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rat brain slices

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5

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P2259
    TAT-GluA2 3Y
    2 Publications Verification

    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 .
    TAT-GluA2 3Y
  • HY-138232

    LTNAM

    Aminopeptidase Neurological Disease
    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.
    Lys-psi(CH2NH)-Trp(Nps)-OMe
  • HY-186094

    Drug Derivative Drug Intermediate Neurological Disease
    (S,S)-Demethyl-reboxetine is a key phenolic precursor for the preparation of the PET tracer (S,S)-[ 11C]-MeNER. (S,S)-Demethyl-reboxetine is also the demethylated derivative of Reboxetine (HY-14560). Efficient synthesis of the norepinephrine transporter (NET)-targeted tracer is achieved through 11C methylation of (S,S)-Demethyl-reboxetine. (S,S)-Demethyl-reboxetine serves as a core raw material for the synthesis of radiopharmaceuticals related to NET imaging .
    (S,S)-Demethyl-reboxetine
  • HY-182944

    GABA Receptor Neurological Disease
    GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC50 of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated 18F-radiofluorination. The radiolabeled GATT-44 ([ 18F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases .
    GATT-44
  • HY-182548

    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

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