作者: C D Strader , R W Ransom , T MacNeil , A W Derrick , J G Menke
DOI: 10.1016/S0021-9258(17)31844-6
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摘要: A cDNA clone encoding a human B1 bradykinin receptor was isolated from embryonic lung fibroblast library by expression cloning. The photoprotein aequorin utilized as an indicator of the ability agonist [des-Arg10]kallidin to mediate Ca2+ mobilization in Xenopus laevis oocytes injected with RNA. 1307-nucleotide insert which contains open reading frame 353-amino acid protein characteristics G-protein-coupled receptor. amino sequence is 36% identical B2 cloned expressed mammalian cells exhibits high affinity binding for 3H-labeled and low bradykinin. antagonist [des-Arg10,Leu9]kallidin effectively displaces receptor, whereas Hoe-140 (D-Arg0-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin, where Thi L-[3-(2-thienyl)alanyl], Tic D-(1,2,3,4-tetrahydroisoquinolin-3-yl-carbonyl), Oic L-[(3aS, 7aS)-octahydroindol-2-yl-carbonyl]) does not. Therefore, has pharmacological subtype. availability both receptors should allow elucidation relative contributions these two subtypes acute chronic inflammatory processes.