Search Result
Results for "
synaptic blocking
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0527A
-
|
|
Serotonin Transporter
5-HT Receptor
mAChR
Histamine Receptor
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
-
- HY-B0527
-
|
|
Serotonin Transporter
Trk Receptor
Sodium Channel
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
mAChR
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
|
-
-
- HY-103259
-
-
-
- HY-P0062B
-
-
-
- HY-B0590
-
|
Ro 1-9569
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-B0590S
-
|
Ro 1-9569-d6
|
Monoamine Transporter
|
Neurological Disease
|
|
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 .
|
-
-
- HY-10035
-
TTA-P2
2 Publications Verification
T-Type calcium channel inhibitor
|
Calcium Channel
|
Neurological Disease
|
|
TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup>[4] .
|
-
-
- HY-134356
-
|
AICAR-5'-MP
|
Endogenous Metabolite
|
Others
|
|
AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
|
-
-
- HY-P0062
-
-
-
- HY-113788
-
|
|
Pyk2
p38 MAPK
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
PF-719 is a highly selective Pyk2 inhibitor with an IC50 value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases .
|
-
-
- HY-P2259
-
|
|
iGluR
|
Neurological Disease
|
|
TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .
|
-
-
- HY-B0590A
-
|
Ro 1-9569 Racemate
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-164288
-
|
TDI-006570
|
Cyclic GMP-AMP Synthase
STING
|
Neurological Disease
Inflammation/Immunology
|
|
TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC50 of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .
|
-
-
- HY-113995
-
|
(-)-AH5183
|
mAChR
|
Neurological Disease
|
|
(-)-Vesamicol (AH5183) is a vesicular acetylcholine transporter inhibitor. (-)-Vesamicol reversibly and non-competitively inhibits the transport of acetylcholine into circulating synaptic vesicles and blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons. (-)-Vesamicol is applicable to research related to central precocious puberty .
|
-
-
- HY-P0099
-
|
|
nAChR
|
Others
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
-
-
- HY-121964
-
|
|
iGluR
|
Neurological Disease
|
|
Cis-piperidine-2,3-dicarboxylic acid is a non-specific antagonist of NMDA, AMPA and kainate ionotropic receptors and a partial agonist for NMDA receptors. Cis-piperidine-2,3-dicarboxylic acid can be used in blocking general excitatory synaptic transmissions .
|
-
-
- HY-B0527AR
-
|
|
Reference Standards
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
-
- HY-B0527AS
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
5-HT Receptor
Histamine Receptor
mAChR
Adrenergic Receptor
Trk Receptor
Sodium Channel
Potassium Channel
Dopamine Transporter
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
-
- HY-100714B
-
|
L-APV; L-2-Amino-5-phosphonovaleric acid
|
iGluR
|
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 .
|
-
-
- HY-107605
-
|
|
iGluR
|
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 .
|
-
-
- HY-P1054
-
|
YNVYGIEEVKI
|
PKC
|
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 .
|
-
-
- HY-100785A
-
|
γDGG acetate; γ-D-Glutamylglycine acetate
|
iGluR
|
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 .
|
-
-
- HY-P0062A
-
-
-
- HY-169871
-
|
|
iGluR
|
Neurological Disease
|
|
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 .
|
-
-
- HY-P10630
-
|
|
Amyloid-β
|
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 .
|
-
-
- HY-175300
-
|
|
Cholinesterase (ChE)
|
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) .
|
-
-
- HY-B0590E
-
|
Ro 1-9569 mesylate
|
Monoamine Transporter
Dopamine Receptor
|
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 .
|
-
-
- HY-B1789
-
|
|
mAChR
|
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) .
|
-
-
- HY-108578
-
|
|
Potassium Channel
|
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 .
|
-
-
- HY-B0590R
-
|
Ro 1-9569 (Standard)
|
Reference Standards
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-B0590S3
-
|
TBZ-d7-d7; Ro 1-9569-d7
|
Isotope-Labeled Compounds
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
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 .
|
-
-
- HY-W795736
-
|
(+)-AH5183
|
nAChR
|
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 .
|
-
-
- HY-183910
-
|
|
GABA Receptor
Glycine Receptor (GlyR)
|
Neurological Disease
|
|
Pitrazepin is a GABAA receptor antagonist and glycine receptor antagonist. Pitrazepin blocks synaptic GABA action, induces neuronal bursting and reduces inhibitory postsynaptic potentials. Pitrazepin can be used in research on depression and psychosis .
|
-
-
- HY-183269
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a Ki of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression .
|
-
-
- HY-180370
-
|
NitroSynapsin; YQW-036; NMI-6979
|
iGluR
Drug Derivative
|
Cardiovascular Disease
Neurological Disease
|
|
Nitromemantine (NitroSynapsin) is a nitrate derivative of Memantine (HY-B0591) and is a dual-functional NMDAR antagonist. Nitromemantine exhibits significant efficacy in rodent models of cerebral infarction through a dual mechanism of blocking channels and regulating receptors via NO/redox regulation. Nitromemantine can target ischemic neurons under hypoxic conditions and enhance its activity. Nitromemantine inhibits the current induced by NMDA, with its IC50 being 2.4 μM. Nitromemantine can be used for the study of cerebral ischemic stroke .
|
-
-
- HY-10035R
-
|
T-Type calcium channel inhibitor (Standard)
|
Calcium Channel
Reference Standards
|
Neurological Disease
|
|
TTA-P2 (Standard) is the analytical standard of TTA-P2 (HY-10035). This product is intended for research and analytical applications. TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy < sup> .
|
-
-
- HY-182707
-
|
|
nAChR
Interleukin Related
TNF Receptor
NF-κB
|
Neurological Disease
|
|
JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0062B
-
-
- HY-P0062
-
-
- HY-P2259
-
|
|
iGluR
|
Neurological Disease
|
|
TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression .
|
-
- HY-P0099
-
|
|
nAChR
|
Others
|
|
Pentapeptide-3 is a pentapeptide fragment of neurotoxin waglerin-1, it can be extracted from the venom of Temple Viper. Pentapeptide-3 is a competitive antagonist of nicotinic acetylcholine receptors (nAChRs), it can blocks nerves at the post-synaptic membrane. Pentapeptide-3 has anti-aging effects and it can be used together with other cosmetic peptides .
|
-
- HY-P1054
-
|
YNVYGIEEVKI
|
PKC
|
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 .
|
-
- HY-P0062A
-
-
- HY-P10630
-
|
|
Amyloid-β
|
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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-134356
-
|
AICAR-5'-MP
|
Human Gut Microbiota Metabolites
Classification of Application Fields
Other Diseases
Endogenous metabolite
Disease Research Fields
Source Classification
|
Endogenous Metabolite
|
|
AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
|
-
-
- HY-169871
-
|
|
Animals
Phenols
Polyphenols
Animal Venoms
Source Classification
|
iGluR
|
|
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 .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0590S
-
|
|
|
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 .
|
-
-
- HY-B0527AS
-
|
|
|
Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
|
-
-
- HY-B0590S3
-
|
|
|
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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