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Abstracts
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.
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Year
Volume
Issue
Pages
1155-1158
Physical description
Dates
published
2001
received
2001-09-19
accepted
2001-12-5
Contributors
author
- Department of Chemistry, University of Wrocław, Wrocław, Poland
author
- Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland
author
- Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland
References
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- 8. Calo, G., Guerrini, R., Bigoni, R., Rizzi, A., Monzola, G., Okawa, H., Bianchi, C., Lambert, D., Severo, S., & Regoli, D. (2000) Br. J. Pharmacol. 129, 1183-1193.
Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv48i4p1155kz