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Guanidine - acylguanidine bioisosteric approach in the design of radioligands: Synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist

Keller, Max and Pop, Nathalie and Hutzler, Christoph and Beck-Sickinger, Annette G. and Bernhardt, Günther and Buschauer, Armin (2008) Guanidine - acylguanidine bioisosteric approach in the design of radioligands: Synthesis of a tritium-labeled N(G)-propionylargininamide ([3H]UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist. Journal of Medicinal Chemistry 51 (24), pp. 8168-8172.

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Other URL: http://pubs.acs.org/doi/full/10.1021/jm801018u, http://pubs.acs.org/doi/pdf/10.1021/jm801018u, http://www.ncbi.nlm.nih.gov/pubmed/19053784?ordinalpos=1&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_DefaultReportPanel.Pubmed_RVDocSum


Abstract

Synthesis and characterization of (R)-N(alpha)-(2,2-diphenylacetyl)-N-(4-hydroxybenzyl)-N(omega)-([2,3-3H2]-propanoyl)argininamide ([3H]-UR-MK114), an easily accessible tritium-labeled NPY Y1 receptor (Y1R) antagonist (KB: 0.8 nM, calcium assay, HEL cells) derived from the (R)-argininamide BIBP 3226, is reported. The radioligand binds with high affinity (KD, saturation: 1.2 nM, kinetic ...

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Item Type:Article
Date:21 November 2008
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1021/jm801018uDOI
19053784PubMed ID
Related URLs:
URLURL Type
http://pubs.acs.org/doi/suppl/10.1021/jm801018u/suppl_file/jm801018u_si_001.pdfSupplementary Material
Keywords:Neuropeptide Y; NPY; radiolabeled Y1 receptor antagonist; BIBP 3226; MCF-7 breast cancer cells; SK-N-MC cells; autoradiography
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
500 Science > 500 Natural sciences & mathematics
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Armin Buschauer
Deposited On:29 Oct 2008 21:06
Last Modified:05 Aug 2009 13:48
Item ID:4678
Owner Only: item control page
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