LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
- CAS号:198419-91-9
- 英文名:LY 367385
- 中文名:LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID
- CBNumber:CB5200038
- 分子式:C10H11NO4
- 分子量:209.2
- MOL File:198419-91-9.mol
- 储存条件 :Desiccate at RT
- 溶解度 :H2O: >10mg/mL
- 形态 :powder
- 颜色 :white to off-white
- WGK Germany :3
LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID性质、用途与生产工艺
- 生物活性 LY367385 是一种高效且选择性的 mGluR1a 拮抗剂,抑制喹喹啉诱导的磷酸肌醇水解的 IC50 值为 8.8 μM,而对 mGlu5a 的 IC50 值大于 100 μM。LY367385 具有神经保护,抗惊厥和抗癫痫作用。
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靶点
mGluR1a
8.8 μM (IC 50 )
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体外研究
LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse attenuates neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se. LY367385 shows potent neuroprotective effects, with causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. Under experimental conditions at higher concentrations of antagonist, LY367385 a completely antagonized the amplification of NMDA toxicity by DHPG.
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体内研究
LY367385 has been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). In DBA/2 mice, LY367385 produces a rapid, transient suppression of sound-induced clonic seizures ED50 = 12 nM, i.c.v., 5 min). In lethargic mice, LY367385 significantly reduces the incidence of spontaneous spike and wave discharges on the electroencephalogram, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v.
In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h.
- 更新日期:2024/04/30
- 产品编号:HY-107515A
- 产品名称:LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID LY367385 hydrochloride
- CAS编号:198419-91-9
- 包装:5mg
- 价格:850元
- 更新日期:2024/04/30
- 产品编号:HY-107515A
- 产品名称:LY-367385;(R)-(+)-ALPHA-AMINO-4-CARBOXY-2-METHYLBENZENEACETIC ACID LY367385 hydrochloride
- CAS编号:198419-91-9
- 包装:10mM * 1mLin DMSO
- 价格:940元
- 公司名称:NACALAI
- 联系电话:--
- 电子邮件:info-tech@nacalai.co.jp
- 国家:日本
- 产品数:6048
- 优势度:75