| ID | 21 |
|---|---|
| Name | chloride channel (protein family or complex) |
| Synonyms | chloride channel |
| ID | 182 |
|---|---|
| Name | endosulfan |
| CAS | 6,7,8,9,10,10-hexachloro-1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepin 3-oxide |
| PubMed | Abstract | RScore(About this table) |
|---|---|---|
| 8968340 | Huang J, Casida JE: Characterization of [3H] ethynylbicycloorthobenzoate ([3H] EBOB) binding and the action of insecticides on the -gated chloride channel in cultured cerebellar granule neurons. J Pharmacol Exp Ther. 1996 Dec;279(3):1191-6. [3H] Ethynylbicycloorthobenzoate ([3H] EBOB) is a recently developed specific radioligand for the noncompetitive blocker site of the (GABA) receptor, which is the target of many polychlorocycloalkane and heterocyclic insecticides. This study characterizes [3H] EBOB binding and the action of insecticides on the -gated chloride channel of cerebellar granule neurons in primary culture. Specific [3H] EBOB binding increases rapidly between days 3 and 7 and then remains constant for days 7 to 12 in culture. A single, high-affinity and saturable binding site is involved with Kd = 0.51 nM and Bmax = 239 fmol/mg protein. and muscimol are 6- to 12-fold more potent as inhibitors of [3H] EBOB binding to membranes from cultured cerebellar granule neurons than from cerebellar tissue, possibly because of localization of specific subunits in the granule cells. -stimulated 36Cl- influx is also inhibited by seven insecticidal compounds (including EBOB, 12-ketoendrin and alpha-endosulfan) as well as picrotoxinin and t-butylbicyclophosphorothionate with IC50 levels ranging from 290 to 15300 nM, which correlate well (r = 0.92) with their inhibitory potencies for [3H] EBOB binding (1 to 773 nM). These findings validate the use of [3H] EBOB binding in cultured cerebellar granule cells for pharmacological studies on insecticides and other toxicants acting at the noncompetitive blocker or coupled site of the GABAA receptor/chloride channel complex. |
3(0,0,0,3) |