Bradykinin binding sites in healthy and carcinomatous human lung

Characterization of the bradykinin receptor in the human nasal airway using the binding of [125I]‐Hoe 140

“…Unlabelled Hoe 140 and NPC 567 also fully displaced the specific binding of ['251 Table 2 shows the bradykinin concentrations recovered by nasal lavage and the changes in Amin following house dust mite antigen challenge of subjects with allergic rhinitis. As previously reported, house dust mite antigen challenge significantly reduced the Amin (Austin et al, 1994 binding curve at 20°C (0.48 nM) and, independently from the association and dissociation rate constants at 40C (0.70 nM), are consistent with estimates in human lung of 0.73 nM (Trifilieff et al, 1994) and in guinea-pig ileum of 0.79 nm (Hock et al, 1991). The presence of multiple ['251]-Hoe 140 binding sites on the human nasal membranes cannot be excluded by using only a low concentration of radioligand in displacement studies as there may be high and low affinity binding sites for [1251]-Hoe 140, as proposed for guinea-pig lung and brain (Sequin et al, 1992).…”

“…The value for the apparent equilibrium dissociation constant for bradykinin which we obtained from binding data was 1 nM and this is similar to the value of 1.1 nM reported for human lung (Trifilieff et al, 1994) but rather higher than the value of 0.3 nM reported for guinea-pig ileum (Scherrer et al, 1995). Multiple binding sites for bradykinin have been reported in the guinea-pig lung, ileum and brain (Trifilieff et al, 1991;Sequin et al, 1992 higher value of 270 nm was obtained (Trifilieff et al, 1994). The value for guinea-pig ileum has been reported as varying from 8 to 210 nM (Farmer et al, 1989;Lyon et al, 1990;Sequin et al, 1992).…”

“…The protein concentration of the preparation was adjusted to 1 mg ml-'. The composition of the buffers used was based on the work of Trifilieff et al (1994) and was: Buffer A: TES 25 mM, 1,10 phenanthroline 1 mM, bacitracin 140 pg ml-', dithiothreitol mM, captopril 10 gM and bovine serum albumin 0.1%. The pH was 6.8.…”

Characterization of Bradykinin Receptors in Canine Cultured Corneal Epithelial Cells: Pharmacological and Functional Studies

“…2). The pharmacological properties of the BK receptors are consistent with those of B 2 receptors [8,17,18,32,33,37,38].…”

International Union of Pharmacology. XLV. Classification of the Kinin Receptor Family: from Molecular Mechanisms to Pathophysiological Consequences

“…The B 2 receptor is thought to be the major kinin receptor involved in airway responses to kinins, and radioligand binding studies have provided independent confirmation of the presence of B 2 receptors in healthy and carcinomatous lung samples (Trifilieff et al, 1994). Inhalation of the B 2 receptor agonists BK or Lys-BK caused bronchospasm in asthmatic but not normal subjects (Polosa and Holgate, 1990;Polosa et al, 1992).…”