Vietinghoff G, Paegelow I, Reissmann S
Department of Pharmacology and Toxicology, University of Rostock, Germany.
Peptides. 1996;17(8):1467-70. doi: 10.1016/s0196-9781(96)00214-8.
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.
在所研究的激肽类似物中，无论它们对不同离体组织制剂具有激动或拮抗活性，均可诱导大鼠腹膜肥大细胞释放组胺。大多数化合物的效力比缓激肽高10至100倍。除了带正电荷的氨基酸外，N端用疏水氨基酸延长以及在缓激肽序列中（特别是第7位）用芳香族残基取代氨基酸对于高组胺释放活性很重要。
