Structure-activity relationships of the oxindole growth hormone secretagogues

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 7, 2005, Pages 1789-1792

  Tokunaga, Teruhisa ^a   Hume, W Ewan ^a   Nagamine, Jun ^a   Kawamura, Tetsuya ^a   Taiji, Mutsuo ^a   Nagata, Ryu ^a  

^a DAINIPPON SUMITOMO PHARMA CO LTD   (Japan)

Author keywords

Ghrelin; Growth hormone secretagogue; SM 130686

Indexed keywords

CAPROMORELIN; CARBON; GHRELIN; GROWTH HORMONE SECRETAGOGUE; IBUTAMOREN; OXINDOLE; SM 130686; TABIMORELIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BINDING; DRUG SYNTHESIS; IC 50; LOW DRUG DOSE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

EID: 15044360777     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.02.042     Document Type: Article

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15. 125I-ghrelin (30,000 dpm/tube), with or without different concentrations (0.01-10,000 nM) of test compounds and the binding buffer up to a total volume of 100 μL. Nonspecific binding was obtained by adding 500 nM of cold ghrelin. The membranes were incubated at 25°C for 30 min, and the bound radioligand was separated from free radioligand by washing three times with 3 mL of the binding buffer through a 0.5% polyethylenimine-presoaked GF/B filter (Whatman). The radioactivity on the filters was counted in 1470 Wallac Wizard Gamma Counter (PerkinElmer, MA)
16. All the other compounds in Table 1 displayed partial agonist activity
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