Keller, Max, Weiss, Stefan, Hutzler, Christoph, Kuhn, Kilian K., Mollereau, Catherine, Dukorn, Stefanie, Schindler, Lisa, Bernhardt, Günther, König, Burkhard and Buschauer, Armin (2015) N(omega)-carbamoylation of the argininamide moiety: an avenue to insurmountable NPY Y1 receptor antagonists and a radiolabeled selective high affinity molecular tool ([3H]UR-MK299) with extended residence time. Journal of Medicinal Chemistry 58 (22), pp. 8834-8849.
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Abstract
Analogs of the argininamide-type NPY Y1 receptor (Y1R) antagonist BIBP3226, bearing carbamoyl moieties at the guanidine group, revealed subnanomolar Ki values and caused depression of the maximal response to NPY (calcium assay) by up to 90% in a concentration- and time-dependent manner, suggesting insurmountable antagonism. To gain insight into the mechanism of binding of the synthesized ...
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| Item type: | Article | ||||||
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| Date: | 2015 | ||||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König | ||||||
| Projects: | GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands", KE 1857/1-1 | ||||||
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| Keywords: | neuropeptide Y; NPY; Y1 receptor antagonist; radioligand; target residence time; argininamide; carbamoylguanidine; | ||||||
| Dewey Decimal Classification: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy | ||||||
| Status: | Published | ||||||
| Refereed: | Yes, this version has been refereed | ||||||
| Created at the University of Regensburg: | Yes | ||||||
| Item ID: | 31955 |
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