1-100 nM.

A-794278 is a potent and selective noncompetitive mGluR1 antagonist, acting on mGluR1 and mGluR5 with IC₅₀ values of 4.1 nM and 147 nM, respectively¹. In vivo it shows analgesic properties, significantly attenuating spontaneous post-operative pain behavior in rats (ED₅₀ = 50 μmol/kg)².

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. Protect from light and moisture.

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

-20°C.

1 nM – 1 µM.

A-850002 inhibits mGluR1 in rat primary cerebellar granule neurons with an IC₅₀ of 27 nM¹ and human mGluR1 expressed in 1321N1 cells with an IC₅₀ of 43 nM².

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.

Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

10 nM – 10 µM.

CFMTI is a selective and potent allosteric antagonist of mGluR1 receptors. It inhibits L-glutamate-induced intracellular Ca²⁺ mobilization in CHO cells expressing human and rat mGluR1a with IC₅₀ values of 2.6 and 2.3 nM, respectively. It is highly selective for mGluR1 over mGluR5 (2000-fold), and does not affect mGluR subtypes and other receptors at 10 µM¹.

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.

Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

10-200 µM.

CPCCOEt is a selective, non-competitive antagonist of mGluR1 receptors, inhibiting hmGluR1b with IC₅₀ of 6.5 µM, whilst having no effect at 100 µM on a range of other receptor subtypes¹. It was shown to inhibit synaptic activation of mGluR1 in Purkinje cell cerebellar slices with IC₅₀ of 37µM².

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. Protect from light and moisture.

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

-20°C.

1 nM – 1 µM.

DM-PPP is a selective and non-competitive antagonist of mGluR1 receptors. It inhibits the receptor in CHO cells with an IC₅₀ of 15.8 nM¹.

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.

Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

10 nM – 10 µM.

FPTQ is a selective allosteric antagonist of the mGluR1 receptors, inhibiting [³H]FTIDC binding with K_i of 14 nM, and inhibiting L-glutamate evoked Ca²⁺ mobilization with IC₅₀ of 3.6 nM in CHO cells expressing human mGluR1¹. It specifically binds mGluR1 in the rat brain².

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.

Up to 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

1-100 nM.

FTIDC is a potent and selective allosteric antagonist of the mGluR1 receptor, shown to inhibit L-glutamate-induced Ca²⁺ mobilization in human and mouse mGluR1a-expressing CHO cells (IC₅₀ values of 5.8 nM and 3.1 nM, respectively), while having a 1000-fold weaker activity against human and rat mGluR5 (IC₅₀ values of 6.2 µM and 9.9 µM, respectively)¹.

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.

Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

1 nM – 1 µM.

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.

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 +4°C.

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

-20°C.

100 nM – 10 µM.

LY 456236 hydrochloride is an antagonist of mGluR1, selective over mGluR5 receptors (IC₅₀ values of 143 nM and >10 μM, respectively)¹.

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

Up to 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Store up to three months at -20°C.

1 nM – 1 µM.

LY456066 is a potent antagonist of mGluR1 receptors. It inhibits human mGluR1 receptors expressed in CHO cells with an IC₅₀ of 28 nM¹.

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.

Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

10 nM – 10 µM.

MK-5435 is a potent and selective allosteric mGluR1 antagonist, inhibiting human and rat mGluR1 with IC₅₀ of 4.3 and 3.6 nM, respectively. It is selective over mGluR5 (IC₅₀ = 1.5 µM), mGluR2 and mGluR8 (IC₅₀ = 10 µM), and has no affinity for the quisqualic binding site (IC₅₀ >10 µM). in vivo, following an oral dose of 1 mg/kg,  plasma and brain concentrations in mice were 0.17 µM and 0.45 nmol/g respectively, at 30 min post-dose¹.

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.

Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.

10 nM – 1 uM.

NPS 2390, a quinoxaline derivative, is a potent and selective non-competitive antagonist of Group I mGluRs, acting on mGluR1 and mGluR5 with IC₅₀ values of to 5.2 and 82 nM, respectively, while having no effect on mGluR2, mGluR8 and other targets at 30 μM^1-3.

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.

Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

-20°C.