5-O-デメチルアベルメクチンA1a

説明

Avermectin B_1a is a macrocyclic lactone disaccharide anthelmintic agent that binds to high and low affinity sites on the mammalian GABA_A receptor. Binding to the high affinity site activates the receptor to increase chloride influx, while binding to the low affinity site blocks the channel. Avermectin B_1a inhibits binding of the glycine receptor antagonist strychnine to membranes and the solubilized receptor from rat spinal cord (K_is = 1.3 and 3.6 μM, respectively). Formulations containing avermectin B_1a (>80%) and avermectin B_1b (~20%; ) are used in insecticides and veterinary anthelmintic formulas as abamectin .

使用

Avermectin B1a is the major component (>80%) of a commercially available anthelmintic used to control parasitic nematodes in livestock. Avermectin B1a contains a secbutyl residue in the 25-position. In vitro and in vivo studies have shown that this analogue is the more potent analogue in the commercial product.

危険性

A poison by ingestion. Moderately toxic by skin contact.

安全性プロファイル

A poison by ingestion.Moderately toxic by skin contact. When heated todecomposition it emits acrid smoke and irritating fumes.