Contractile and binding activities of structural analogues of LTC4 in the longitudinal muscle of guinea-pig ileum.

Abstract

High affinity binding sites for LTC4 have been identified in various tissues, including guinea-pig ileal longitudinal muscle. More recently, it has been shown that LTC4 binds to non-receptor sites as well, particularly to glutathione transferases. In the present study, LTC4 and 9 chemically synthesized analogues, as well as the SRS-A antagonist FPL 55712 and S-decyl-glutathione, were tested for their ability to inhibit 3H-LTC4 binding in membranes from guinea-pig ileal longitudinal muscle and to affect the tone of the ileum in vitro. A significant correlation between binding and contractile activities was found for the LTC4 analogues and FPL 55712. However, S-decyl-glutathione, although possessing some affinity for LTC4 binding sites, was devoid of any effect on guinea-pig ileum tone at least up to 10(-5) M, thus indicating that these sites cannot be functional receptors, although they may represent other units involved in leukotriene action, e.g. uptake sites.