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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

Pack Size	Availability	Price/USD	Quantity
10 mg	4-5 weeks	$ 595.00
50 mg	4-5 weeks	$ 2,480.00

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Biological Description

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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 effectively suppresses sound-induced clonic seizures in DBA/2 mice with a rapid onset, achieving a median effective dose (ED50) of 12 nM when administered intracerebroventricularly (i.c.v.) 5 minutes prior. It also significantly reduces the frequency of spontaneous electroencephalogram (EEG) spike and wave discharges in lethargic (lh/lh) mice, maintaining this effect from 30 to over 150 minutes post-administration at a concentration of 250 nM, i.c.v. Furthermore, LY367385 has been utilized in both DBA/2 and lethargic mice, in addition to direct application into the inferior colliculus of genetically epilepsy-prone rats (GEPR), demonstrating its efficacy in reducing seizures across different models. Specifically, in GEPR, a bilateral dose of 160 nM substantially mitigates clonic seizures within 2-4 hours.

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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 Metabolism FXR LY-367385 LY 367385 inhibitor inhibit

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