化合物LY404039 T6022

Product Introduction
Bioactivity


英文名: LY404039

描述: LY404039 (pomaglumetad) 是可口服的mGluR2和mGluR3选择性激动剂，有抗精神病和抗焦虑的作用。它对重组人mGluR2和mGluR3的Ki 分别为 149 和 92 nM，比对其他受体/转运蛋白的抑制性高 100 倍以上。

激酶实验: Immunoblotting assay of histone acetylation: PANC-1 cells are treated with 2 μg/mL of Scriptaid for 18 h in culture medium. Treated and untreated cells are harvested with trypsin-EDTA, washed with PBS, and resuspended in a protein sample buffer. Protein concentration is determined by BCA protein assay reagents. Fifty μg of proteins from each sample is loaded on a 12% denaturing polyacrylamide gel. Proteins are subsequently transferred to a nylon membrane using MilliblotGraphite Electroblotter I. The nylon membrane is incubated with rabbit antihuman acetyl-lysine antibody, followed by goat antirabbit antibody coupled to horseradish peroxidase, developed with SuperSignal substrates, and detected by film.

体内活性: LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis. [1] In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice. [2] LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior. [3] Moreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex. [4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : Slightly soluble


关键字: inhibit | Metabotropic glutamate receptors | mGluR | cAMP | LY-404039 | mGlu3 | LY404039 | L-glutamate | mGlu2 | Inhibitor | LY 404039 | anxiolytic | antipsychotic

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相关库: Neurotransmitter Receptor Compound Library | Anti-Cancer Compound Library | Glutamine Metabolism Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Nuclear Receptor Compound Library | Endocrinology-Hormone Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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