| Name | gamma aminobutyric acid receptor (protein family or complex) |
|---|---|
| Synonyms | GABA receptor; GABA receptors; GABA(A) receptor; GABA(A) receptors; Gamma aminobutyric acid receptor; Gamma aminobutyric acid receptors |
| Name | cypermethrin |
|---|---|
| CAS | cyano(3-phenoxyphenyl)methyl 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 6090849 | Cole LM, Lawrence LJ, Casida JE: Similar properties of [35S] t-butylbicyclophosphorothionate receptor and coupled components of the GABA receptor-ionophore complex in brains of human, cow, rat, chicken and fish. Life Sci. 1984 Oct 22;35(17):1755-62. This species similarity includes dissociation constants of 61-77 nM at 37 degrees C, maximum receptor densities of 3-7 pmol/mg protein, and sensitivity to inhibition or displacement by two cage convulsants (picrotoxinin and t-butylbicycloorthobenzoate) and the insecticide [1R,cis, alpha S]-cypermethrin, indicating a constancy during vertebrate evolution of the [35S] TBPS binding site and its coupling with other components of the GABA receptor-ionophore complex. |
83(1,1,1,3) | Details |
| 6310756 | Lawrence LJ, Casida JE: Stereospecific action of pyrethroid insecticides on the gamma-aminobutyric acid receptor-ionophore complex. Science. 1983 Sep 30;221(4618):1399-401. Scatchard analysis indicates that picrotoxinin inhibition of t-butylbicyclophosphorothionate binding is competitive whereas cypermethrin inhibition possibly involves a closely associated site in the gamma-aminobutyric acid receptor-ionophore complex. |
82(1,1,1,2) | Details |
| 3029901 | Crofton KM, Reiter LW, Mailman RB: Pyrethroid insecticides and radioligand displacement from the GABA receptor ionophore complex. Toxicol Lett. 1987 Feb;35(2-3):183-90. |
2(0,0,0,2) | Details |
| 2981097 | Seifert J, Casida JE: Solubilization and detergent effects on interactions of some drugs and insecticides with the t-butylbicyclophosphorothionate binding site within the gamma-aminobutyric acid receptor-ionophore complex. J Neurochem. 1985 Jan;44(1):110-6. Levels of (1R, alpha S)-cis-cypermethrin and dimethylbutylbarbiturate which are inhibitory with RBM are moderately stimulatory after TBPS receptor solubilization. |
2(0,0,0,2) | Details |
| 2998820 | Seifert J, Casida JE: Regulation of [35S] t-butylbicyclophosphorothionate binding sites in rat brain by pyrethroid and barbiturate. Eur J Pharmacol. 1985 Sep 24;115(2-3):191-8. regulates the binding of [35S] t-butylbicyclophosphorothionate ([35S] TBPS) within the GABA receptor-ionophore complex by decreasing the rate of radioligand association and increasing the rate of dissociation but in different ways for the EDTA/water-dialyzed rat brain membranes and a solubilized preparation obtained on treatment with the zwitterionic detergent CHAPS. GABA at micromolar levels also greatly influences the action of compounds within the TBPS domain, facilitating and modulating displacement of [35S] TBPS from EDTA/water-dialyzed membranes by the alpha-cyanopyrethroid cypermethrin and the barbiturate 5-(1',3'-dimethylbutyl)-5-ethylbarbiturate. |
1(0,0,0,1) | Details |
| 2985459 | Gammon DW: Correlations between in vitro and in vivo mechanisms of pyrethroid insecticide action. Fundam Appl Toxicol. 1985 Feb;5(1):9-23. Studies of poisoning signs and nerve disruptions in vivo in the mouse and cockroach, using diazepam in conjunction with pyrethroids, implicated the GABA-receptor complex as a target for alpha-CN-phenoxybenzyl pyrethroids. It also showed two modes of action for permethrin and cypermethrin, its alpha-cyano analog. |
1(0,0,0,1) | Details |
| 2850922 | Seifert J: Ontogenesis and properties of the convulsant recognition site (s) of the (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 and inhibition of radioligand binding by endrin, picrotoxinin and TBPS. |
1(0,0,0,1) | Details |
| 2455860 | Brown GB, Gaupp JE, Olsen RW: Pyrethroid insecticides: stereospecific allosteric interaction with the batrachotoxinin-A binding site of mammalian voltage-sensitive channels. Mol Pharmacol. 1988 Jul;34(1):54-9. Their mechanism of action is thought to involve effects primarily at the voltage-sensitive sodium channel of both insect and mammalian neurons, although recent studies have raised the possibility that these compounds may also act at the gamma-aminobutyric acid receptor- ionophore complex. Comparison of the rank order of potency for enhancement of [3H] batrachotoxinin-A 20-alpha- binding and insecticidal activity in a series of toxic stereoisomers of cypermethrin, representative of the class, reveals a correlation between the two measures. |
1(0,0,0,1) | Details |
| 3009836 | Abalis IM, Eldefrawi ME, Eldefrawi AT: Effects of insecticides on -induced 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 (GABA) receptors were studied on the function of GABAA receptors in rat brain as assayed by -induced 36Cl- influx into membrane microsacs. The four pyrethroids tested also inhibited the -induced 36Cl- flux with the following decreasing potencies: 1R,cis,alpha S-cypermethrin greater than 1R,trans, alpha S-cypermethrin greater than fluvalinate greater than allethrin. |
1(0,0,0,1) | Details |
| 8054658 | Bloomquist JR: Cyclodiene resistance at the insect GABA receptor/chloride channel complex confers broad cross resistance to convulsants and experimental phenylpyrazole insecticides. Arch Insect Biochem Physiol. 1994;26(1):69-79. In contrast, this strain was susceptible to cypermethrin and the avermectins MK-243, abamectin, and abamectin 8,9-oxide. |
1(0,0,0,1) | Details |