http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=16392809&query_hl=7&itool=pubmed_docsum
J Med Chem. 2006 Jan 12;49(1):246-55.
Analogues with fluorescent leaving groups
for screening and selection of enzymes that efficiently hydrolyze
organophosphorus nerve agents.
Briseno-Roa L, Hill J, Notman S, Sellers
D, Smith AP, Timperley CM, Wetherell J, Williams NH, Williams
GR, Fersht AR, Griffiths AD.
Medical Research Council Centre for Protein Engineering, Hills
Road, Cambridge, CB2 2QH, UK.
Enzymes that efficiently hydrolyze highly toxic organophosphorus
nerve agents could potentially be used as medical countermeasures.
As sufficiently active enzymes are currently unknown, we synthesized
twelve fluorogenic analogues of organophosphorus nerve agents
with the 3-chloro-7-oxy-4-methylcoumarin leaving group as probes
for high-throughput enzyme screening. This set included analogues
of the pesticides paraoxon, parathion, and dimefox,
and the nerve agents DFP, tabun, sarin, cyclosarin, soman, VX,
and Russian-VX. Data from inhibition of acetylcholinesterase,
in vivo toxicity tests of a representative analogue (cyclosarin),
and kinetic studies with phosphotriesterase (PTE) from Pseudomonas
diminuta, and a mammalian serum paraoxonase (PON1), confirmed
that the analogues mimic the parent nerve agents effectively.
They are suitable tools for high-throughput screens for the directed
evolution of efficient nerve agent organophosphatases.
PMID: 16392809 [PubMed - in process]
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=16392809&query_hl=7&itool=pubmed_docsum
J Med Chem. 2006 Jan 12;49(1):246-55.
Analogues with fluorescent leaving groups
for screening and selection of enzymes that efficiently hydrolyze
organophosphorus nerve agents.
Briseno-Roa L, Hill J, Notman S, Sellers
D, Smith AP, Timperley CM, Wetherell J, Williams NH, Williams
GR, Fersht AR, Griffiths AD.
Medical Research Council Centre for Protein Engineering, Hills
Road, Cambridge, CB2 2QH, UK.
Enzymes that efficiently hydrolyze highly toxic organophosphorus
nerve agents could potentially be used as medical countermeasures.
As sufficiently active enzymes are currently unknown, we synthesized
twelve fluorogenic analogues of organophosphorus nerve agents
with the 3-chloro-7-oxy-4-methylcoumarin leaving group as probes
for high-throughput enzyme screening. This set included analogues
of the pesticides paraoxon, parathion, and dimefox,
and the nerve agents DFP, tabun, sarin, cyclosarin, soman, VX,
and Russian-VX. Data from inhibition of acetylcholinesterase,
in vivo toxicity tests of a representative analogue (cyclosarin),
and kinetic studies with phosphotriesterase (PTE) from Pseudomonas
diminuta, and a mammalian serum paraoxonase (PON1), confirmed
that the analogues mimic the parent nerve agents effectively.
They are suitable tools for high-throughput screens for the directed
evolution of efficient nerve agent organophosphatases.
PMID: 16392809 [PubMed - in process]
TOXICOLOGY AND INDUSTRIAL
HEALTH; 15 (1-2). 1999. 119-132.
Immunotoxicity
of pesticides: A review.
VOCCIA
I, BLAKLEY B, BROUSSEAU P, FOURNIER M
INRS-Sante, 245 Boulevard
Hymus, Pointe-Claire, Quebec, H9R 1G6, Canada.
The intricate balance
that is the hallmark of the immune system shows vulnerability
to any chemical, including pesticides, that can cause structural
and functional alterations to the system. The immunotoxic effects
of xenobiotics include: histopathologic effects in immune tissues
and organs; cellular pathology; altered maturation of immunocompetent
cells; changes in B and T cell subpopulations; and functional
alterations of immunocompetent cells. Pesticides, including fungicides,
herbicides, and
ZHONGGUO YAOLIXUE YU DULIXUE
ZAZHI; 11 (4). 1997. 291-293.
Mutagenicity
of 19 organophosphorus pesticides in Saccharomyces cerevisiae
D61.M.
SONG
XIAO-OU LIN FAN JIANG YOU-CHUN LIU XIAO-RONG ZHANG PEI-HOU LIU
YU-QING
Res. Lab. Toxicol.,
West China Univ. Med. Sci., Chengdu 610041, China.
Mutagenicity of 19
organophosphorus pesticides (OPP) was tested by yeast system,
Saccharomyces cerevisiae D61.M. The results were compared with
those tested by other mutagenicity assays in our laboratory. 89.5%
(17/19) of the OPP tested were positive in D61.M system. It suggested
that most OPP might be potential aneuploidogens. Fourteen OPP
were positive both in D61.M and either micronucleus test (in vitro
or in vivo), that these OPP may possess aneuploidizing effect
singly, or both aneuploidizing and clastogenic effects concurrently.
Only 2 OPP, ethion and disulfoton, were positive in micronucleus
test singly but negative in D61.M, thus suggested only 2 few OPP
might possess clastogenic effect singly. Nevertheless, it is the
first time to show rigidly aneuploidizing effect in OPP. As comparing
results from mouse and CHL cell micronucleus tests, it was found
that the differences of the metabolic deactivating activity for
dealkylation besides deethylation among the mouse
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7968576&dopt=Abstract
Mutagenesis. 1994
Jul;9(4):341-6.
The w/w+
SMART is a useful tool for the evaluation of pesticides.
Aguirrezabalaga
I, Santamaria I, Comendador MA.
Departamento de Biologia
Funcional, Facultad de Medicina, Universidad de Oviedo, Spain.
Genotype-dependent
variability in the response of several Drosophila strains to hexamethylphosphoramide
(HMPA) has been studied using the white/white+ (w/w+) somatic
mutation and recombination test (SMART). Among the tester strains,
there were three wild-type laboratory strains (Leiden-S, Oregon-K
and 91-C) and three insecticide-resistant strains (Haag-79, Hikone-R
and 91-R). The response to HMPA of larvae from a cross between
two wild-type strains (Leiden-S and Berlin-K) was also measured.
The strains have been evaluated in terms of spontaneous frequencies
of mosaic eyes, lowest effective dose and dose-response relationship.
Strong variability was found among the strains, the best performance
to HMPA being obtained with the strain Oregon-K. In addition,
a series of pesticides structurally related to HMPA, such as dimefox,
hexamethylmelamine, hexazinone, alachlor, CAM, pirimicarb, dimetilan,
thiram and methabenzthiazuron have been tested with the Oregon-K
strain. Some of these pesticides had already been shown to be
genotoxic in other systems, whereas others have either not been
tested or gave negative results in in vitro systems. Although
genotoxicity was expressed only within a narrow dose range, all
pesticides were genotoxic in the w/w+ system with the Oregon-K
strain. Thus, these compounds may be a genotoxic hazard
to man. These results suggest the suitability of the strain Oregon-K
for genotoxicity testing with the w/w+ eye mosaic system, although
more information about the performance of this strain with other
compounds must be obtained.(ABSTRACT TRUNCATED AT 250 WORDS)
PMID: 7968576
[PubMed - indexed for MEDLINE]
Hua Hsi I Ko Ta Hsueh
Hsueh Pao 1993 Mar;24(1):82-6
[Induction
of micronucleus by organophosphorus pesticides both in vivo and
in vitro]
Ni
Z, Li S, Liu Y, Tang Y, Pang D
English Abstract Indicator:
A Abstract: A total of 22 organophosphorus pesticides (OPPs),
including 8 ethyl-, 9 methyl-, and 5 other OPPs, were tested for
mutagenicity in micronucleus assay system both in 615 mouse marrow
cells in vivo with multi-intraperitoneal administrations and in
cultured Chinese hamster lung (CHL) cells in vitro; and structure-mutagenicity
relationship of OPPs was analyzed. Among the OPPs tested in vivo,
5 ethyl-(diazinon, chlorpyrifos, disulfoton, ethion, and parathion),
and only 1 methyl-(dimethoate) were found mutagenic, while the
other OPPs were negative. Six ethyl- (azinphos ethyl, chlorpyrifos,
ethion, parathion, phosaione, and quinaphos), 8 methyl- (azinophos
methyl, chlorpyrifos methyl, dichlorvos, dimethoate, fenitrothion,
malathion, parathion methyl, and trimethyl phosphate), and 2 other
OPPs (EII and MIA), however, induced micronucleus in CHL cells
in vitro. The results indicated that most of the ethyl-OPPs tested
showed the ability to induce micronucleus both in vivo and in
vitro, and that most of the methyl-OPPs were positive only in
vitro. The mechanism for the adversity of mutagenic activity in
micronucleus assay in vivo and in vitro produced by different
kinds of OPPs was also discussed.
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7170026&dopt=Abstract
Neurobehav Toxicol
Teratol. 1982 Nov-Dec;4(6):665-9.
Effect
of pesticides on central and peripheral nervous system function
in rats.
Lehotzky
K.
The neurobehavioral
toxicity of three organophosphate pesticides, sumithion, dimefox
and trichlorphon, was evaluated in rats using measures of open
field activity, rotorod performance, conditioned escape from shock,
and nerve conduction velocity. These measures were correlated
with blood and brain cholinesterase level determinations. All
three chemicals disrupted behavior ranging from transient disruptions
accompanied by alterations in nerve conduction to disruption throughout
the exposure. Even in the case of prolonged behavioral
disruption, however, some recovery of performance occurred. Cholinesterase
in both blood and brain decreased with initial dosing and remained
low with continued dosing regardless of changes in the behavioral
measures. The results are discussed in terms of the necessity
of using mammalian behavioral tests to determine the toxicity
of organophosphorous compounds in order to safeguard the health
of the human population.
PMID: 7170026
[PubMed - indexed for MEDLINE]
•
The abstracts, above and below, are for the same paper
Neurobehavioral
Toxicology and Teratology, Vol. 4, No. 6, pages 665-669, 18 references,
1982
Effect
Of Pesticides On Central And Peripheral Nervous System Function
In Rats
Lehotzky
K
Abstract: The neurobehavioral
toxicity of the organophosphate pesticides sumithion (122145),
dimefox (115264), and trichlorphon
(52686) was evaluated in rats. Rats were administered perorally
10 milligrams per kilogram per day (mg/kg/day) sumithion, 0.25mg/kg/day
dimefox, or 12.5mg/kg/day trichlorphon. Behavioral activities
were monitored. Open field activity was measured in an area measuring
20 by 20 centimeters and consisting of 24 squares. Conditioned
escape from an electric foot shock of 1.8 milliAngstroms, rotorod
performance through a pole connected with a spring, and learning
ability through an unconditioned stimulus such as a bell were
also measured. Acetylcholinesterase activity in blood and brain
were also measured. Sumithion treated rats showed a mild increase
in both rearing and grooming but no signs of incoordinated locomotion
in the open field activity. Dimefox treated
animals showed about a 40 percent increase in rearing and grooming
activities; trichlorphon caused only a transient increase.
In the conditioned reflex activities, sumithion treated rats extinguished
more rapidly than controls, dimefox treated
rats showed normal reflexes but with slower extinction than controls,
and trichlorphon treated rats were able to acquire the
conditioned escape reflex but the latency period of the escape
responses increased significantly. In rotorod performance, rats
treated with sumithion showed a decline, whereas the dimefox
treated group showed an initial jump but failed to fall down.
The trichlorphon treated group showed only a transient
decline. A similar pattern of results was obtained with regard
to learning ability for all three pesticides. Acetylcholinesterase
activity decreased significantly in the case of dimefox and
sumithion, but activity did not correlate with the dose; trichlorphon
was inactive with respect to this enzyme. The author concludes
that experiments with animals are necessary to understand poisoning
in humans due to these pesticides.
SATELLITE SYMPOSIUM ON
ENVIRONMENTAL NEUROTOXICOLOGY: ASSESSMENT OF NERVOUS SYSTEM AND
BEHAVIORAL DYSFUNCTION HELD AT THE 1ST WORLD CONGRESS OF THE INTERNATIONAL
BRAIN RESEARCH ORGANIZATION, DUSSELDORF, MARCH 29-31, 1982.
NEUROBEHAV TOXICOL TERATOL; 4 (6). 1982
(RECD. 1983). 665-670.
EFFECT
OF PESTICIDES ON CENTRAL AND PERIPHERAL NERVOUS SYSTEM FUNCTION
IN RATS
LEHOTZKY
K
Abstract: HEEP COPYRIGHT:
BIOL ABS. RRM HUMAN RISK BLOOD BRAIN CHOLIN ESTERASE ORGANO PHOSPHATES
DIMEFLOX SUMITHION TRICHLORPHON OPEN FIELD ACTIVITY ROTOROD PERFORMANCE
SHOCK CONDITIONED ESCAPE
CAS Registry Numbers:
122-14-5
122-14-5
115-26-4
52-68-6
Agrochemia 20(3):
84-85 1980 (4 References)
Evaluation
of rodenticides certified in the CSSR and the prospect for new
preparations.
Vanurova
E
Ukzuz-okor, Brno, Czechoslovakia
Abstract: PESTAB.
Stringent requirements for the use of rodenticides to control
Microtus arvalis in Czechoslovakia are given. High toxicity to
the pest, safety for humans, non-target insects, wildlife and
myophages, and rapid decomposition must be demonstrated before
rodenticides can be used. Endrin is the only rodenticide certified
in Czechoslovakia for use as a surface spray. The rodenticidal
effects of scilliroside, endosulfan, camphechlor (toxaphene) and
carbofuran, and the prospects of monocrotofos (Nuvacron 40 WSC,
Ciba-Geigy), are considered. Phosphine, baits, modes of application,
and the mechanized spreading of rodenticides are presented. The
Czechoslovakian products Stutox and grazin, the imported products
Arrex M Koeder klein and Castrix Pellets (crimidine), and preparations
based on dimefox, Delicia (aluminum
phosphide) chlorphacinone granules, difenacoum and brodifacoum
are also discussed.
CAS Registry Numbers:
535-89-7
535-89-7
115-26-4
20859-73-8
3691-35-8
Pharmacol. Ther.
Part A 6(3): 579-628 1979 (114 References)
Mode
of action
of anticholinesterases.
Main
AR
Dep. Biochem., North
Carolina State Univ., Raleigh, NC 27650
Abstract: PESTAB. Organophosphate
and carbamate insecticides achieve their effects primarily as
nerve poisons by inhibiting cholinesterase (ChE) activity. In
this review the classification and substrate specificities of
various ChEs, the reactive sites of ChEs, and kinetics of inhibition
by compounds such as paraoxon, malaoxon, DFP, amiton, parathion,
TEPP, diazinon, fenthion, trichlorofon, fonofos, dimefox,
carbaryl, aldicarb, carbofuran, pirimicarb, and mobam are discussed.
Egeszsegtudomany
22(3): 253-259 1978
(31 References)
Effect
of dimefox on the nerve conduction velocity and cholinesterase
activity in rats.
Lehotzky
K, Szeberenyi J, Ungvary Gy
Munic. & County Public
Health Inst., Budapest, Hungary
Abstract: PESTAB. The
effect of Terra systam (dimefox, acute oral
LD50 in rats: 5.59 mg/kg) on the motor conduction velocity
(MCV) of the tail nerve and on whole-body cholinesterase activity
was studied in rats in acute (2.8 mg/kd po) and subacute (0.10
and 0.25 mg/kg/day) poisoning tests for 6 wk.
In the acute posioning tests, dimefox caused dose-dependent cholinesterase
inhibition; it developed rapidly, and persisted for a fairly long
time. The MCV showed an over 50% decrease 24 hr after poisoning;
this decrease was accompanied by a marked elevation of the stimulus
threshold. The animals were symptom-free in the subacute experiments,
but the whole-blood cholinesterase activity
was inhibited by about 40% in the animals treated with 0.10 mg/kg/day
doses, and by about 70% in those treated with 0.25 mg/kg/day doses.
The inhibition rate was totally independent of the total
dose administered. The MCV was significantly reduced in both groups,
but the stimulus threshold of the evoked muscular potential remained
unchanged. The light and electron micrograms of the sciatic nerve
showed no difference from the control. The cause and mechanism
of the change in the MCV is yet unknown.
Khim. Sel'sk Khoz. (1):
54-64 1978 (39 References)
Metabolism
of organophosphate pesticides.
Rozengart
VI
I. M. Sechenov Inst.
Evol. Physiol. Biochem., USSR Acad. Sci., Yalta, USSR
Abstract: PESTAB. Studies
on the metabolism of organophosphorus pesticides in insects and
higher animals are reviewed. Hydrolytic splitting, catalyzed by
hydrolases, includes the hydrolysis of bonds at the phosphorus
atom or in the phosphoryl part of the molecule (catalyzed by phosphatases),
the carboxyester bond (catalyzed by carboxy esterases), of the
carboxyamide bond (catalyzed by carboxy amidases), and of the
N-alkyl bond. Hydrolysis leads to detoxification in most cases.
Dimethoate, trichlorfon, malathion, dimefox,
crufomate, acethion, and phosphamidon are decomposed according
to this mechanism. The transfer of alkyl and aryl groups, catalyzed
by transferases, is another possible metabolic pathway leading
to detoxification. The redox conversions, catalyzed by oxido reductases,
include such processes as oxidative desulfurization, oxidation
of alkyl groups, thioether groups, oxidative O-dearylation, O-dealkylation,
N-dealkylation and reduction of the nitro group. Such conversions
are typical for tricresylphosphate and o-cresyl- phosphate analogs,
disyston and dicrotophos. Trichlorfon and dibrom can degrade through
non-enzymatic dehydrohalogenation.
MUTAT RES 38:136-137,1976
FORMATION
OF DIMETHYLNITROSAMINE FROM CHLOROXURON, CYCLURON, DIMEFOX AND
THIRAM IN THE PRESENCE OF NITRITE
EGERT
G, GREIM H
No
abstract available
Food Cosmet. Toxicol.
14(3): 193-195; 1976. (18 references)
Formation
of dimethylnitrosamine from pesticides carrying methylated tertiary
aminogroups in the presence of nitrite at pH 3.
Egert
G, Greim H
Pesticides and nitrite
present in human food may be a hazard to man, since many pesticides
are secondary or tertiary amines, which are known to form nitroso
compounds in the presence of nitrite under conditions resembling
those in the human stomach. Four tertiary amine pesticidesštwo
dimethylurea derivatives, one thiuram disulphide, and one phosphine
compoundšwere incubated for 4 hr at 37DEG C in the presence of
excess nitrite at pH 3. The reaction products were extracted with
dichloromethane and were analyzed qualitatively and quantitatively
by infrared spectrophotometry, nuclear magnetic resonance spectrometry,
gas chromatographyšmass spectrometry, and light spectrometry.
All four pesticides formed carcinogenic
dimethylnitrosamine, the yields obtained being cycluron
4%, chloroxuron 3%, thiram 9%, and dimefox
22%. (Author abstract by permission)
Int. Pest Control16(6):
4-9; 1974 (REF:45)
Organophosphorus
insecticides.
Cremlyn
RJW
Abstract: PESTAB.
The article reviews the main types of organophosphorus insecticides.
Early examples such as dimefox, tabun,
sarin, pestox, and parathion had
the disadvantage of high mammalian toxicity. Sumithion, which
has a similar insecticidal spectrum to parathion, has a lower
toxicity. A larger number of phosphorothioates have been developed
which combine good insecticidal properties with very low mammalian
toxicity, such as bromophos. Generally, the systox group, including
systox, metasystox, or demetonmethyl, have fairly high mammalian
toxicities and protective clothing is required when using these
chemicals. Phorate, or Thimet is also a systemic insecticide with
high mammalian toxicity. Malathion, developed in 1950, is an important
and widely used contact insecticide and acaricide with remarkably
low mammalian toxicity. Another important series of insecticides
contains alkene double bonds such as dichlorvos. Mevinphos or
phosdrin has replaced tetraethyl pyrophosphate as a contact insecticide
where a rapid kill of a pest is required close to harvest. Though
mevinphos is highly toxic, it is rapidly hydrolyzed in plants
to non-toxic materials so that only 3 days are needed between
the last application and harvesting of edible crops. One group
of organophosphorus insecticides is obtained by combination with
heterocyclic compounds, including menazon, and derivatives of
phthalidide, benzotriazole, quanizolone, pyridines, quinolines,
thiazoles, thiadiazoles, and diazines. Gusathion was one of the
more active members of this series. Diazinon is another example.
Another type of organophosphorus insecticide is the N-methylcarbamoyl
derivative, dimethoate or Rogor. Dimethoate has a moderate mammalian
toxicity and is not absorbed by the oily phase and thus has good
residual properties. The insecticidal activity of a given organophosphorus
compound is primarily related to its ability to phosphorylate
cholinesterase, which in turn should be generally indicated by
its reactivity as a phosphorylating agent for simple hydroxylic
substrates. Still some very closely related compound exhibit markedly
different activity, thus it is still necessary to synthesize a
large number of analogous compounds and determine the optimum
insecticide by trial and error. Potential advantages, selectively
and toxicity of organophosphorus
insecticides is briefly discussed.
Pestic. Sci.5(5): 549-554;
1974 (REF:4)
Uptake
and translocation
of dimefox and schradan in hops.
Dejonchkeere
W, Steurbaut W, Dynoodt R, Kips RH
Abstract: PESTAB.
During the 1971 growing season an experiment was carried out to
study the uptake, translocation and residue levels of dimefox
and schradan in hops after applying a soil drench of Terra-Sytam
(222 g/litre dimefoxš20 g/liter schradan) at various times in
varying concentrations. Residue analysis shows that the dimefox
concentration in the hop plants reaches a peak about one week
after application, which increases with the amount applied. Then
a gradual breakdown sets in so that at the time of harvesting
the differences between the dosages have virtually disappeared.
Translocation of dimefox in the hop plant is very rapid, but the
breakdown is faster at the top of the plant. Schradan concentrations
were usually very low and residues at harvest time negligible.
(Author abstract by permission)
RESIDUE REV; 46. 1973
1-240
THE PROBLEM
OF RESIDUES IN MEAT OF EDIBLE DOMESTIC ANIMALS AFTER APPLICATION
OR INTAKE OF ORGANOPHOSPHATE ESTERS.
KAEMMERER
K, BUNTENKOETTER S
Abstract: HEEP COPYRIGHT:
BIOL ABS. HUMAN PESTICIDE INSECTICIDE LEGISLATION
Int. Dig. Health Leg.;
17(1): 180-181, 1966
CONTROL
OF THE MANUFACTURE OF AND TRADE IN POISONS
ANON
Abstract: HAPAB A
Yugoslavian decree of April 4, 1965, summarizes the laws pertaining
to production of and trade in poisons; from the Official List
of April 6, 1965, No. 16, Serial No. 342, pp. 781-783. Storage,
packaging, labeling, and sale to authorized persons of poisons
( including aldrin, dimefox, endrin,
methyl parathion, schradan, chlordane, lindane, etc. ) are mentioned.
GENERAL 66/10/00, 2 1966
CAS Registry Numbers:
57-74-9
58-89-9
72-20-8
115-26-4
152-16-9
298-00-0
309-00-2
Food and Cosmetics Toxicology,
Vol. 2, pages 311-316, 1964
Summaries
of Toxicological Data. No-Effect Levels of Three Organophosphates
in the Rat, Pig and Man
Edson
EF
Abstract: The toxicological
effects of schradan (152169), dimefox
(115264), and parathion (56382) were investigated in rats, pigs,
and humans. Schradan was given to rats on diet at concentrations
from 0.05 to 5.0 parts per million (ppm) or by intraperitoneal
(ip) injection of 0.007 to 2.5 milligrams per kilogram (mg/kg).
Pigs were fed 0.1 to 2.5ppm in diet. Human
subjects were given 1.4mg 5 days per week to a total of 44mg.
Brain and plasma cholinesterase (ChE) were determined in animals.
Blood ChE was determined in humans. Rats
were fed 0.01 to 5.0ppm dimefox in diets for 28 to 287 days.
Pigs received 0.005 to 0.5ppm for 133 days. Humans
were given oral doses of 0.0014mg/kg for 14 days, then 0.004mg/kg
for 95 days, or 0.0012, 0.002, or 0.0034mg/kg for 70 days.
Inhibition of ChE was determined. For parathion, rats were fed
0.05, 0.5, or 5.0ppm in diet for 84 days. Pigs were fed 0.02 to
100ppm in increasing doses from 33 to 122 days. Humans received
oral doses of 0.6mg per day until week 4, then increased to 4.8mg
to week 13; 7.2mg for 6 weeks; or 1.2 or 2.4mg for 25 to 70 weeks.
ChE inhibition was determined. The no effect concentrations were
determined for each of the compounds. For schradan, the no effect
dose was 0.02mg/kg per day for rats and pigs. In man, 3ppm presented
no hazard. Based on changes in red cell
ChE, the no effect concentrations of dimefox were 0.003, 0.006,
and 0.002mg/kg per day for rat, pig, and man, respectively.
Obvious ill effects or illness in man would occur at about 100
times that concentration. The no effect dose of parathion was
estimated as 0.002mg/kg per day in rats, 1.0mg/kg per day in pigs,
and 0.05mg/kg per day for humans. A 60kg adult could consume 3mg
per day of parathion, or 1kg containing 3ppm with no ChE depression.
The author concludes that the doses used cause, at most, slight
and fully reversible physiological effects.
TOXICOL APPL PHARMACOL
13:1-15,1968
CHICK AND
DUCK EMBRYOS IN THE EVALUATION OF PESTICIDE TOXICITY
KHERA
KS, LYON DA
Name of Agent (CAS
RN):
PHOSDRIN ( 7786-34-7 )
2,2-DICHLOROVINYL DIMETHYL PHOSPHATE ( 62-73-7 )
RUELENE ( 299-86-5 )
DIMEFOX ( 115-26-4 )
DIAZINON ( 333-41-5 )
PARATHION ( 56-38-2 )
MALATHION ( 121-75-5 )
TRITHION ( 786-19-6 )
DIMETHOATE ( 60-51-5 )
ETHION ( 563-12-2 )
CARBARYL ( 63-25-2 )
BAYER 37344 ( 2032-65-7 )
BAYER 39007 ( 114-26-1 )
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=5650527&dopt=Abstract
J Chromatogr. 1968
May 7;34(4):558-9.
No
Abstract available
Ninhydrin
reaction used for thin-layer chromatographic detection of bis(dimethylamino)fluorophosphine
oxide (dimefox).
Coha
F.
PMID: 5650527
[PubMed - indexed for MEDLINE]
http://www.ncbi.nlm.nih.gov:80/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=4391585&dopt=Abstract
Z Naturforsch B.
1969 Dec;24(12):1605-9.
No
Abstract available
[The utilization
of 32P-labelled Dimefox]
[Article in German]
Koch
H, Abendroth HC, Jeske A.
PMID: 4391585
[PubMed - indexed for MEDLINE]
• See
full paper
The Conversion of Dimefox into an Anticholinesterase
by Rat Liver in vitro
BY M. L. FENWICK*, JANE R. BARRON AND W.
A. WATSON
Fisons Pest Control Ltd., Chesterford Park Research Station,
Saffron Walden, Essex
* Department of Biochemistry, 9 Hyde Terrace, The University,
Leeds, 2.
This paper presents further studies on the mode of action and
metabolism of dimefox in mammals. The work was undertaken as part
of a progranmme of investigation of the toxicology of dimefox,
the systemic insecticidal properties of which are utilized to
combat insect infestation on hops, sugar
beet and other crops.
