Actions of picrodendrin antagonists on dieldrin‐sensitive and ‐resistant Drosophila GABA receptors

• Published in: British journal of pharmacology Vol. 119; no. 8; pp. 1569 - 1576
• Main Authors: Hosie, Alastair M., Ozoe, Yoshihisa, Koike, Kazuo, Ohmoto, Taichi, Nikaido, Tamotsu, Sattelle, David B.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.12.1996; Nature Publishing
• Subjects: Aminoacid receptors (glycine, glutamate, gaba); Animals; Biological and medical sciences; Cell receptors; Cell structures and functions; Dieldrin - pharmacology; dihydrotutin; Drosophila; Drosophila melanogaster; Electrophysiology; Fundamental and applied biological sciences. Psychology; GABA Antagonists - pharmacology; GABA receptor; Insecticides - pharmacology; Molecular and cellular biology; Mutation; Oocytes - metabolism; Picrodendrins; Rats; Receptors, GABA - biosynthesis; Receptors, GABA - drug effects; Receptors, GABA - genetics; RNA, Messenger - biosynthesis; Structure-Activity Relationship; Terpenes - antagonists & inhibitors; Terpenes - pharmacology; tutin; Xenopus laevis - metabolism; Insecta; Amphibia; Molecular interaction; Gabaergic receptor; Structure activity relation; Dicotyledones; Angiospermae; Antagonist; Recombinant protein; Pharmacognosy; Interspecific comparison; Drosophila; Xenopus laevis; Salientia; In vitro; Drosophilidae; Vertebrata; Biological fixation; Picrodendraceae; Arthropoda; Plant origin; Spermatophyta; Invertebrata; Diptera; Oocyte

1 A series of terpenoid compounds, recently isolated from Picrodendron baccatum, share a picrotoxane skeleton with picrotoxinin, an antagonist of ionotropic GABA receptors. Referred to as picrodendrins, they inhibit the binding of [35S]‐tert‐butylbicyclophosphorothionate (TBPS) to rat GABAA receptor...