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glycine receptor blocker

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

3

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-113329
    Guanidinoethyl sulfonate
    5 Publications Verification

    Taurocyamine

    		 Endogenous Metabolite Metabolic Disease
    Guanidinoethyl sulfonate (Taurocyamine) is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
    Guanidinoethyl sulfonate
  • HY-I0096
    Indole-2-carboxylic acid

    		iGluR HIV HIV Integrase Neurological Disease
    Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (Ki=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg 2+ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection .
    Indole-2-carboxylic acid
  • HY-18698
    L-701324

    		iGluR Neurological Disease
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
    L-701324
  • HY-100822
    (R)-(+)-HA-966

    (+)-HA-966

    		 iGluR Neurological Disease
    (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine . (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain .
    (R)-(+)-HA-966
  • HY-113329R
    Guanidinoethyl sulfonate (Standard)

    Taurocyamine (Standard)

    		 Endogenous Metabolite Reference Standards Metabolic Disease
    Guanidinoethyl sulfonate (Standard) is the analytical standard of Guanidinoethyl sulfonate. This product is intended for research and analytical applications. Guanidinoethyl sulfonate is an orally available, blood-brain permeable competitive inhibitor of taurine transporters and a competitive antagonist of glycine receptors (GlyR) (IC50=565 μM). Guanidinoethyl sulfonate has both weak agonist and antagonist effects on GABAA receptors. Guanidinoethyl sulfonate inhibits taurine transmembrane transport and competitively binds to the GlyR ligand binding domain, thereby blocking glycine-mediated chloride influx, and may regulate brain pH to exert neuroprotective effects. Guanidinoethyl sulfonate can be used for neuroprotection studies of ischemic brain injury .
    Guanidinoethyl sulfonate (Standard)
  • HY-B0884
    Minaprine

    		Monoamine Oxidase Cholinesterase (ChE) Neurological Disease
    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 .
    Minaprine
  • HY-W424730
    HA-966 hydrochloride

    		iGluR Others
    HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
    HA-966 hydrochloride
  • HY-103570
    MCPG sodium

    		mGluR Neurological Disease
    MCPG is a carboxylic phenyl glycine. MCPG can block metabotropic glutamate receptor (mGluR)(HY-15129) and has antagonistic activity of mGluR subtype. MCPG can be used to study the induction and maintenance of long-term potentiation (LTP) .
    MCPG sodium
  • HY-183910
    Pitrazepin

    		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 .
    Pitrazepin
  • HY-182484
    Org 24461

    		GlyT Neurological Disease
    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 .
    Org 24461
  • HY-131691
    NMDAR blocker 1

    		iGluR Calcium Channel Neurological Disease
    NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca 2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases .
    NMDAR blocker 1
  • HY-182548
    BTS 72664

    		GABA Receptor Sodium Channel iGluR Cardiovascular Disease Neurological Disease
    BTS 72664 is a broad-spectrum, non-sedating, orally effective anticonvulsant. Its anticonvulsant effect mainly arises from enhancing GABAA receptor (GABAA receptor)-mediated chloride channel currents, while it exerts weak blocking effects on Na + channels (Ki = 350 μM) and NMDA receptors (NMDA receptor) (IC50 = 43 μM). BTS 72664 prevents the elevation of extracellular glutamate, glycine and serine concentrations in neurons, reduces cerebral infarct size, promotes functional recovery, prevents multiple types of epileptic seizures, and has low sedative potential. BTS 72664 can be used for the research of epilepsy, stroke and migraine .
    BTS 72664
  • HY-100822R
    (R)-(+)-HA-966 (Standard)

    (+)-HA-966 (Standard)

    		 iGluR Reference Standards Neurological Disease
    (R)-(+)-HA-966 (Standard) is the analytical standard of (R)-(+)-HA-966 (HY-100822). This product is intended for research and analytical applications. (R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine . (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain .
    (R)-(+)-HA-966 (Standard)

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