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1 Polish Journal of Chemistry

1 2002

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New Galanin Analogues with Contractile Activities on Rat Gastric Smooth MusclesR

Ruczyński J., Sawuła A., Konstański Z., Korolkiewicz R., Rekowski P.

Polish Journal of Chemistry

2002

Vol. 76 / nr 1

57-66

We synthesized new 15-amino-acid-residue analogues of porcine galaninmodified in positions 2, 6, 8 or 14 and studied their activity on isolated rat gastric smooth muscles. Thus, we intended to characterize the molecular domains of GAL responsible for binding to its receptors and biological activity in the gastric fundus. All peptides were synthesized by the solid phase peptide synthesis with the use of Fmoc strategy. All galanin analogues contracted rat gastric fundus strips in a concentration-dependent manner with significantly increased or decreased activities as compared to GAL(1-15)NH2. As expected, the modifications introduced into the amino acid sequence of galanin caused changes in the interaction of GAL(1-15)NH2 with its receptors. Thus, residues: Trp2, Ser6, Gly8 and His14 in the amino acid sequence of GAL(1-15)NH2 play an important roles in the high-affinity binding of GAL to its receptors and biological activity in rat gastric smooth muscle cells.