Novel nociceptin analogues.

• Authors: Hubert Bartosz-Bechowski , Ryszard Międzybrodzki , Stanisław Szymaniec
• Languages of publication: EN

Abstracts

EN

A series of new nociceptin analogues containing cysteine was tested for their nociceptive effects in tail-flick test on mice after icv injection. The cysteines were introduced in order to get irreversibly binding analogues based on the assumption that the cysteines in the ligand can interact with the cysteines from the receptor to form an S-S bridge. In vivo tests revealed that Cys1-nociceptin (1-13)-NH2 (Cys1-NC) is an antagonist, whereas Cys7-NC is an agonist. Gly1,[Phe(p-NO2)]4-NC was less active indicating that the antagonist properties of Cys1-NC are associated with the presence of the sulfhydryl group of cysteine. The analogues D-Cys2 and Cys3 were also almost inactive.

Keywords

EN

orphanin; nociceptin; neuropeptide; antiopioid

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2001
• Volume: 48
• Issue: 4
• Pages: 1155-1158

Dates

published

2001

received

2001-09-19

accepted

2001-12-5

Contributors

author

Hubert Bartosz-Bechowski

• Department of Chemistry, University of Wrocław, Wrocław, Poland

author

Ryszard Międzybrodzki

• Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland

author

Stanisław Szymaniec

• Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland

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