Novel nociceptin analogues. | Zendy

Hubert Bartosz-Bechowski | Zendy; Ryszard Międzybrodzki | Zendy; S Szymaniec | Zendy

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Novel nociceptin analogues.

Author(s) -

Hubert Bartosz-Bechowski,

Ryszard Międzybrodzki,

S Szymaniec

Publication year - 2001

Publication title -

acta biochimica polonica

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.452

H-Index - 78

eISSN - 1734-154X

pISSN - 0001-527X

DOI - 10.18388/abp.2001_3883

Subject(s) - nociceptin receptor , chemistry , antagonist , cysteine , in vivo , agonist , receptor , nociception , ligand (biochemistry) , nop , stereochemistry , pharmacology , biochemistry , opioid , opioid peptide , biology , microbiology and biotechnology , enzyme

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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