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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
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