title: Kinin receptors in experimental inflammation.
abstract: The contractile response of the rat isolated urinary bladder to kinins is meated by receptors of the B1 and of the B2 types, as this preparation responds to des-Arg9-bradykinin (des-Arg9-BK), a fairly selective stimulant of receptor B1 and to [Tyr(Me)8]-BK, a potent agonist on receptor B2. Des-Arg10-[Leu9]-kallidin, a specific and competitive antagonist of the action of kinins on receptor B1, has been found to block the effect of des-Arg9-BK in concentrations similar to those required in the rabbit aorta; therefore, the B1 receptor of the rat urinary bladder is analogous to that of the rabbit vascular tissue. The response of the rat urinary bladder to des-Arg9-BK increases progressively from near null level during the incubation in vitro and can be abolished by cycloheximide; this suggests that receptor B1 of the rat urinary bladder is formed de novo. The inflammation of the bladder induced by intravesical injection of the detergent Triton X-100 enhances the initial response to des-Arg9-BK without modifying the response to other agents. The B1 receptor is formed in vivo in the rat urinary bladder submitted to the Triton X-100 treatment but not in the control untreated organ. The local de novo synthesis of B1 receptors for kinins that follows a noxious stimulus is proposed as a possible mechanism implicated in the chemical mediation of the inflammatory process.
mesh_terms: D000818:Animals; D001665:Binding Sites; D003556:Cystitis / Q000139:chemically induced / Q000378:metabolism*; D066298:In Vitro Techniques; D007705:Kinins / Q000378:metabolism* / Q000494:pharmacology; D008297:Male; D008642:Mesenteric Veins / Q000378:metabolism; D009130:Muscle, Smooth / Q000378:metabolism; D051381:Rats; D018002:Receptors, Bradykinin; D011956:Receptors, Cell Surface / Q000378:metabolism*; D001743:Urinary Bladder / Q000187:drug effects / Q000378:metabolism
chemical_list: D007705:Kinins; D018002:Receptors, Bradykinin; D011956:Receptors, Cell Surface