Avermectin B1a  (Synonyms: Abamectin B1a)

Avermectin B1a is an antiparasitic agent that paralyzes nematodes without causing hypercontraction or flaccid paralysis.

[³H]AVM B1a preferentially binds to synaptic membranes from several regions of rat brain. [³H]AVM B1a specific binding to intact monolayers of granule cells increases rapidly with time of incubation and reaches equilibrium after approximately 20 min at 24°C. Higher concentrations of [³H]AVM B1a leads to markedly greater nonspecific binding, 60% at 25 nM. Various AVM analogs also produce concentration-dependent inhibition of [³H]AVM B1a binding in intact cerebellar neurons. AVM B1a and moxidectin are similar in potency (IC₅₀ values, 120 and 126 nM, respectively)^[3]. AVMB1a-stimulated chloride efflux from mouse brain synaptic vesicles results from the activation of GABA-insensitive chloride channels and that this action is distinct from their previously documented effects on GABA-gated chloride channels in mouse brain preparations^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bacteria are significantly inhibited when the AVM B1a concentration is higher than 83.3 mg/kg, while fungi are less impaired in soil. Soil respiration is also inhibited by high concentration AVM B1a, which differs with soil types. The half lethal dosage (LD₅₀) of AVM B1a to soil earthworm is estimated as 4.63 mg × cm² in filter paper contact test, and as 24.13 and 17.06 mg/kg, respectively after treated 7 and 14 days in artificial soil^[1]. Iin artificial soil, the LC50 of AVM B1a on earthworms are 24.1 mg/kg and 17.1 mg/kg, respectively, for 7 and 14 days. About 80.0% and 94.8% of the accumulated AVM B1a are eliminated respectively in two groups within 1 day after they are exposed to AVM B1a-free soil, but a trace amount of AVM B1a is found for a relative long time in earthworms^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

873.08

Solid

C₄₈H₇₂O₁₄

65195-55-3

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Room temperature in continental US; may vary elsewhere.

• [1]. Sun Y, et al. [Effects of avermectin B1a on soil microorganism and earthworm (Eisenia fetida)]. Ying Yong Sheng Tai Xue Bao. 2005 Nov;16(11):2140-3.  [Content Brief]

  [2]. Sun Y, et al. Bioaccumulation and elimination of avermectin B1a in the earthworms (Eisenia fetida). Chemosphere. 2005 Jul;60(5):699-704  [Content Brief]

  [3]. Huang J, et al. Avermectin B1a binds to high- and low-affinity sites with dual effects on the gamma-aminobutyric acid-gated chloride channel of cultured cerebellar granule neurons. J Pharmacol Exp Ther. 1997 Apr;281(1):261-6.  [Content Brief]

  [4]. Payne GT, et al. Activation of gamma-aminobutyric acid insensitive chloride channels in mouse brain synaptic vesicles by avermectin B1a. J Biochem Toxicol. 1991 Winter;6(4):283-92.  [Content Brief]