Histamine release from rat peritoneal mast cells by kinin antagonists.
作者： Philippe Devillier , Mario Renoux , Guy Drapeau , Domenico Regoli
DOI: 10.1016/0014-2999(88)90051-9
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摘要: Kinins are known to be potent releasers of histamine. In the present study, B2 antagonist analogues bradykinin (BK) and kallidin (KD): [( Thi6,9,D-Phe8]KD, [Thi5,8,D-Phe7]BK) were also found histamine from rat mast cells not exert any antagonistic effect. Similarly, two B1 receptor antagonists, des-Arg10-[Leu9]KD des-Arg9-[Leu8]BK, shown promote release acted only as agonists. The order potency these was following: [Thi6,9,D-Phe8]KD greater than [Thi5,8,D-Phe7]BK des-Arg10- [Leu9]KD des-Arg9-[Leu8]BK. high activity some compounds suggests that (1) kinins for increases in parallel with number positively charged amino acids (Lys, Arg) but also, because others factors such peptide conformation, binding affinity or accessibility, (2) by is either a non-specific effect mediated receptors or, if involved, sites may different other kinin (i.e. B2).
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