Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 6, 2008, Pages 2203-2205

  Witherington, Jason ^a   Abberley, Lee ^a   Briggs, Michael A ^a   Collis, Katharine ^a   Dean, David K ^a   Gaiba, Alessandra ^a   King, N Paul ^a   Kraus, Helmut ^a   Shuker, Nicola ^a   Steadman, Jon G A ^a   Takle, Andrew K ^a   Sanger, Gareth ^b   Wadsworth, Graham ^b   Butler, Sharon ^b   McKay, Fiona ^b   Muir, Alison ^b   Winborn, Kim ^b   Heightman, Tom D ^b  

^a Department of Medicinal Chemistry   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Agonist; Ghrelin; Growth hormone

Indexed keywords

GROWTH HORMONE DERIVATIVE; GROWTH HORMONE SECRETAGOGUE RECEPTOR; SB 791016; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; HIGH THROUGHPUT SCREENING; HYDROGEN BOND; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; FLUORESCENCE; INDOLES; MALE; MOLECULAR STRUCTURE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTORS, GHRELIN; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 40749117607     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.12.021     Document Type: Article

References (9)

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8. 2 + 0.714 mg/ml probenicid (predissolved in 1 M NaOH) + 0.5 mM brilliant black + 2.5 μM Fluo 4 dye) and incubated at 37.5 °C for 1 h. Ten microliters from compound plates is then added immediately to cell plates using a FLIPR 3 calcium imaging instrument. Fluorescence measurements are then taken. Intrinsic activity is expressed relative to human ghrelin.
9. -1) po. Total food consumption was measured up to 2 h post-dose.