Ivermectin binding sites in sensitive and resistant Haemonchus contortus.
Membranes from both ivermectin-sensitive and -resistant Haemonchus contortus L3 larvae were examined for the presence of high affinity [3H]ivermectin binding sites. Both tissue preparations displayed high affinity drug binding sites (Kd = 0.13 nM). Receptor density (Bmax = 0.4 pmol/mg) was the same in both the sensitive and resistant nematodes suggesting that target site modification was not involved in the development of drug resistance in this particular strain of H. contortus. The H. contortus ivermectin binding site appeared to be similar to the well characterized Caenorhabditis elegans ivermectin binding site with respect to affinity for ivermectin and receptor density.
Rohrer
S P
SP
Basic Animal Science Research, Merck Research Laboratories, Rahway, New Jersey 07065.
Birzin
E T
ET
Eary
C H
CH
Schaeffer
J M
JM
Shoop
W L
WL
D000818:Animals; D001665:Binding Sites; D004351:Drug Resistance / Q000502:physiology; D006189:Haemonchus / Q000187:drug effects / Q000378:metabolism*; D007559:Ivermectin / Q000378:metabolism* / Q000494:pharmacology; D007814:Larva / Q000378:metabolism; D011955:Receptors, Drug / Q000032:analysis* / Q000502:physiology
D011955:Receptors, Drug; D007559:Ivermectin