a Department of Pharmacology and Toxicology, University of Rostock, Schillingallee 70, D-18055, Rostock, Germany
b Department of Biophysics and Biochemistry, Friedrich-Schiller-University, Philosophenweg 12, D-07743, Jena, Germany
Abstract:
Independently of their agonistic or antagonistic activity on different isolated tissue preparations, the kinin analogues investigated induce histamine release on rat peritoneal mast cells. The effectivity of most compounds is 10 to 100 times higher than that of bradykinin. Beside the positively charged amino acids, the elongation at the N-terminus with hydrophobic amino acids and the replacement of amino acids in the bradykinin sequence (especially at position 7) with aromatic residues is important for a high histamine-releasing activity.