The metabotropic glutamate receptor 2 (mGluR2) is a Gi/o-coupled receptor which is expressed on presynaptic nerve terminals and modulates the release of neurotransmitters like glutamate and GABA. Biphenylindanone A (BINA) is a positive allosteric modulator of mGluR2, stimulating the human and rat receptors with EC50 values of 33.2 and 96 nM, respectively. It has no effect on glutamate-induced activation of other mGluR types. BINA can be used on cells, tissues, or animals. Because of its selectivity for mGluR2, robust in vivo activity, and brain penetrance, BINA can be used to elucidate the role of mGluR2 in such diverse processes as psychosis, schizophrenia, and drug addiction.
