LY367385 hydrochloride
目录号 : GC61816LY367385 hydrochloride 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 hydrochloride 具有神经保护,抗惊厥和抗癫痫作用。
Cas No.:2829282-00-8
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
- Datasheet
LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 µM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 µM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects[1][2].
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].
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].
References:
[1]. Clark et al. (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. November 1997, 7 (21): 2777-2780.
[2]. Bruno V, et al. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 receptors. Neuropharmacology. 1999 Feb;38(2):199-207.
[3]. Chapman AG, et al. Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24.
Cas No. | 2829282-00-8 | SDF | |
Canonical SMILES | OC([C@H](C1=C(C=C(C(O)=O)C=C1)C)N)=O.[H]Cl | ||
分子式 | C10H12ClNO4 | 分子量 | 245.66 |
溶解度 | DMSO : 125 mg/mL (508.83 mM)|Water : 12.5 mg/mL (50.88 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.0707 mL | 20.3533 mL | 40.7067 mL |
5 mM | 0.8141 mL | 4.0707 mL | 8.1413 mL |
10 mM | 0.4071 mL | 2.0353 mL | 4.0707 mL |
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