198419-91-9

198419-91-9 structure

Name: LY 367385
Chemical Name: 4-[(S)-amino(carboxy)methyl]-3-methylbenzoic acid
CAS Number: 198419-91-9
Molecular Formula: C₁₀H₁₁NO₄
Molecular Weight: 209.19900
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2017-01-18 12:53:07
Modify Date: 2024-01-08 15:49:30
LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects[1][2].

Name	4-[(S)-amino(carboxy)methyl]-3-methylbenzoic acid
Synonyms	Tocris-1237 (S)-(+)-a-amino-4-carboxy-2-methylbenzeneacetic acid

Description	LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with > 100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	mGluR1a:8.8 μM (IC50)
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].
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].
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.

Molecular Formula	C₁₀H₁₁NO₄
Molecular Weight	209.19900
Exact Mass	209.06900
PSA	100.62000
LogP	1.47790

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