- Synthesis and Binding Affinity of Fluorine Containing NG-acyl and -sulfonyl BIBP3226 Derivatives: Ligands for the NPY Y1 Receptor
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The neuropeptide Y (NPY) receptors are abundant in a range of tumours hence are a molecular target for tumour imaging and therapy, particularly by the use of radiolabelled molecules. NG-Substituted derivatives of the NPY receptor antagonist, BI
- Lengkeek, Nigel A.,Roberts, Maxine P.,Zhang, Lei,Lee, I-Chieh J.,Fookes, Christopher J. R.,Dikic, Branko,Herzog, Herbert,Katsifis, Andrew,Greguric, Ivan
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- Guanidine-acylguanidine bioisosteric approach in the design of radioligands: Synthesis of a tritium-labeled NG-propionylargininamide ([3H]-UR-MK114) as a highly potent and selective neuropeptide Y Y1 receptor antagonist
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Synthesis and characterization of (R)-Nα-(2,2- diphenylacetyl)-N-(4-hydroxybenzyl)-Nω-([2,3- 3H]-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 experiments: 1.1 nM, SK-N-MC cells) and selectivity for Y1R over Y2, Y 4, and Y5 receptors. The title compound is a useful pharmacological tool for the determination of Y1R ligand affinities, quantification of Y1R binding sites, and autoradiography.
- Keller, Max,Pop, Nathalie,Hutzler, Christoph,Beck-Sickinger, Annette G.,Bernhardt, Günther,Buschauer, Armin
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supporting information; experimental part
p. 8168 - 8172
(2009/12/07)
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