Ro67-4853 Explained

Ro67-4853 is a drug used in scientific research, which acts as a selective positive allosteric modulator for the metabotropic glutamate receptor subtype mGluR₁.^{[1] [2] [3]} It was derived by modification of the simpler compound Ro01-6128, and has itself subsequently been used as a lead compound to develop a range of potent and selective mGluR₁ positive modulators.^{[4] [5]}

See also

C₁₉H₁₉NO₄

Notes and References

1. Knoflach F, Mutel V, Jolidon S, Kew JN, Malherbe P, Vieira E, Wichmann J, Kemp JA . Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site . Proceedings of the National Academy of Sciences of the United States of America . 98 . 23 . 13402–7 . November 2001 . 11606768 . 60883 . 10.1073/pnas.231358298 . 2001PNAS...9813402K . free .
2. Hemstapat K, de Paulis T, Chen Y, Brady AE, Grover VK, Alagille D, Tamagnan GD, Conn PJ . A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators . Molecular Pharmacology . 70 . 2 . 616–626 . August 2006 . 16645124 . 10.1124/mol.105.021857 . 2719603 . https://web.archive.org/web/20190222090830/http://pdfs.semanticscholar.org/3c5d/1685fa51ec475d1ee0b1500af13d3150a182.pdf . dead . 2019-02-22 .
3. Sheffler DJ, Conn PJ . Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells . Neuropharmacology . 55 . 4 . 419–27 . September 2008 . 18625258 . 10.1016/j.neuropharm.2008.06.047 . 2600811.
4. Vieira E, Huwyler J, Jolidon S, Knoflach F, Mutel V, Wichmann J . 9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides as potent, orally available mGlu1 receptor enhancers . Bioorganic & Medicinal Chemistry Letters . 15 . 20 . 4628–31 . October 2005 . 16099654 . 10.1016/j.bmcl.2005.05.135 .
5. Vieira E, Huwyler J, Jolidon S, Knoflach F, Mutel V, Wichmann J . Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers . Bioorganic & Medicinal Chemistry Letters . 19 . 6 . 1666–9 . March 2009 . 19233648 . 10.1016/j.bmcl.2009.01.108 .