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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

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

subject

Has Abstract

pub_date

2000-07-17 00:00:00

pages

1597-600

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(00)00292-4

journal_volume

10

pub_type

杂志文章

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