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  • Title: Contractile and binding activities of structural analogues of LTC4 in the longitudinal muscle of guinea-pig ileum.
    Author: Sala A, Civelli M, Oliva D, Spur B, Crea AE, Folco GC, Nicosia S.
    Journal: Eicosanoids; 1990; 3(2):105-10. PubMed ID: 2206559.
    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.
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