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LY367385
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LY367385图片
CAS NO:198419-91-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
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。
生物活性

LY367385 is a highly selective and potentmGluR1aantagonist. LY367385 has anIC50of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects[1][2].

IC50& Target[1]

mGluR1a

8.8 μM (IC50)

体外研究
(In Vitro)

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[2].

体内研究
(In Vivo)

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[3].
In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3].

分子量

209.20

性状

Solid

Formula

C10H11NO4

CAS 号

198419-91-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month