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. Comb...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-07, Vol.10 (14), p.1597-1600
Hauptverfasser:	AIGLSTORFER, I, HENDRICH, I, MOSER, C, BERNHARDT, G, DOVE, S, BUSCHAUER, A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arginine - analogs & derivatives Arginine - chemical synthesis Arginine - chemistry Arginine - pharmacology Biological and medical sciences Drug Design Humans Kinetics Leukemia, Erythroblastic, Acute Medical sciences Molecular Conformation Molecular Structure Neuropeptide Y - pharmacokinetics Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Receptors, Neuropeptide Y - antagonists & inhibitors Structure-Activity Relationship Swine Tumor Cells, Cultured
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00292-4