Aiglstorfer, Iris and Hendrich, Ingo and Moser, Christiane and Bernhardt, Günther and Dove, Stefan and Buschauer, Armin (2000) Structure-Activity Relationships of Neuropeptide Y Y_1 Receptor Antagonists Related to BIBP 3226,. Bioorganic & Medicinal Chemistry Letters 10 (14), pp. 1597-1600.
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Abstract
Analogues of BIBP 3226, (R)-Nα-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 NG-phenylpropyl arginine and a Nα-p-biphenylylacetyl moiety shifted the NPY receptor selectivity towards Y5.
| Item Type: | Article | ||||
|---|---|---|---|---|---|
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) | ||||
| Identification Number: |
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| Subjects: | 500 Science > 570 Life sciences 600 Technology > 610 Medical sciences Medicine | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Owner: | Prof. Armin Buschauer | ||||
| Deposited On: | 22 Feb 2008 08:51 | ||||
| Last Modified: | 05 Aug 2009 15:42 | ||||
| Item ID: | 3407 |
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