387-13-4
Synonyms: γDGG acetate; γ-D-Glutamylglycine acetate
Target:  

iGluR

Forschungsgebiete:  

Neurological Disease

gamma-DGG acetate (γDGG acetate) is a competitive AMPA receptor blocker. gamma-DGG acetate is also a reversible Excitatory post-synaptic potentials (e.p.s.p.s) antagonist .
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Art. -Nr.: HY-P0062A
Synonyms: SNX-111 TFA
Ziconotide TFA (SNX-111 TFA), a peptide, is a potent and selective block of N-type calcium channels antagonist. Ziconotide TFA reduces synaptic transmission, and can be used for chronic pain research .
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Art. -Nr.: HY-169871
CAS. Nr.: 105029-41-2
Argiotoxin 636 is a toxin and the non-specific, non-competitive, and potent ionotropic glutamate receptor (iGluR) antagonist. Argiotoxin 636 blocks excitatory synaptic transmission in neurons and has paralysis and muscle relaxation effects. Argiotoxin 636 can be used in the study of nervous system diseases .
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Art. -Nr.: HY-P10630
CAS. Nr.: 1781242-18-9
Target:  

Amyloid-β

Forschungsgebiete:  

Neurological Disease

Pep63 is a neuroprotective peptide (VFQVRARTVA). Pep63 has a neuroprotective effect on synaptic plasticity and memory. Pep63 can competitively bind with Aβ1-42 oligomers, and can block Aβ fiber formation. Pep63 can be used for Alzheimer’s disease (AD) research .
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Art. -Nr.: HY-175300
CAS. Nr.: 2421120-68-3
Target:  

Cholinesterase (ChE)

Forschungsgebiete:  

Neurological Disease

AChE-IN-92 (Compound L4R1-3) is a highly selective acetylcholinesterase (AChE) inhibitor (IC50=4.6 nM). AChE-IN-92 blocks acetylcholine hydrolysis and elevates synaptic acetylcholine levels. AChE-IN-92 is promising for research of Alzheimer’s disease (AD) .
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Art. -Nr.: HY-B0590E
CAS. Nr.: 804-53-5
Synonyms: Ro 1-9569 mesylate
Forschungsgebiete:  

Neurological Disease

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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Art. -Nr.: HY-B1789
CAS. Nr.: 80880-90-6
Target:  

mAChR

Forschungsgebiete:  

Neurological Disease

Telenzepine is an antimuscarinic agent with Kis of 0.94 nM (M1 mAChR) and 17.8 nM (M2 mAChR) binding to muscarinic receptors. Telenzepine effectively blocks synaptic transmission promoted by muscarinic or M1 receptor agonists. Thus, Telenzepine can reduce the amplitude of extracellular slow excitatory postsynaptic potentials (EC50=38 nM) and slow inhibitory postsynaptic potentials (EC50=253 nM) .
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Art. -Nr.: HY-108578
CAS. Nr.: 851956-02-0
Target:  

Potassium Channel

Forschungsgebiete:  

Neurological Disease

RuBi-4AP, a derivative of 4-aminopyridine (4AP; HY-B0604), is a caged Kv channel blocker. RuBi-4AP contains a photolabile protecting group, allowing its effect to be controlled precisely in both space and time with light. RuBi-4AP can be used for the research of neuronal excitability, synaptic transmission, and signal propagation .
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Art. -Nr.: HY-B0590R
CAS. Nr.: 58-46-8
Synonyms: Ro 1-9569 (Standard)
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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Art. -Nr.: HY-B0590S3
CAS. Nr.: 2701977-99-1
Synonyms: TBZ-d7-d7; Ro 1-9569-d7
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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Art. -Nr.: HY-W278867R
CAS. Nr.: 21956-56-9
Synonyms: trans-Pinosylvin dimethyl ether (Standard)
trans-3,5-Dimethoxystilbene (Standard) is the analytical standard of trans-3,5-Dimethoxystilbene (HY-W278867). This product is intended for research and analytical applications. trans-3,5-Dimethoxystilbene (trans-Pinosylvin dimethyl ether) is a natural stilbenoid metabolite. trans-3,5-Dimethoxystilbene acts as an acetylcholinesterase inhibitor with a IC50 of 9 μM against Electrophorus electricus acetylcholinesterase. trans-3,5-Dimethoxystilbene binds to acetylcholinesterase and blocks acetylcholine hydrolysis, thereby increasing acetylcholine levels in the cholinergic synaptic cleft. trans-,5-Dimethoxystilbene can be used in the research of neurodegenerative diseases such as Alzheimer's disease .
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Art. -Nr.: HY-W004464R
CAS. Nr.: 20980-22-7
2-(1-Piperazinyl)pyrimidine Standard is the analytical standard of 2-(1-Piperazinyl)pyrimidine (HY-W004464). This product is intended for research and analytical applications. 2-(1-Piperazinyl)pyrimidine is an orally effective α2-adrenoceptor antagonist and 5-HT1A receptor agonist. 2-(1-Piperazinyl)pyrimidine is an in vivo metabolite related to buspirone. 2-(1-Piperazinyl)pyrimidine modulates excitatory synaptic transmission in the hippocampus and the release of monoamine transmitters such as norepinephrine and 5-HT by blocking α2-adrenoceptor and activating 5-HT1A Receptor. 2-(1-Piperazinyl)pyrimidine is used in research on psychiatric disorders such as anxiety and depression .
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Art. -Nr.: HY-103430
CAS. Nr.: 108179-91-5
SKF-83566 hydrobromide is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM. SKF-83566 hydrobromide modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 hydrobromide acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 hydrobromide competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 hydrobromide is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
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Art. -Nr.: HY-W795736
CAS. Nr.: 112709-60-1
Synonyms: (+)-AH5183
Target:  

nAChR

Forschungsgebiete:  

Neurological Disease

(+)-Vesamicol ((+)-AH5183) is an acetylcholine vesicular transport system inhibitor. (+)-Vesamicol blocks acetylcholine storage and uptake by synaptic vesicles, reducing transmitter availability for neuromuscular junction release. (+)-Vesamicol acts as a neuromuscular blocking agent, producing frequency-dependent neuromuscular block in rat hemidiaphragm preparations .
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Art. -Nr.: HY-118278
CAS. Nr.: 161832-71-9
Synonyms: LY303070
Target:  

iGluR

GYKI 53784 (LY303070) is an orally active, blood-brain penetrant, selective, non-competitive AMPA receptor antagonist (IC50 = 0.32 μM). GYKI 53784 completely blocks AMPA-mediated synaptic transmission, protects against excitotoxicity, and partially inhibits Kainite (Kainic acid) (HY-N2309) responses, revealing both AMPA and kainate receptors. GYKI 53784 selectively blocks synaptic transmission (IC50 = 365.3 nM) without affecting neuronal excitability, and exhibits potent stereoselective antinociceptive effects via an opioid-independent mechanism. GYKI 53784 is a versatile tool for studying AMPA receptor function in synaptic transmission, excitotoxicity, neuroprotection, pain, and inflammation, with potential relevance to hearing loss, neonatal ischemia, neurodegenerative disorders, schizophrenia, and Alzheimer's disease .
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