Protein Information

Name cholinesterase
Synonyms Acylcholine acylhydrolase; BCHE; BCHE protein; Butyrylcholine esterase; Butyrylcholinesterase; CHE1; Choline esterase II; Cholinesterase…

Compound Information

Name leptophos
CAS

Reference List

PubMed Abstract RScore(About this table)
8511793 Veronesi B, Ehrich M: Differential cytotoxic sensitivity in mouse and human cell lines exposed to organophosphate insecticides. Toxicol Appl Pharmacol. 1993 Jun;120(2):240-6.

Baseline activities of the major target esterases, i.e., cholinesterase, carboxylesterase, and neurotoxic esterase, were assayed in mouse and several human neural candidate cell lines.
IC50 data indicated that the tested mouse cell line was consistently more sensitive than the human cell line to equimolar doses of various OP compounds (e.g., mipafox, parathion, paraoxon, DFP, leptophos oxon, fenthion, and fenitrothion).
1(0,0,0,1) Details
72085 Bradway DE, Shafik TM, Lores EM: Comparison of cholinesterase activity, residue levels, and urinary metabolite excretion of rats exposed to organophosphorus pesticides. J Agric Food Chem. 1977 Nov-Dec;25(6):1353-8.

1(0,0,0,1) Details
6178187 Moroi K, Kuga T: Inhibitory effect of leptophos on carboxylesterase (isocarboxazid amidase) in rat liver. Toxicol Lett. 1982 Apr;11(1-2):81-5.

0(0,0,0,0) Details
565668 Obersteiner EJ, Sharma RP: Evaluation of cytotoxic responses caused by selected organophosphorus esters in chick sympathetic ganglia cultures. Can J Comp Med. 1978 Jan;42(1):80-8.


Concentrations that produced half-maximal effects ranged from 1 x 10 (-6) M (severely toxic) for methylparathian, diazinon, paraoxon, mevinphos, diisopropylfluorophosphate, tri-o-tolyl phosphate and its mixed isomers to a 1 x 10 (-3) M (intermediate) for malathion, leptophos, coumaphos, mono- and dicrotophos.
0(0,0,0,0) Details
6154073 Riskallah MR: Reduced sensitivity of cholinesterase as a factor of resistance in leptophos selected strain in the Egyptian cotton leafworm. J Environ Sci Health B. 1980;15(2):181-92.

On the other hand, there was a considerable degree of insensitivity of cholinesterase to inhibition by leptophos-oxon, methyl paraoxon, cyolane, cytrolane, monocrotophos, and matacil in larvae of the resistant strain.
115(1,2,2,5) Details
12742374 Yen JH, Tsai CC, Wang YS: Separation and toxicity of enantiomers of organophosphorus insecticide leptophos. Ecotoxicol Environ Saf. 2003 Jun;55(2):236-42.

From the inhibition test of butyrylcholinesterase, the half-inhibitory concentrations, IC (50), of (+)-leptophos, (-)-leptophos, and (+/-)-leptophos were 0.241, 1.17, and 1.05 gmL (-1), respectively.
82(1,1,1,2) Details
72768 El-Sebae AH, Soliman SA, Elamayem MA, Ahmed NS: Neurotoxicity of organophosphorus insecticides Leptophos and EPN. J Environ Sci Health B. 1977;12(4):269-87.

The results revealed that all five compounds were inhibitors of cholinesterase, but only Leptophos and EPN were shown to be potent inhibitors for both neurotoxic esterase and monoamine oxidase in the mouse brain.
32(0,1,1,2) Details
2446940 Gant DB, Eldefrawi ME, Eldefrawi AT: Action of organophosphates on GABAA receptor and voltage-dependent chloride channels. Fundam Appl Toxicol. 1987 Nov;9(4):698-704.

The industrial organophosphate tri-o-cresyl phosphate and the anticholinesterase organophosphate insecticides leptophos, leptophos oxon, and O-ethyl O-4-nitrophenyl phenylphosphonothioate inhibited GABA-regulated chloride channels and bound with high affinity to the voltage-dependent chloride channels (IC50 = 0.3 to 8.7 microM).
31(0,1,1,1) Details
1200722 Davies JE, Barquet A, Freed VH, Haque R, Morgade C, Sonneborn RE, Vaclavek C: Human pesticide poisonings by a fat-soluble organophosphate insecticide. Arch Environ Health. 1975 Dec;30(12):608-13.

Two patients died, and in the three survivors, cholinesterase symptoms persisted for five to 48 days.
The partition coefficient of dichlofenthion in fat was 20 times greater than parathion, and exceeded only by leptophos.
2(0,0,0,2) Details
6470929 Matsubara T, Horikoshi I: Spontaneous reactivation of mouse plasma cholinesterase after inhibition by various organophosphorus compounds. J Pharmacobiodyn. 1984 May;7(5):322-8.

The plasma ChEs inhibited by surecide, salithion and leptophos, which contain no O,O-dimethyl moiety, were not reactivated or only slightly so.
2(0,0,0,2) Details
7338954 Nishio A, Uyeki EM: Induction of sister chromatid exchanges in Chinese hamster ovary cells by organophosphate insecticides and their oxygen analogs. J Toxicol Environ Health. 1981 Nov-Dec;8(5-6):939-46.

Induction of sister chromatid exchanges (SCEs) in cultures of Chinese hamster ovary cells by 10 anticholinesterase organophosphate insecticides was investigated.
The insecticides were two phosphates (dichlorvos and dicrotophos), four sulfur-containing organophosphates (malathion, parathion, leptophos, and diazinon), and four oxygen analogs of the latter (malaoxon, paraoxon, leptophosoxon, and diazoxon).
1(0,0,0,1) Details
6205472 Hoffman DJ, Sileo L, Murray HC: Subchronic organophosphorus ester-induced delayed neurotoxicity in mallards. Toxicol Appl Pharmacol. 1984 Aug;75(1):128-36.

Brain acetylcholinesterase, plasma cholinesterase, and plasma alkaline phosphatase were significantly inhibited as well.
Additional ducks were exposed in a similar manner to 60-, 270-, or 540-ppm leptophos (phosphonothioic acid O-4-bromo-2,5-dichlorophenyl-O-methylphenyl ester) which resulted in similar behavioral, biochemical, and histopathological alterations.
1(0,0,0,1) Details
56273 Freed VH, Matin MA, Fang SC, Kar PP: Role of striatal dopamine in delayed neurotoxic effects of organophosphorus compounds. Eur J Pharmacol. 1976 Jan;35(1):229-32.

Treatment with Leptophos for the same period produced slight motor dysfunction and a small but significant reduction in the level of striatal dopamine.
The cholinesterase activity of corpus striatum was inhibited by all the compounds.
1(0,0,0,1) Details
6169754 El-Sebae AH, Soliman SA, Ahmed NS, Curley A: Biochemical interaction of six OP delayed neurotoxicants with several neurotargets. J Environ Sci Health B. 1981;16(4):465-74.

Five organophosphorous insecticides: Leptophos, EPN, Cyanofenphos, trichloronate and salithion proved to cause irreversible ataxia not only to chicken but also to mice and sheep.
The six compounds and their oxons were screened for their in-vitro inhibition to monamine oxidase (MAO), acetyl cholinesterase (AChE) and neurotoxic esterase (NTE) in the brain of either mouse, lamb or chicken.
1(0,0,0,1) Details