ADX-47273 explained

ADX-47273 is a research pharmaceutical developed by Addex Therapeutics which acts as a positive allosteric modulator (PAM) selective for the metabotropic glutamate receptor subtype mGluR₅.^{[1] [2]} It has nootropic and antipsychotic effects in animal studies,^[3] and has been used as a lead compound to develop improved derivatives.^[4]

See also

• Dipraglurant
• Raseglurant

Notes and References

1. de Paulis T, Hemstapat K, Chen Y, Zhang Y, Saleh S, Alagille D, Baldwin RM, Tamagnan GD, Conn PJ . Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes . Journal of Medicinal Chemistry . 49 . 11 . 3332–44 . June 2006 . 16722652 . 10.1021/jm051252j .
2. Stauffer. Shaun R.. Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5). ACS Chemical Neuroscience. 17 August 2011. 2. 8. 450–470. 10.1021/cn2000519. 3369763. 22860171.
3. Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, Marquis KL . ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities . The Journal of Pharmacology and Experimental Therapeutics . 327 . 3 . 827–39 . December 2008. 18753411 . 10.1124/jpet.108.136580 . 19362501 .
4. Engers DW, Rodriguez AL, Williams R, Hammond AS, Venable D, Oluwatola O, Sulikowski GA, Conn PJ, Lindsley CW . Synthesis, SAR and unanticipated pharmacological profiles of analogues of the mGluR5 ago-potentiator ADX-47273 . ChemMedChem . 4 . 4 . 505–11 . April 2009 . 19197923 . 10.1002/cmdc.200800357 . 2865690.