Tomizawa_2001_J.Neurochem_78_1359

Reference

Title : Photoaffinity labeling of insect nicotinic acetylcholine receptors with a novel [(3)H]azidoneonicotinoid - Tomizawa_2001_J.Neurochem_78_1359
Author(s) : Tomizawa M , Wen Z , Chin HL , Morimoto H , Kayser H , Casida JE
Ref : Journal of Neurochemistry , 78 :1359 , 2001
Abstract : The nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel in the insect CNS and a target for major insecticides. Here we use photoaffinity labeling to approach the functional architecture of insect nAChRs. Two candidate 5-azido-6-chloropyridin-3-yl photoaffinity probes are evaluated for their receptor potencies: azidoneonicotinoid (AzNN) with an acyclic nitroguanidine moiety; azidodehydrothiacloprid. Compared to their non-azido parents, both probes are of decreased potencies at Drosophila (fruit fly) and Musca (housefly) receptors but AzNN retains full potency at the Myzus (aphid) receptor. [(3)H]AzNN was therefore radiosynthesized at high specific activity (84 Ci/mmol) as a novel photoaffinity probe. [(3)H]AzNN binds to a single high-affinity site in Myzus that is competitively inhibited by imidacloprid and nicotine and further characterized as to its pharmacological profile with various nicotinic ligands. [(3)H]AzNN photoaffinity labeling of Myzus and Homalodisca (leafhopper) detects a single radiolabeled peak in each case displaceable with imidacloprid and nicotine and with molecular masses corresponding to approximately 45 and approximately 56 kDa, respectively. The photoaffinity-labeled receptor in both Drosophila and Musca has imidacloprid- and nicotine-sensitive profiles and migrates at approximately 66 kDa. These photoaffinity-labeled polypeptides are considered to be the insecticide-binding subunits of native insect nAChRs.
ESTHER : Tomizawa_2001_J.Neurochem_78_1359
PubMedSearch : Tomizawa_2001_J.Neurochem_78_1359
PubMedID: 11579144

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Tomizawa M, Wen Z, Chin HL, Morimoto H, Kayser H, Casida JE (2001)
Photoaffinity labeling of insect nicotinic acetylcholine receptors with a novel [(3)H]azidoneonicotinoid
Journal of Neurochemistry 78 :1359

Tomizawa M, Wen Z, Chin HL, Morimoto H, Kayser H, Casida JE (2001)
Journal of Neurochemistry 78 :1359