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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

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
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
Identification Number:
ValueType
10.1021/acs.jmedchem.5b00925DOI
26466164PubMed ID
Related URLs:
URLURL Type
http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00925Publisher
http://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.5b00925Supplementary Material
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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