Characterization of the leukotriene D4 receptor in hyperreactive rat lung.
A [3H]leukotriene D4 radioreceptor binding assay has been established in rat lung and has been used to fully characterize the leukotriene D4 receptor in lung membranes from an inbred strain of rats displaying non-specific bronchial hyperreactivity. [3H]leukotriene D4 specific binding in this tissue is of high affinity (KD 0.12 nM), saturable (Bmax 42 fmol/mg protein), inhibited by both guanine nucleotide analogues and sodium ions and increased by divalent cations. In addition, Ki values show that agonists, but not antagonists, compete for [3H]leukotriene D4 binding in rat lung with the same potency as they compete for [3H]leukotriene D4 binding in guinea-pig lung, the classical tissue for leukotriene D4 receptor studies. Finally, [3H]leukotriene D4 binding in hyperreactive rat lung has been compared with [3H]leukotriene D4 binding in lung tissue from Fischer rats, which are a less responsive strain.
Metters
K M
KM
Department of Pharmacology, Merck Frosst Centre for Therapeutic Research, Dorval, Quebec, Canada.
Frey
E A
EA
Ford-Hutchinson
A W
AW
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D006967:Hypersensitivity / Q000378:metabolism*; D066298:In Vitro Techniques; D007191:Indazoles / Q000494:pharmacology; D007700:Kinetics; D008168:Lung / Q000378:metabolism*; D008297:Male; D011422:Propionates / Q000494:pharmacology; D011506:Proteins / Q000378:metabolism; D011804:Quinolines / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors / Q000378:metabolism*; D018077:Receptors, Leukotriene; D013189:SRS-A / Q000037:antagonists & inhibitors / Q000378:metabolism*
D007191:Indazoles; D011422:Propionates; D011506:Proteins; D011804:Quinolines; D011971:Receptors, Immunologic; D018077:Receptors, Leukotriene; D013189:SRS-A; C054217:ICI 198615; C059141:verlukast