Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.
Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)-phenylpropyl arginine and a N(alpha)-p-biphenylylacetyl moiety shifted the NPY receptor selectivity towards Y5.
Institute of Pharmacy, University of Regensburg, Germany.
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Aiglstorfer
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Hendrich
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Moser
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Bernhardt
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Dove
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Buschauer
D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D004915:Leukemia, Erythroblastic, Acute; D008968:Molecular Conformation; D015394:Molecular Structure; D009478:Neuropeptide Y / Q000493:pharmacokinetics; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013552:Swine; D014407:Tumor Cells, Cultured
C092926:BIBP 3226; D009478:Neuropeptide Y; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor; D001120:Arginine