Expression of bradykinin B1 receptors in colonic epithelia.
The rat colonic epithelium shows no response to [des-Arg9] bradykinin (DAB) in newly isolated tissues, but does so after 3 h in vitro. The EC50 for DAB is circa 50 nM and the maximal response is 57.8 +/- 5.3 microA cm-2 (n = 68). The whole of the current increase is sensitive to frusemide and is predominantly due to electrogenic chloride secretion. The development of responsiveness is prevented by inhibitors of translation (cycloheximide) and transcription (actinomycin D). Thus the receptor for DAB has the hall marks of a classical B1 kinin receptor. While the classical B2 kinin receptor antagonist HOE140, has no effect on the responses, the classical B1 kinin receptor antagonist, [Leu8]DAB, behaves as an agonist in this system. It is concluded that there may be more than one type of B1 kinin receptor.
Cuthbert
A W
AW
Department of Pharmacology, University of Cambridge, U.K.
Teather
S
S
D000818:Animals; D001920:Bradykinin / Q000031:analogs & derivatives / Q000494:pharmacology; D065168:Bradykinin Receptor Antagonists; D002712:Chlorides / Q000378:metabolism; D003106:Colon / Q000187:drug effects / Q000378:metabolism*; D003513:Cycloheximide / Q000633:toxicity; D003609:Dactinomycin / Q000633:toxicity; D004232:Diuretics / Q000494:pharmacology; D004848:Epithelium / Q000187:drug effects / Q000378:metabolism; D005665:Furosemide / Q000494:pharmacology; D066298:In Vitro Techniques; D007473:Ion Channels / Q000187:drug effects; D017136:Ion Transport / Q000187:drug effects; D007928:Lethal Dose 50; D014176:Protein Biosynthesis / Q000187:drug effects / Q000235:genetics; D011500:Protein Synthesis Inhibitors / Q000633:toxicity; D051381:Rats; D043783:Receptor, Bradykinin B1; D018002:Receptors, Bradykinin / Q000096:biosynthesis* / Q000187:drug effects / Q000378:metabolism; D014158:Transcription, Genetic / Q000187:drug effects / Q000235:genetics
D065168:Bradykinin Receptor Antagonists; D002712:Chlorides; D004232:Diuretics; D007473:Ion Channels; D011500:Protein Synthesis Inhibitors; D043783:Receptor, Bradykinin B1; D018002:Receptors, Bradykinin; C024626:bradykinin, des-Arg(9)-; D003609:Dactinomycin; C051090:bradykinin, Leu(8)-des-Arg(9)-; D005665:Furosemide; C065679:icatibant; D003513:Cycloheximide; D001920:Bradykinin