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

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

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. © 1995 Elsevier Science B.V. All rights reserved.

Original language	English
Pages (from-to)	257-260
Number of pages	3
Journal	Brain research
Volume	693
Issue number	1-2
DOIs	https://doi.org/10.1016/0006-8993(95)00605-P
Publication status	Published - 25 Sept 1995

Keywords

Bicyclic dinitrile
Convulsant site
Drosophila melanogaster
GABA receptor
RDL (resistance to dieldrin) subunit

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10.1016/0006-8993(95)00605-P

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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

@article{62b718f670944572a0860349b53c10fc,

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. {\textcopyright} 1995 Elsevier Science B.V. All rights reserved.",

keywords = "Bicyclic dinitrile, Convulsant site, Drosophila melanogaster, GABA receptor, RDL (resistance to dieldrin) subunit",

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.\}",

year = "1995",

month = sep,

day = "25",

doi = "10.1016/0006-8993(95)00605-P",

language = "English",

volume = "693",

pages = "257--260",

journal = "Brain research",

issn = "0006-8993",

publisher = "Elsevier BV",

number = "1-2",

}

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

TY - JOUR

T1 - 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

AU - Hosie, A. M.

AU - Shirai, Y.

AU - Buckingham, S. D.

AU - Rauh, J. J.

AU - Roush, R. T.

AU - Baylis, H. A.

AU - Sattelle, D. B.

PY - 1995/9/25

Y1 - 1995/9/25

N2 - 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. © 1995 Elsevier Science B.V. All rights reserved.

AB - 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. © 1995 Elsevier Science B.V. All rights reserved.

KW - Bicyclic dinitrile

KW - Convulsant site

KW - Drosophila melanogaster

KW - GABA receptor

KW - RDL (resistance to dieldrin) subunit

U2 - 10.1016/0006-8993(95)00605-P

DO - 10.1016/0006-8993(95)00605-P

M3 - Article

C2 - 8653417

SN - 0006-8993

VL - 693

SP - 257

EP - 260

JO - Brain research

JF - Brain research

IS - 1-2

ER -

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

Keywords

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