A non-competitive antagonist of mGluR5 (Ki = 3.5 nM in a radioligand binding assay using L(tk-) cell membranes expressing human receptors); binds at an allosteric binding site; selective for mGluR5 receptors over a panel of CNS G protein-coupled receptors

ABP 688 – 5 mg

Brand:
Cayman
CAS:
924298-51-1
Storage:
-20
UN-No:
Non-Hazardous - /

ABP 688 is a non-competitive antagonist of metabotropic glutamate receptor 5 (mGluR5; Ki = 3.5 nM in a radioligand binding assay using L(tk-) cell membranes expressing human receptors).{53878} It is selective for mGluR5 receptors over a panel of CNS G protein-coupled receptors, ion channels, and transporters at 10 μM. ABP 688 inhibits quisqualate-induced phosphoinositol accumulation in and glutamate-induced calcium release from L(tk-) cells expressing human mGluR5 (IC50s = 2.4 and 2.3 nM, respectively). Radiolabeled forms of ABP 688 have been used as PET tracers for in vivo imaging of mGluR5 receptors in rodents.{53878,53879}  

 

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SKU: 30929 - 5 mg Category:

Description

A non-competitive antagonist of mGluR5 (Ki = 3.5 nM in a radioligand binding assay using L(tk-) cell membranes expressing human receptors); binds at an allosteric binding site; selective for mGluR5 receptors over a panel of CNS G protein-coupled receptors, ion channels, and transporters at 10 μM; inhibits quisqualate-induced phosphoinositol accumulation in and glutamate-induced calcium release from L(tk-) cells expressing human mGluR5 (IC50s = 2.4 and 2.3 nM, respectively); radiolabeled forms have been used as PET tracers for in vivo imaging of mGluR5 receptors in rodents

Formal name: 3-[2-(6-methyl-2-pyridinyl)ethynyl]-2-cyclohexen-1-one, O-methyloxime

Synonyms: 

Molecular weight: 240.3

CAS: 924298-51-1

Purity: ≥98%

Formulation: A solid

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