title: Antagonism of the algesic action of bradykinin on the human blister base.
abstract: The effect of bradykinin (BK) and some analogues of BK on the human blister base was studied. BK produced reproducible dose-related increases in pain responses. A characteristic delay, which was not dose-related occurred between application of BK and the resultant response. The rank order of potency of several kinin analogues on the pain response was BK much much greater than sigma-cyclo-(Lys1-Gly6)-BK = sigma-cyclo-kallidin greater than des-Arg9-BK. No increase in pain response was seen with repeated application of the selective B1-receptor agonist des-Arg9-BK to the same blister base at 4h intervals. The B1 receptor antagonist des-Arg9-Leu8-BK was without effect against BK-induced responses. The B2-receptor antagonists, D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Phe-Thi-Arg-TFA and D-Pro-Phe-Arg-heptylamide produced significant antagonism of the bradykinin-induced pain responses at doses which had no effect against 5-hydroxytryptamine or potassium chloride. It is concluded that the kinin receptor mediating pain on the human blister base is of the B2 type.
authors.affiliation: Dep. of Physiol. Sci., Univ. of Manchester, UK.
authors.forename: E T
authors.initials: ET
authors.lastname: Whalley
authors.forename: S
authors.initials: S
authors.lastname: Clegg
authors.forename: J M
authors.initials: JM
authors.lastname: Stewart
authors.forename: R J
authors.initials: RJ
authors.lastname: Vavrek
mesh_terms: D000287:Administration, Topical; D001768:Blister / Q000503:physiopathology*; D001920:Bradykinin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010146:Pain / Q000503:physiopathology*; D010147:Pain Measurement
chemical_list: D001920:Bradykinin