Avermectin B1a inhibits the binding of strychnine to the glycine receptor of rat spinal cord.
The anthelmintic drug, avermectin B1a, has been reported to interfere with gamma-aminobutyric acid-mediated chloride conductance. Also, enhancement of diazepam binding to mammalian brain membranes by avermectin B1a has led to the suggestion that avermectin B1a interacts with the 'benzodiazepine receptor-gamma-aminobutyric acid receptor-chloride ionophore' complex. Here we report an interaction of avermectin B1a with the glycine receptor. The binding of the glycine receptor antagonist, strychnine, to both membranes and solubilized receptor from rat spinal cord, was inhibited by avermectin B1a with Ki values of 1.3 microM and 3.6 microM, and Hill coefficients of 0.46 and 0.62, respectively.
D000818:Animals; D007559:Ivermectin / Q000031:analogs & derivatives*; D007783:Lactones / Q000494:pharmacology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D018009:Receptors, Glycine; D013116:Spinal Cord / Q000187:drug effects* / Q000378:metabolism; D013331:Strychnine / Q000037:antagonists & inhibitors* / Q000378:metabolism
D007783:Lactones; D011956:Receptors, Cell Surface; D018009:Receptors, Glycine; C022120:avermectin B(1)a; D007559:Ivermectin; D013331:Strychnine