Synthesis of HYNIC- and DOTA-Conjugates with mi-Opioid Receptor Ligands: Morphiceptin and Endomorphin-2

• Autorzy: Fichna J. , Janecka A. , Kosson P. , Maecke H.
• Języki publikacji: EN

Abstrakty

EN

Opioid peptides recently attracted much attention as low molecular weight compounds, which can target malignant cells expressing opioid receptors on their cell surface. Therefore opioid peptides have a potential to be introduced as radiopharmaceuticals. In this paper, we describe the method of conjugation of two bifunctional chelating agents (BFCAs), hydrazinopyridine-3-carboxylic acid (HYNIC) and 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid (DOTA), to the N-terminal amino group of morphiceptin, endomorphin-2, and two of their analogs modified in position 3. GABA was used as a spacer molecule. mi-Opioid binding affinities of the peptides were compared with the binding affinities of BFCA-GABA-peptide conjugates. It was shown that the introduction of HYNIC to mi-opioid ligands causes only a slight decrease of -opioid receptor affinity, while DOTA-conjugates loose their affinity for mi-receptors completely.

Słowa kluczowe

EN

solid phase peptide synthesis; bifunctional chelating agents; receptor binding assay; opioid receptors

• Wydawca: Polskie Towarzystwo Chemiczne
• Czasopismo: Polish Journal of Chemistry
• Rocznik: 2004
• Tom: Vol. 78 / nr 7
• Strony: 951--959
• Opis fizyczny: Bibliogr. 24 poz., rys.

Twórcy

autor

Fichna J.

• Department of Medicinal Chemistry, Medical University of Łódź, Mazowiecka 6/8, Łódź, Poland

autor

Janecka A.

• Department of Medicinal Chemistry, Medical University of Łódź, Mazowiecka 6/8, Łódź, Poland

autor

Kosson P.

• Medical Research Center, Polish Academy of Sciences, Warsaw, Poland

autor

Maecke H.

• Department of Nuclear Medicine, University Hospital, Basel, Switzerland

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