| Identification | Back Directory | [Name]
(S)-4-(amino(carboxy)methyl)-3-methylbenzoic acid hydrochloride | [CAS]
2829282-00-8 | [Synonyms]
(S)-4-(amino(carboxy)methyl)-3-methylbenzoic acid hydrochloride
Benzeneacetic acid, α-amino-4-carboxy-2-methyl-, hydrochloride (1:1), (αS)- | [Molecular Formula]
C10H12ClNO4 | [MOL File]
2829282-00-8.mol | [Molecular Weight]
245.66 |
| Hazard Information | Back Directory | [Uses]
LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects[1][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].
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In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3]. | [IC 50]
mGluR1a: 8.8 μM (IC50) | [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. DOI:10.1016/s0028-3908(98)00159-2
[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. DOI:10.1016/s0014-2999(99)00014-x |
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