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Neuropeptide Y Y 1  receptors (Y 1 R) have been found to be overexpressed in a number of different tumours, such as breast, ovarian or renal cell cancer. In mammary carcinoma the high Y 1 R density together with its high incidence of 85% in primary human breast cancers and 100% in breast cancer derived lymph node metastases attracted special attention. Therefore, the aim of this study was the development of radioligands for Y 1 R imaging by positron emission tomography (PET) with a special emphasis on imaging agents with reduced lipophilicity to provide a PET ligand with improved biodistribution in comparison with previously published tracers targeting the Y 1 R. Three new radioligands based on BIBP3226, bearing an  18 F-fluoroethoxy linker ( 12 ), an  18 F-PEG-linker ( 13 ) or an  18 F-fluoroglycosyl moiety ( 11 ) were radiosynthesised in high radioactivity yields. The new radioligands displayed Y 1 R affinities of 2.8 nM ( 12 ), 29 nM ( 13 ) and 208 nM ( 11 ) and were characterised  in vitro  regarding binding to human breast cancer MCF-7-Y1 cells and slices of tumour xenografts.  In vivo , small animal PET studies were conducted in nude mice bearing MCF-7-Y1 tumours. The binding to tumours, solid tumour slices and tumour cells correlated well with the Y 1 R affinities. Although  12  and  13  showed displaceable and specific binding to Y 1 R  in vitro  and  in vivo , the radioligands still need to be optimised to achieve higher tumour-to-background ratios for Y 1 R imaging by PET. Yet the present study is another step towards an optimized PET radioligand for imaging of Y 1 R  in vivo .

18F-labelled triazolyl-linked argininamides targeting the neuropeptide Y Y1R for PET imaging of mammary carcinoma