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Author Kalinichev, Mikhail ♦ Rouillier, Mélanie ♦ Girard, Francoise ♦ Royer-Urios, Isabelle ♦ Bournique, Bruno ♦ Finn, Terry ♦ Charvin, Delphine ♦ Campo, Brice ♦ Poul, Emmanuel Le ♦ Mutel, Vincent ♦ Poli, Sonia ♦ Neale, Stuart A. ♦ Salt, Thomas E. ♦ Lütjens, Robert
Source CiteSeerX
Content type Text
File Format PDF
Language English
Subject Domain (in DDC) Computer science, information & general works ♦ Data processing & computer science
Description Metabotropic glutamate receptor 7 (mGlu7) has been suggested to be a promising novel target for treatment of a range of disorders, including anxiety, post-traumatic stress disorder, depression, drug abuse, and schizophrenia. Here we character-ized a potent and selective mGlu7 negative allosteric modulator (NAM) (1)-6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydrobenzo[d]oxazol-4(5H)-one (ADX71743). In vitro, Schild plot analysis and re-versibility tests at the target confirmed the NAM properties of the compound and attenuation of L-(1)-2-amino-4-phosphonobutyric acid–induced synaptic depression confirmed activity at the native receptor. The pharmacokinetic analysis of ADX71743 in mice and rats revealed that it is bioavailable after s.c. admin-istration and is brain penetrant (cerebrospinal fluid concentration/ total plasma concentration ratio at Cmax 5 5.3%). In vivo,
Educational Role Student ♦ Teacher
Age Range above 22 year
Educational Use Research
Education Level UG and PG ♦ Career/Technical Study
Learning Resource Type Article
Publisher Date 2013-01-01
Publisher Institution In vitro and in