Synthesis and biological properties of new chimeric galanin analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2

• Autorzy: Ruczynski J. , Konstanski Z. , Cybal M. , Petrusewicz J. , Wojcikowski C. , Rekowski P. , Kaminska B.
• Języki publikacji: EN

Abstrakty

EN

Several chimeric peptides consisting of the N-terminal fragment of galanin (GAL) and C-terminal fragments of other bioactive peptides (e.g. substance P, bradykinin, neuropeptide Y, mastoparan) have been synthesized and reported as high-affinity galanin receptor antagonists. Recently we have synthesized a new chimeric peptide, GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2, consisting of the N-terminal fragment of GAL and the C-terminal fragment of endothelin-1 (ET-1) analogue. This chimera was previously shown to be a moderate-affinity ligand to hypothalamic galanin receptors with a KD value of 205 nM. However, its biological action has been unknown so far. In our studies we characterized the biological properties of this new chimeric analogue, investigating its action on rat isolated gastric smooth muscles and influence on insulin secretion from rat isolated islets of Langerhans. Data acquired in the course of our studies suggest that analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2 does not seem to be a potent galanin receptor antagonist in the gastrointestinal tract.

Słowa kluczowe

EN

gastric smooth muscle; galanin; synthesis; biological property; smooth muscle; chimeric analogue; insulin secretion

• Wydawca: -
• Czasopismo: Journal of Physiology and Pharmacology
• Rocznik: 2005
• Tom: 56
• Numer: 2
• Opis fizyczny: p.273-285,fig.,ref.

Twórcy

autor

Ruczynski J.

• University of Gdansk, Sobieskiego 18, 80-952 Gdansk, Poland

autor

Konstanski Z.

autor

Cybal M.

autor

Petrusewicz J.

autor

Wojcikowski C.

autor

Rekowski P.

autor

Kaminska B.