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

100%

Ruczynski J., Konstanski Z., Cybal M., Petrusewicz J., Wojcikowski C., Rekowski P., Kaminska B.

Journal of Physiology and Pharmacology

2005

tom 56

nr 2

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.

Effects of tyrosine kinase inhibitors on voltage-dependent BA2+ currents in the guinea-pig gastric antrum

100%

Zhu H. L., Ito Y., Teramoto N.

Journal of Physiology and Pharmacology

2006

tom 57

nr 3

We have investigated whether tyrosine kinases modify the activity of voltage-dependent Ba2+ currents (IBa) recorded from guinea-pig gastric myocytes by use of patch-clamp techniques. All experiments were carried on single smooth muscle cells, dispersed from the circular layer of the guinea-pig gastric antrum. Genistein (10 µM), a specific tyrosine kinase inhibitor, reduced the peak amplitude of IBa in a voltage- and concentration-dependent manner. Daidzein (30 µM), an inactive analog of genistein, also inhibited IBa in a concentration-dependent manner. Similarly, other types of tyrosine kinase inhibitors (lavendustin A and tyrphostin 23) suppressed the peak amplitude of IBa in a concentration-dependent manner. These results indicate that tyrosine kinases may be essential to regulate Ca2+ mobilization through voltage-dependent Ca2+ channels in gastric myocytes.

Ograniczanie wyników

2 Journal of Physiology and Pharmacology

1 Cybal M.

1 Ito Y.

1 Kaminska B.

1 Konstanski Z.

1 Petrusewicz J.

1 Rekowski P.

1 Ruczynski J.

1 Teramoto N.

1 Wojcikowski C.

1 Zhu H. L.

1 2006

1 2005

Wyniki wyszukiwania

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

Effects of tyrosine kinase inhibitors on voltage-dependent BA2+ currents in the guinea-pig gastric antrum