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Volumn 19, Issue 23, 2009, Pages 6502-6506

Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

Author keywords

mGluR5; Negative allosteric modulator; Positive allosteric modulator

Indexed keywords

2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; METABOTROPIC RECEPTOR 5;

EID: 71749106942     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.059     Document Type: Article
Times cited : (19)

References (28)
  • 16
    • 65749112588 scopus 로고    scopus 로고
    • Rodriguez, A.L, Williams, R, Zhou, Y, Lindsley, S.R, Le, U, Grier, M.D, Weaver, C.D, Conn, P.J, Lindsley, C.W. Bioorg. Med. Chem. Lett. 2009, 19, 3209; (b) mGluR5 in vitro functional assay. HEK293A cells expressing rat mGluR5 receptor were plated (BD Falcon Poly-d-lysine Cellware) at 50,000 cells/well in assay media (DMEM, 20 mM HEPES, 10% dialyzed FBS, and 1 mM sodium pyruvate, The plates were incubated overnight at 37 °C in 5% CO2. Media was removed and assay buffer (Hanks Balanced Salt Solution, 20 mM HEPES, 2.5 mM Probenecid, pH 7.4) containing 4.0 μM Fluo4-AM dye (Invitrogen) was added. Cells were incubated for 45 min (37 °C, 5% CO2) to allow for dye loading. Dye was removed, 20 μL assay buffer was added and the cell plate was allowed to incubate for 10 min. After incubation in assay buffer, cell plates were loaded into Flexstation II Molecular Devices Corp, Test compound in assay buffer was added 19 seconds into the assay and subsequ
    • max (100 μΜ glutamate), and glutamate concentration response curve. Assays were performed in triplicate on three different days. Concentration response curves were generated using GraphPad Prism 4.0.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.