Protein Information

Name glycine receptor (protein family or complex)
Synonyms Glycine receptor; Glycine receptors

Compound Information

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

Reference List

PubMed Abstract RScore(About this table)
12614680 Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA (A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403.

Lindane inhibited with similar potency both GABA (A) (IC (50): 6.1 microM) and glycine (5.0 microM) receptors. alpha-Endosulfan and dieldrin inhibited the GABA (A) receptor (IC (50) values: 0.4 microM and 0.2 microM, respectively) more potently than the glycine receptor (IC (50) values: 3.5 microM and 3 microM, respectively).
87(1,1,1,7) Details
9432128 Turner KO, Syvanen M, Meizel S: The human acrosome reaction is highly sensitive to inhibition by cyclodiene insecticides. J Androl. 1997 Nov-Dec;18(6):571-5.

It can be initiated in vitro by progesterone, a putative physiological initiator that helps to activate sperm GABA (A) receptor/chloride channels and by glycine, a substitute for the egg zona pellucida, which activates sperm glycine receptor/chloride channels.
Even at 1 nM (0.41 ng/ml or 0.41 ppb), chlordane and endosulfan, chlorinated cyclodiene blockers of insect neuronal GABA (A) receptor/chloride channels, strongly inhibited the AR initiated by progesterone or glycine.
1(0,0,0,1) Details
10698677 Kamijima M, Casida JE: Regional modification of [(3) H] Ethynylbicycloorthobenzoate binding in mouse brain GABA (A) receptor by endosulfan, fipronil, and avermectin B (1a). Toxicol Appl Pharmacol. 2000 Mar 1;163(2):188-94.

AVM increased [(3) H] EBOB binding in most regions and was the only one of the three agents inhibiting in vitro [(3) H] strychnine binding to the glycine receptor.
1(0,0,0,1) Details