Chemical Name: [6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](fluorophenyl)methanone
Biological ActivityVU 0409551 is a selective mGlu5 positive allosteric modulator (EC50 = 260 nM). Selective for mGlu5 over other mGluR subtypes, as well as 66 other receptors and ion channels. Selectively potentiates mGlu5 signaling via Gαq. Exhibits wake-promoting, antipsychotic-like and cognition-enhancing effects in animal models. Brain penetrant and orally available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in Schizophrenia.
Ghoshal et al.
ACS Chem.Neurosci., 2017;8:2254
Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents.
Rook et al.
Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia.
Conde-Ceide et al.
ACS Med.Chem.Lett., 2015;6:716
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