Leukotriene C4 binding sites in the rat central nervous system.
Binding sites for [3H]LTC4 were observed in crude membrane preparations of rat central nervous system tissue. Equilibrium binding studies indicated one high affinity [3H]LTC4 binding site with a KD of 31.4 +/- 3.4 nM for whole brain preparations. The binding was highly specific for [3H]LTC4 and could be inhibited by the SRS-A antagonist FPL 55172. Specific binding was increased with both mono- and di-valent ions. Regional distribution studies revealed a three-fold difference in binding capacity within different regions of the brain with the highest binding capacity in the brainstem (94.1 +/- 6.9 fmol/mg of protein) and the lowest in the hypothalamus (29.6 +/- 12.8 fmol/mg of protein). In addition, weak low capacity binding was observed for [3H]LTB4 and [3H]LTE4, while no saturable binding was observed for [3H]LTD4. The order of selectivity in inhibiting [3H]LTC4 binding was LTC4 much greater than LTD4 = LTE4 greater than LTB4.
D000818:Animals; D001881:Borates / Q000494:pharmacology; D001921:Brain / Q000378:metabolism*; D002412:Cations / Q000378:metabolism; D002867:Chromones / Q000494:pharmacology; D005978:Glutathione / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D007975:Leukotriene B4 / Q000378:metabolism; D008566:Membranes / Q000378:metabolism; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism*; D018077:Receptors, Leukotriene; D011982:Receptors, Prostaglandin / Q000378:metabolism*; D013189:SRS-A / Q000378:metabolism; D012694:Serine / Q000494:pharmacology
D001881:Borates; D002412:Cations; D002867:Chromones; D011956:Receptors, Cell Surface; D018077:Receptors, Leukotriene; D011982:Receptors, Prostaglandin; D013189:SRS-A; C040900:serine-borate complex; D007975:Leukotriene B4; D012694:Serine; C006312:FPL 55712; D005978:Glutathione