Search Result
Results for "
rat brain neurons
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-10864
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URB-597
5 Publications Verification
KDS-4103
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FAAH
Autophagy
Mitophagy
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Neurological Disease
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URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
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- HY-100834
-
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5,7-DCKA
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iGluR
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Neurological Disease
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5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
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- HY-120751
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Calcium Channel
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Neurological Disease
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TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
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- HY-B0596
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TA-0910
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Thyroid Hormone Receptor
Apoptosis
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Neurological Disease
Endocrinology
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Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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- HY-14604
-
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SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
Trk Receptor
PKC
ERK
Akt
JNK
|
Neurological Disease
Metabolic Disease
|
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Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
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- HY-N2160
-
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GABA Receptor
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Neurological Disease
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6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons .
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- HY-U00050
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E-10-OH-NT
|
Drug Metabolite
Adrenergic Receptor
mAChR
|
Neurological Disease
|
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(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a blood-brain barrier-permeable norepinephrine uptake inhibitor. (E)-10-Hydroxynortriptyline effectively promotes central norepinephrine neuronal transmission, with little interindividual variation in in vivo potency. (E)-10-Hydroxynortriptyline has low affinity for muscarinic receptors, exhibits only extremely weak anticholinergic activity, and does not inhibit salivary secretion. (E)-10-Hydroxynortriptyline can be used in studies related to depression .
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- HY-168906
-
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Bradykinin Receptor
PI3K
Akt
TNF Receptor
ERK
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Neurological Disease
Inflammation/Immunology
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BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
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- HY-P2259
-
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iGluR
HIV Integrase
Adenosine Receptor
|
Cardiovascular Disease
Neurological Disease
|
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TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .
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- HY-160959
-
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nAChR
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Neurological Disease
|
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AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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- HY-B0596A
-
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TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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- HY-W004425
-
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3,7-Dimethyl-1-propargylxanthine
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Adenosine Receptor
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Neurological Disease
|
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DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease .
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- HY-P3071
-
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Stichodactyla helianthus neurotoxin
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Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
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ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
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- HY-10864R
-
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KDS-4103 (Standard)
|
FAAH
Autophagy
Mitophagy
Reference Standards
|
Neurological Disease
|
|
URB-597 (Standard) is the analytical standard of URB-597. This product is intended for research and analytical applications. URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
|
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- HY-P3071A
-
|
Stichodactyla helianthus neurotoxin TFA
|
Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
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ShK toxin TFA (Stichodactyla helianthus neurotoxin TFA) is a neurotoxin. ShK toxin TFA blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin TFA can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin TFA competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin TFA suppresses K + currents in cultured rat dorsal root ganglion neurons. ShK toxin TFA also inhibits T lymphocyte proliferation .
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- HY-P1426
-
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Potassium Channel
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Neurological Disease
|
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AmmTX3 is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 can be used in research related to pain, epilepsy, and autism spectrum disorder .
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- HY-178153
-
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iGluR
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Neurological Disease
|
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BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
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- HY-100458
-
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NO Synthase
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Neurological Disease
|
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SCR-4026 is a neuroprotective agent with blood-brain barrier penetration ability. SCR-4026 exerts neuroprotective effects by disrupting the interaction between neuronal nNOS and PSD9, with an IC50 of 6.3 μM. SCR-4026 alleviates N-methyl-D-aspartate (NMDA)-induced excitotoxic damage in primary cortical neurons, and also protects neurons in the oxygen-glucose deprivation (OGD) model. SCR-4026 can reduce the cerebral infarct volume in the rat middle cerebral artery occlusion (MCAO) reperfusion model. SCR-4026 can be used for the study of stroke .
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- HY-15076
-
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NS-1209 sodium
|
iGluR
|
Neurological Disease
|
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SPD-502 sodium is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 sodium effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 sodium may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity .
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- HY-15074
-
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NS-1209
|
iGluR
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Neurological Disease
|
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SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity .
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- HY-100834A
-
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5,7-DCKA sodium
|
iGluR
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Neurological Disease
|
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5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
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- HY-119820
-
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SR57746A free base
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Akt
Dopamine Receptor
Trk Receptor
5-HT Receptor
PKC
JNK
ERK
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Neurological Disease
|
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Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
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- HY-182631
-
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iGluR
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Neurological Disease
|
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CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression .
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- HY-186105A
-
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Opioid Receptor
Apoptosis
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Neurological Disease
|
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(-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease .
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- HY-182548
-
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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 .
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- HY-W714853
-
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Akt
Src
STAT
EGFR
Drug Isomer
|
Neurological Disease
Inflammation/Immunology
|
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(+)-Theta-cypermethrin is a stereoisomer of Cypermethrin (HY-B0829) that possesses blood-brain barrier penetration ability and binds to AKT1, SRC, STAT3 and EGFR with high affinity. (+)-Theta-cypermethrin reduces the amplitude of delayed rectifier potassium channel currents, shifts the steady-state activation curve to negative potentials, and shifts the steady-state inactivation curve to negative potentials at higher concentrations. (+)-Theta-cypermethrin induces abnormal electrical activity in rat hippocampal neurons. (+)-Theta-cypermethrin causes chronic respiratory system damage and exhibits neurotoxicity .
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-
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- HY-120751A
-
|
|
Drug Isomer
Calcium Channel
|
Neurological Disease
|
|
(S)-TROX-1 is the S-enantiomer of TROX-1 (HY-120751). TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC50 value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .
|
-
-
- HY-14604R
-
|
SR57746A (Standard); SR57746 hydrochloride (Standard)
|
Reference Standards
Akt
Dopamine Receptor
Trk Receptor
5-HT Receptor
PKC
JNK
ERK
|
Neurological Disease
Cancer
|
|
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2259
-
|
|
iGluR
HIV Integrase
Adenosine Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .
|
-
- HY-P3071
-
|
Stichodactyla helianthus neurotoxin
|
Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
ShK toxin blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin suppresses K+ currents in cultured rat dorsal root ganglion neurons. ShK toxin also inhibits T lymphocyte proliferation .
|
-
- HY-P3071A
-
|
Stichodactyla helianthus neurotoxin TFA
|
Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
ShK toxin TFA (Stichodactyla helianthus neurotoxin TFA) is a neurotoxin. ShK toxin TFA blocks voltage-dependent potassium channel (Kv1.3 channel). ShK toxin TFA can be isolated from the whole body extract of the Caribbean sea anemone (Stichodactylu helianthus). ShK toxin TFA competes with dendrotoxin I and α-dendrotoxin for binding to synaptosomal membranes of rat brain, facilitates acetylcholine release. ShK toxin TFA suppresses K + currents in cultured rat dorsal root ganglion neurons. ShK toxin TFA also inhibits T lymphocyte proliferation .
|
-
- HY-P1426
-
|
|
Potassium Channel
|
Neurological Disease
|
|
AmmTX3 is a peptide toxin identified from the venom of the scorpion Androctonus mauretanicus. AmmTX3 is a highly specific blocker of Kv4 channels, which selectively and almost completely blocks transient A-type K + currents with a Ki of 131 nM. AmmTX3 induces epileptiform behaviors and causes death in mice receiving intracerebroventricular injection. AmmTX3 increases the excitability of dentate gyrus granule cells, reduces GABAergic inhibition, enhances and stabilizes the EPSP-spike component of long-term potentiation, and impairs reference memory. AmmTX3 can be used in research related to pain, epilepsy, and autism spectrum disorder .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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