| Description |
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM[1][3].
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| Related Catalog |
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| Target |
IC50: 0.145 μM (mGlu1), 0.91 μM (EGFR)[1]
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| In Vitro |
LY456236 (2 μM; 30 min) 降低 DHPG (HY-12598A) 刺激的 OCCM-30 增殖[2]。 Cell Proliferation Assay[2] Cell Line: OCCM-30 cells Concentration: 2 μM Incubation Time: 30 min, followed by 72 h incubation with DHPG (HY-12598A) Result: Reduced DHPG-stimulated OCCM-30 proliferation.
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| In Vivo |
LY456236 在小鼠 (3-100 mg/kg; i.p.; once) 和大鼠 (10-60 mg/kg; oral; once) 中显示抗惊厥作用。 Animal Model: DBA/2 mice and CD1 mice, seizure models[3] Dosage: 3-100 mg/kg Administration: IP, once Result: Produced dose-related anticonvulsant effects in preventing audiogenic-induced (tonic-clonic) seizures in DBA/2 mice, threshold electroshock-induced seizures in CD1 mice, and 6 Hz electroshock-induced seizures in CD1 mice. Animal Model: Amygdala-kindled Sprague-Dawley rats[3] Dosage: 10, 30 and 60 mg/kg Administration: Oral, once Result: Produced dose-related decreases in behavioral and electrographic seizures at threshold stimulus intensity. Produced a dose-related increase in the stimulus intensity required to produce generalized seizures.
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| References |
[1]. Ravikumar B, et al. Chemogenomic Analysis of the Druggable Kinome and Its Application to Repositioning and Lead Identification Studies. Cell Chem Biol. 2019 Nov 21;26(11):1608-1622.e6. [2]. Kanaya S, et al. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. [3]. Shannon HE, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95.
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