Correlations of the electrophysiological activity of neonicotinoids with their binding and insecticidal activities.
The electrophysiological actions of various neonicotinoids, including substituted benzyl derivatives, against recombinant Drosophila SAD/chicken beta2 hybrid nicotinic acetylcholine receptor (nAChR) were measured to analyze the relationships between the in vivo (insecticidal) and in vitro (binding and agonist) activities. Most of the neonicotinoids tested were capable of inducing inward currents by activating the hybrid nAChRs expressed in Xenopus laevis oocytes, whereas some compounds had no agonist activity and only blocked the acetylcholine-induced currents. Variations in the agonist activity were well correlated with those in the binding potency evaluated using [3H]imidacloprid as well as insecticidal activities.
Nishiwaki
Hisashi
H
Faculty of Agriculture, Kinki University, Nakamachi 3327-204, Nara 631-8505, Japan. nhisa@nara.kindai.ac.jp
Nakagawa
Yoshiaki
Y
Kuwamura
Morihiko
M
Sato
Kazuyuki
K
Akamatsu
Miki
M
Matsuda
Kazuhiko
K
Komai
Koichiro
K
Miyagawa
Hisashi
H
D000465:Algorithms; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000819:agonists / Q000737:chemistry / Q000494:pharmacology; D002038:Bungarotoxins / Q000494:pharmacology; D004330:Drosophila / Q000187:drug effects; D004594:Electrophysiology / Q000379:methods; D007093:Imidazoles / Q000378:metabolism; D007306:Insecticides / Q000737:chemistry / Q000494:pharmacology*; D000073943:Neonicotinoids; D009538:Nicotine / Q000819:agonists / Q000031:analogs & derivatives / Q000494:pharmacology*; D018722:Nicotinic Agonists / Q000737:chemistry / Q000494:pharmacology*; D009574:Nitro Compounds; D009865:Oocytes / Q000187:drug effects / Q000502:physiology; D011725:Pyridines / Q000819:agonists / Q000737:chemistry / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D014316:Tritium; D014982:Xenopus laevis
D019086:Bridged Bicyclo Compounds, Heterocyclic; D002038:Bungarotoxins; D007093:Imidazoles; D007306:Insecticides; D000073943:Neonicotinoids; D018722:Nicotinic Agonists; D009574:Nitro Compounds; D011725:Pyridines; D011978:Receptors, Nicotinic; D014316:Tritium; C082359:imidacloprid; D009538:Nicotine; C082748:epibatidine