title: Correlations of the electrophysiological activity of neonicotinoids with their binding and insecticidal activities.
abstract: 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.
authors.affiliation: Faculty of Agriculture, Kinki University, Nakamachi 3327-204, Nara 631-8505, Japan. nhisa@nara.kindai.ac.jp
authors.forename: Hisashi
authors.initials: H
authors.lastname: Nishiwaki
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Nakagawa
authors.forename: Morihiko
authors.initials: M
authors.lastname: Kuwamura
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Sato
authors.forename: Miki
authors.initials: M
authors.lastname: Akamatsu
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Matsuda
authors.forename: Koichiro
authors.initials: K
authors.lastname: Komai
authors.forename: Hisashi
authors.initials: H
authors.lastname: Miyagawa
mesh_terms: 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
chemical_list: 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