A chemiluminescent assay for measuring avermectin binding sites.
Avermectins are potent, broad spectrum anthelmintics. We describe the synthesis of a biologically active chemiluminescent compound, 22,23-dihydroavermectin B1a, 4"-[4-[[4-[ethyl(1,2,3,4-tetrahydro-1,4-dioxo-6- phthalazinyl)amino]butyl]amino]-4-oxobutanoate] (ivermectin-luminol). This compound retains its anthelmintic properties and provides an extremely sensitive nonradioactive probe to study avermectin binding sites.
Schaeffer
J M
JM
Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
Stiffey
J H
JH
Mrozik
H
H
D000818:Animals; D000871:Anthelmintics / Q000378:metabolism*; D002107:Caenorhabditis / Q000378:metabolism*; D007559:Ivermectin / Q000031:analogs & derivatives* / Q000032:analysis / Q000378:metabolism; D007700:Kinetics; D008163:Luminescent Measurements; D008165:Luminol / Q000031:analogs & derivatives / Q000032:analysis*; D008566:Membranes / Q000378:metabolism; D011724:Pyridazines / Q000032:analysis*
D000871:Anthelmintics; D011724:Pyridazines; C059895:22,23-dihydroavermectin B(1a)-4''-(4-((4-(ethyl(1,2,3,4-tetrahydro-1,4-dioxo-6-phthalazinyl)amino)butyl)amino)-4-oxobutanoate); D008165:Luminol; D007559:Ivermectin; C019264:avermectin