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Okaramine insecticidal alkaloids show similar activity on both exon 3c and exon 3b variants of glutamate-gated chloride channels of the larval silkworm, Bombyx mori

Furutani, S; Ihara, M; Kai, K; Tanaka, K; Sattelle, DB; Hayashi, H; Matsuda, K; (2017) Okaramine insecticidal alkaloids show similar activity on both exon 3c and exon 3b variants of glutamate-gated chloride channels of the larval silkworm, Bombyx mori. NeuroToxicology , 60 pp. 240-244. 10.1016/j.neuro.2016.05.002. Green open access

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Abstract

The okaramine indole alkaloids were recently shown to be more selective than ivermectin in activating the glutamate-gated chloride channels of the silkworm larvae of Bombyx mori (BmGluCls). Those studies were carried out using the exon 3b variant as a representative of BmGluCls. However, it remains unknown whether okaramines are similarly effective on other silkworm GluCl variants and whether they share the same binding site as ivermectin on GluCls. To begin to address these questions, we examined the potency of four okaramines on the exon 3c variant of BmGluCls by two-electrode voltage clamp voltage recordings of glutamate-induced chloride currents. The potency of okaramines in activating the exon 3c BmGluCl agreed well with findings on the exon 3b BmGluCl and insecticidal potency. Okaramine B (10μM) reduced the maximum binding (Bmax) but not the dissociation constant (KD) of [(3)H]ivermectin in studies on plasma membrane fractions of HEK293 cells expressing the exon 3c variant. These findings indicate that activation of GluCls is important in the insecticidal actions of okaramines.

Type: Article
Title: Okaramine insecticidal alkaloids show similar activity on both exon 3c and exon 3b variants of glutamate-gated chloride channels of the larval silkworm, Bombyx mori
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.neuro.2016.05.002
Publisher version: http://doi.org/10.1016/j.neuro.2016.05.002
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions
Keywords: Binding assay, Glutamate-gated chloride channels, Ivermectin, Okaramines, Silkworm (Bombyx mori), Voltage-clamp electrophysiology
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Respiratory Medicine
URI: http://discovery.ucl.ac.uk/id/eprint/1499999
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