LY 367385 has been shown to act as a selective mGluR-1a receptor antagonist, with an IC₅₀ value of 8.8 μM for blockade of quisqualate-induced phosphoinositide hydrolysis vs > 100 μM for mGluR-5a, while showing negligible action on group II and III receptors.

A selective mGluR-1a antagonist

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

Solid

(S)-(+)-α-Amino-4-carboxy-2-methylbenzeneacetic acid

white to off-white powder

mGluR-1α: IC₅₀ = 8.8 µM; mGluR-5: IC₅₀ = >100 µM

pK_a: 1.72 (Predicted), pK_b: 10.18 (Predicted)

Soluble in 1.1eq. NaOH (100 nM), water (5 mM) with gentle warming, phosphate buffered saline (5 mM) with gentle warming, and DMSO (10 mM) with gentle warming.

Compared with the activity of LY367385, the novel compound LY367366 antagonizes both mGlu1a and -5 receptors at low micromolar concentrations, but also recruits other subtypes at higher concentrations. LY367366 possessing neuroprotective ability was in general less efficacious than LY357385. This fact suggested that inhibitors of mGlu1 receptors is a potential agent to confer significant neuroprotection.

LY 367385 and AIDA have been administered intracerebroventricularly (i.c.v.) to lethargic mice and DBAr2 mice, and focally into the inferior colliculus of GEPR. In lethargic mice both compounds significantly decrease the incidence of spontaneous spike and wave discharges on the electroencephalogram, after the administration of LY 367385, 250 nmol, i.c.v. LY 367385, 50 nmol, inhibites spontaneous spike and wave discharges from 30 to 60 min. In DBAr2 mice both compounds produce a rapid, transient suppression of sound-induced clonic seizures. In genetically epilepsy prone rats, both compounds decreases sound-induced clonic seizures. The results suggestes that antagonists of mGlu1 receptors are potential anticonvulsant tools and that activation of mGlu1 receptors likely contributes to a variety of epilepticsyndromes.