Parallel synthesis and pharmacological screening of nonpeptide ligands of the neuropeptide Y receptor subtype Y-5

Several series of low-molecular-mass ligands of the neuropeptide receptor subtype Y5 were prepared using a mixed strategy of synthesis on solid phase and in solution. Collections of single compounds were obtained by an automated parallel procedure which allowed quick variation and investigation of t...

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Bibliographic Details
Published inThe journal of peptide research Vol. 57; no. 5; pp. 419 - 427
Main Authors Henlin, JM, Boutin, JA, Duchene-Roger, F, Nicolas, JP, Desmet-Beaufort, C, Levens, N, Fauchere, JL
Format Journal Article
LanguageEnglish
Published COPENHAGEN Wiley 01.05.2001
Subjects
Biochemical Research Methods
Biochemistry & Molecular Biology
Life Sciences & Biomedicine
Science & Technology
G protein-coupled receptors
FOOD-INTAKE
neuropeptide Y
neuropeptide Y5 antagonist
nonpeptide antagonists
solid-phase synthesis
parallel synthesis
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Summary:Several series of low-molecular-mass ligands of the neuropeptide receptor subtype Y5 were prepared using a mixed strategy of synthesis on solid phase and in solution. Collections of single compounds were obtained by an automated parallel procedure which allowed quick variation and investigation of the central spacer moiety, as well as of the aromatic substituents on each side. The strategy of parallel synthesis and screening of partially purified analogs helped to select rapidly potent and selective leads which displayed comparable antagonistic potency against neuropeptide Y activity on the Y5 receptor and better receptor selectivity than the original reference compounds.
ISSN:1397-002X
DOI:10.1034/j.1399-3011.2001.00766.x