Protein Information

Name GABA receptor (protein family or complex)
Synonyms GABA receptor; GABA receptors; GABA(A) receptor; GABA(A) receptors; Gamma aminobutyric acid receptor; Gamma aminobutyric acid receptors

Compound Information

Name endrin
CAS

Reference List

PubMed Abstract RScore(About this table)
2474166 Wafford KA, Lummis SC, Sattelle DB: Block of an insect central nervous system GABA receptor by cyclodiene and cyclohexane insecticides. Proc R Soc Lond B Biol Sci. 1989 Jun 22;237(1286):53-61.

The results demonstrate that endrin and lindane block functional insect neuronal GABA receptors.
119(1,2,3,4) Details
1685414 Bloomquist JR, Grubs RE, Soderlund DM, Knipple DC: Prolonged exposure to GABA activates GABA-gated chloride channels in the presence of channel-blocking convulsants. Comp Biochem Physiol C. 1991;99(3):397-402.

In electrophysiological assays of GABA receptors expressed in Xenopus oocytes following injection with rat brain mRNA, endrin (20 microM) effectively blocked the transient currents elicited by brief exposure of oocytes to GABA (200 microM).
31(0,1,1,1) Details
3009836 Abalis IM, Eldefrawi ME, Eldefrawi AT: Effects of insecticides on GABA-induced chloride influx into rat brain microsacs. J Toxicol Environ Health. 1986;18(1):13-23.

The actions of different insecticides known to affect binding of ligands to gamma-aminobutyric acid (GABA) receptors were studied on the function of GABAA receptors in rat brain as assayed by GABA-induced 36Cl- influx into membrane microsacs.
The GABA-induced 36Cl- flux was inhibited by several cyclodienes and gamma-hexachlorocyclohexane (gamma-BHC) with the following order of decreasing potency: endosulfan I greater than endrin greater than endosulfan II greater than dieldrin greater than heptachlor epoxide greater than gamma-BHC greater than heptachlor.
1(0,0,0,1) Details
3000377 Bloomquist JR, Soderlund DM: Neurotoxic insecticides inhibit GABA-dependent chloride uptake by mouse brain vesicles. Biochem Biophys Res Commun. 1985 Nov 27;133(1):37-43.

The neurotoxic insecticides endrin, dieldrin, aldrin, lindane (gamma-1,2,3,4,5,6-hexachlorocyclohexane) and deltamethrin inhibited gamma-aminobutyric acid-dependent 36Cl- uptake by mouse brain vesicles.
These results demonstrate the disruption of gamma-aminobutyric acid receptor-chloride ionophore function in mammalian brain by neurotoxic insecticides and provide evidence that this complex is the principal site of cyclodiene action.
1(0,0,0,1) Details
1722072 Narahashi T: Transmitter-activated ion channels as the target of chemical agents. Adv Exp Med Biol. 1991;287:61-73.

Lindane and the cyclodienes dieldrin, endrin, heptachlor-epoxide, and isobenzan suppressed the GABA-activated chloride current.
It seems that general anesthetics have a specific affinity for the GABA receptor-channel complex.
2(0,0,0,2) Details
2850922 Seifert J: Ontogenesis and properties of the convulsant recognition site (s) of the gamma-aminobutyric acid (GABA) receptor complex in chicken embryo. Eur J Pharmacol. 1988 Jul 14;151(3):443-8.

The pharmacological properties of the embryonic recognition site (s) do not undergo significant changes during hatching based on the affinity of embryonic and chick brain membranes for [3H] TBOB; the rate of association and dissociation for TBOB; non-competitive inhibition of [3H] TBOB binding and modulation of 1R, alpha S-cis-cypermethrin interaction with the recognition site (s) by GABA; and inhibition of radioligand binding by endrin, picrotoxinin and TBPS.
1(0,0,0,1) Details
2409983 Abalis IM, Eldefrawi ME, Eldefrawi AT: Binding of GABA receptor channel drugs to a putative voltage-dependent chloride channel in Torpedo electric organ. Biochem Pharmacol. 1985 Jul 15;34(14):2579-82.

1(0,0,0,1) Details
2458634 Matsumoto K, Eldefrawi ME, Eldefrawi AT: Action of polychlorocycloalkane insecticides on binding of [35S] t-butylbicyclophosphorothionate to Torpedo electric organ membranes and stereospecificity of the binding site. Toxicol Appl Pharmacol. 1988 Sep 15;95(2):220-9.


Endrin was more potent than dieldrin, but endosulfan I and II had similar effects.
0(0,0,0,0) Details