Abstract
The actions of LY255283, a leukotriene (LT) B 4 receptor antagonist, were examined on guinea pig lung. LTB 4 and LY255283 displaced [ 3H]LTB 4 from its binding site on lung membranes with pK i values of 9.9 and 7.0, respectively. In the functional correlate of the binding studies, LY255283 competitively reduced contractile responses of lung parenchyma to LTB 4 (pA 2 = 7.2). LTB 4 produced airway obstruction which was reduced by LY255283 administered i.v. (ED 50 = 2.8 mg/kg) or orally (ED 50 = 11.0 mg/kg). Contractile responses to histamine, LTD 4 and the thromboxane mimetic, U46619, were not reduced by LY255283. The compound also did not inhibit cyclooxygenase or 5-lipoxygenase enzymes. We conclude that LY255283 selectively antagonized pharmacologic responses to LTB 4 on lung tissue and appears to be a useful tool to investigate the role of LTB 4 in pulmonary disease.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
