JNJ 16259685

Non Antibodies

mGluR1

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

325, 41

A Potent and Selective Antagonist of mGluR1

Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

JNJ 16259685 is a potent and selective non-competitive antagonist of mGluR1 receptors, inhibiting human mGluR1 and mGluR5 mediated glutamate-induced Ca2+ mobilization with IC50 values of 1.21 nM and 28.3 µM, respectively, whilst having no effect on a range of other receptor subtypes at over 10 µM1.It is systemically active, occupying central mGluR1 receptors in the rat cerebellum and thalamus (ED50 = 40 and 14 µg/kg, respectively) when administered subcutaneously1. JNJ 16259685 inhibits synaptic activation of mGluR1 in Purkinje cells in cerebellar slices with IC50 of 19 nM2.

Yes

JNJ 16259685 is a potent, specific, and non-competitive antagonist of mGluR1 displaying an IC50 of 19 nM1. The compound shows a much lower potency towards mGluR5 receptor1, 2.Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8.mGluR1 plays an important role in the central sensitization of pain and in various physiological functions including regulating ion channels, synaptic transmission, and synaptic plasticity2.