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Volumn 19, Issue 15, 2009, Pages 4264-4267

Discovery and optimization of a novel Neuromedin B receptor antagonist

Author keywords

Antagonist; Ary hexahydro dibenzodiazepin 1 one; NMBR; Parallel synthesis

Indexed keywords

ARY HEXAHYDRO DIBENZODIAZEPIN 1 ONE; BENZODIAZEPINE DERIVATIVE; NEUROMEDIN B; NEUROMEDIN B RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

EID: 67649965567     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.05.124     Document Type: Article
Times cited : (19)

References (29)
  • 17
    • 67649939751 scopus 로고    scopus 로고
    • note
    • 6 transfected cells in Dulbeco's Modified Eagle Media (Mediatech, Inc.) in 100 μL in 96 well plates. Bound ligand was separated from unbound ligand by filtration using a Filtermate (Packard) and total counts bound determined on a TopCount NTX reader (Packard). Standard error of the assay day-to-day was <30%; well-to-well variability was <10%.
  • 25
    • 67649907158 scopus 로고    scopus 로고
    • note
    • 1H NMR.
  • 26
    • 67649931217 scopus 로고    scopus 로고
    • note
    • 3OH).
  • 27
    • 67649924185 scopus 로고    scopus 로고
    • note
    • 2O requires 426.5.
  • 28
    • 67649907157 scopus 로고    scopus 로고
    • note
    • Protocol for cytotoxicity assay: HeLa cells were seeded at 5 k/well in a 96 well plate (6 plates-for triplicate 0 and 72 h readings). A threefold dilution series of each compound was generated, starting at 10 mM. The solution was diluted eight times to prepare 9 concentrations ranging from 10 mM to 150 nM. Compound was added to cells (1-100 μL total volume), and the final concentration of compound was 100 μM to 15 nM. Zero and 72 h time points were recorded as follows: (a) 10 μL Alamar Blue reagent was added to the wells, and the samples were incubated at 37 °C for 3 h; (b) fluorescence intensity was then recorded on an LJL Analyst. The relative growth was compared to a DMSO control well for each compound.
  • 29
    • 67649942804 scopus 로고    scopus 로고
    • note
    • 3H]Inositol (82.0 Ci/mmol, Amersham Pharmacia Biotech) overnight at 37 °C. Test compounds were then added in inositol-free DMEM containing 0.3% BSA (Sigma) and 10 mM LiCl (Sigma) for 60 min at 37 °C. The cells were lysed with 20 mM formic acid for 2 h at 4 °C and added to RNA-binding Ysi scintillation proximity assay beads (Amersham Pharmacia Biotech) for 30 min. Plates were stored overnight at room temperature in the dark and read the next day on a TopCount NTX.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.