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Syntheses of Fmoc-alfa-aminoalkyltetrazoles and Tetrazole Analogue of Leu-enkephalin

Manturewicz M., Kosson P., Grzonka Z.

Polish Journal of Chemistry

2007

Vol. 81, nr 7

1327-1334

Five Fmoc-alfa-aminoalkyltetrazoleswere synthesized starting from Fmoc-alfa-amino acids. Fmoc-LeuT was applied in synthesis of tetrazole analogue of Leu-enkephalin by solid phase peptide synthesis (SPPS), aswell as in solution. Radioreceptor assays showed high affinity of [LeuT5]-enkephalin for opiate receptors.

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

Fichna J., Janecka A., Kosson P., Maecke H.

Polish Journal of Chemistry

2004

Vol. 78 / nr 7

951-959

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.