Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226

I Aiglstorfer; I Hendrich; C Moser; G Bernhardt; S Dove; A Buschauer

doi:10.1016/s0960-894x(00)00292-4

Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1597-600. doi: 10.1016/s0960-894x(00)00292-4.

Authors

I Aiglstorfer¹, I Hendrich, C Moser, G Bernhardt, S Dove, A Buschauer

Affiliation

¹ Institute of Pharmacy, University of Regensburg, Germany.

PMID: 10915060
DOI: 10.1016/s0960-894x(00)00292-4

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Arginine / analogs & derivatives*
Arginine / chemical synthesis
Arginine / chemistry*
Arginine / pharmacology
Drug Design
Humans
Kinetics
Leukemia, Erythroblastic, Acute
Molecular Conformation
Molecular Structure
Neuropeptide Y / pharmacokinetics
Receptors, Neuropeptide Y / antagonists & inhibitors*
Structure-Activity Relationship
Swine
Tumor Cells, Cultured

Substances

BIBP 3226
Neuropeptide Y
Receptors, Neuropeptide Y
neuropeptide Y-Y1 receptor
Arginine