Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes

A. M. Hosie; Y. Shirai; S. D. Buckingham; J. J. Rauh; R. T. Roush; H. A. Baylis; D. B. Sattelle

doi:10.1016/0006-8993(95)00605-P

Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes

A. M. Hosie, Y. Shirai, S. D. Buckingham, J. J. Rauh, R. T. Roush, H. A. Baylis, D. B. Sattelle

College of Agricultural Sciences

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Abstract

The receptor antagonist actions are described for a novel bicyclic dinitrile compound (BIDN, 3,3-bis-(trifluoromethyl)-bicyclo [2.2.1] heptane-2,2-dicarbonitrile) on a Drosophila melanogaster homo-oligomeric GABA receptor expressed in Xenopus oocytes. BIDN blocked the wild-type form of the receptor in a neither purely competitive, nor purely non-competitive manner, being dependent on the GABA concentration yet insurmountable, and block was independent of the membrane potential. BIDN was found to be less effective against a mutant (A³⁰² → S) form of the receptor resistant to dieldrin and picrotoxinin. This cross resistance of dieldrin-resistant receptors to BIDN is of interest in the light of recent findings that BIDN binding to insect membranes is displaced competitively by dieldrin, but not by picrotoxinin.

Original language	English (US)
Pages (from-to)	257-260
Number of pages	4
Journal	Brain research
Volume	693
Issue number	1-2
DOIs	https://doi.org/10.1016/0006-8993(95)00605-P
State	Published - Sep 25 1995

All Science Journal Classification (ASJC) codes

General Neuroscience
Molecular Biology
Clinical Neurology
Developmental Biology

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Hosie, A. M., Shirai, Y., Buckingham, S. D., Rauh, J. J., Roush, R. T., Baylis, H. A., & Sattelle, D. B. (1995). Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes. Brain research, 693(1-2), 257-260. https://doi.org/10.1016/0006-8993(95)00605-P

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title = "Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes",

abstract = "The receptor antagonist actions are described for a novel bicyclic dinitrile compound (BIDN, 3,3-bis-(trifluoromethyl)-bicyclo [2.2.1] heptane-2,2-dicarbonitrile) on a Drosophila melanogaster homo-oligomeric GABA receptor expressed in Xenopus oocytes. BIDN blocked the wild-type form of the receptor in a neither purely competitive, nor purely non-competitive manner, being dependent on the GABA concentration yet insurmountable, and block was independent of the membrane potential. BIDN was found to be less effective against a mutant (A302 → S) form of the receptor resistant to dieldrin and picrotoxinin. This cross resistance of dieldrin-resistant receptors to BIDN is of interest in the light of recent findings that BIDN binding to insect membranes is displaced competitively by dieldrin, but not by picrotoxinin.",

author = "Hosie, {A. M.} and Y. Shirai and Buckingham, {S. D.} and Rauh, {J. J.} and Roush, {R. T.} and Baylis, {H. A.} and Sattelle, {D. B.}",

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Hosie, AM, Shirai, Y, Buckingham, SD, Rauh, JJ, Roush, RT, Baylis, HA & Sattelle, DB 1995, 'Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes', Brain research, vol. 693, no. 1-2, pp. 257-260. https://doi.org/10.1016/0006-8993(95)00605-P

Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes. / Hosie, A. M.; Shirai, Y.; Buckingham, S. D. et al.
In: Brain research, Vol. 693, No. 1-2, 25.09.1995, p. 257-260.

Research output: Contribution to journal › Article › peer-review

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Blocking actions of BIDN, a bicyclic dinitrile convulsant compound, on wild-type and dieldrin-resistant GABA receptor homo-oligomers of Drosophila melanogaster expressed in Xenopus oocytes

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