Overview
- Varty, G.B. et al. (2005) Psychopharmacology (Berl). 179, 207.
Alomone Labs LY 456236 hydrochloride inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.Dose-response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by LY 456236 hydrochloride (#L-235). IC50 was determined at 1.56 µM. hmGluR1-expressing U2OS cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of LY 456236 hydrochloride, and stimulated by 15 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
- Varty, G.B. et al. (2005) Psychopharmacology (Berl). 179, 207.
- Shannon, H.E. et al. (2005) Neuropharmacology 49, 188.
- Satow, A. et al. (2008) J. Pharmacol. Exp. Ther. 326, 577.
- Eom, H.S. et al. (2016) PLoS One 11, e0147538.
LY 456236 hydrochloride is a potent and selective antagonist of mGluR1 receptors with an IC50 value of 140 + 5 nM2.
Several studies in rat and mouse models have shown that systemic administration of LY 456236 reduces hyperalgesia induced by formalin and mechanical allodynia following spinal nerve ligation. In the anxiety models tested, LY 456236 produces anxiolytic-like effects1. Another study shows that LY456236 may have clinical value in the treatment of epilepsy and other seizure disorders2.
Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) and play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found in somatodendritic domains and postsynaptically regulate neuronal excitability and synaptic transmission through several intracellular second messenger systems3,4.
LY 456236 hydrochloride (#L-235) is a highly pure, synthetic, and biologically active compound.
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