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
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Arginine / analogs & derivatives*
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Arginine / chemical synthesis
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Arginine / chemistry*
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Arginine / pharmacology
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Drug Design
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Humans
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Kinetics
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Leukemia, Erythroblastic, Acute
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Molecular Conformation
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Molecular Structure
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Neuropeptide Y / pharmacokinetics
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Structure-Activity Relationship
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Swine
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Tumor Cells, Cultured
Substances
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BIBP 3226
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Neuropeptide Y
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Receptors, Neuropeptide Y
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neuropeptide Y-Y1 receptor
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Arginine