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LY367385

Catalog No. T15818 CAS 198419-91-9

LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.

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LY367385, CAS 198419-91-9

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Purity: 98%

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Storage & Solubility Information

Description	LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.
Targets&IC50	mGluR1a:8.8 μM
In vitro	LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se and it also displays effective neuroprotective effects, causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse decreases neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 fully antagonized the amplification of NMDA toxicity by DHPG under experimental conditions at higher concentrations of the antagonist[2].
In vivo	LY367385 produces a rapid, transient suppression of sound-induced clonic seizures (ED50 = 12 nM, i.c.v., 5 min), in DBA/2 mice. LY367385 significantly decreases the incidence of spontaneous spike and wave discharges on the electroencephalogram in lethargic mice, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v. 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). LY367385 reduces sound-induced clonic seizures, in genetically epilepsy prone rats. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3].

Molecular Weight	209.2
Formula	C10H11NO4
CAS No.	198419-91-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

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( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Keywords

LY367385 198419-91-9 代谢 FXR LY-367385 Inhibitor inhibitor inhibit

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