Nitromethylene actions on in situ and expressed insect nicotinic acetylcholine receptors

FEBS Letters

Marshall, J.³  Jewess, P.¹  Sattelle, D.B.²  Leech, C.A.² 

[1] Sittingbourne Research Centre, Shell Research, Sittingbourne, Kent, ME9 8AG, UK;AFRC Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge, Downing Street, Cambridge, CB2 3EJ, UK;Department of Pharmacology, Yale University School of Medicine, Sterling Hall of Medicine, PO Box 3333, New Haven, CT 06510-8066, USA

关键词: Nicotinic receptor;    Receptor subunit;    Nitromethylene;    Insect;   

DOI  :  10.1016/0014-5793(91)81233-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Single channel recordings from dissociated housefly (Musca domestica) neurons show that a novel type of nitromethylene insecticide, 2(nitromethylene)tetrahydro-1,3-thiazine (NMTHT) gates a channel, the conductance and open time histogram of which resemble those obtained when acetylcholine is the agonist. Injection into Xenopus oocytes of a locust (Schistocerca gregaria) α-subunit mRNA results in the expression of functional nicotinic receptors sensitive to NMTHT. Control oocytes injected with distilled water are insensitive to the same concentration of this compound. Thus NMTHT exhibits agonist actions at both in situ and expressed insect nicotinic receptors, and one site of action of this compound is on an insect nicotinic receptor α-subunit.

【 授权许可】

Unknown