Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Isoflurophate”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources
PubMed1979

Separation and spectral properties of diisopropylphosphate, the major decomposition product of isoflurophate.

The reaction of water with isoflurophate to form diisopropylphosphate was examined and confirmed. Isolation of this decomposition product from an antiglaucoma drug formulation is described. A known reference compound was isolated from a commercial mixture also containing the monoisopropyl ester. The isolation, purification, and molecular spectroscopic and elemental confirmation of structure are described. IR, NMR, and mass spectra are included. Additionally, a GLC procedure and parameters used to identify diisopropylphosphate in a degraded peanut oil formulation of isofluorphate are reported. Reaction mixtures of this drug with water and sodium hydroxide were analyzed by GLC with the expected results.

Chromatography, Gas↗
PubMed1977

Acetylcholinesterase staining in subdivisions of the cat's inferior olive.

The present paper describes a unique distribution of true AChE activity in the IO. In the dorsal accessory olive three areas with high AChE activity can be distinguished. The medial accessory olive can be subdivided into a caudal part which shows rostro-caudally directed bands with different enzymatic activity, and a rostral part which shows a more uniform, medium activity. In the nucleus beta and the dorso-medial cell column, AChE activity is low. The ventral and dorsal lamellae of the principal olive contain areas with high, medium, and low activity. The dorsal cap is strongly positive, while the ventrolateral outgrowth is negative for AChE. Enzyme distribution cannot be fully explained on the base of the known afferent and efferent connections with the IO. However, histochemical results provide evidence that generally supports a subdivision of the IO that mirrors these connections (Brodal, '40; Armstrong et al., '74' Boesten and Voogd, '75; Groenewegen et al., '75).

Acetylcholinesterase↗
PubMed1976

Biological responsiveness to cholinesterase inhibition: a test for exploring the developmental maturity of the cholinergic system.

The acute mortality caused by two irreversible inhibitors of cholinesterases [diisopropylfluorophosphate (DFP) and diethoxyphosphorylthiocholine, 217 MI-phospholine iodide] has been investigated on chick embryos at different stages of development. The results demonstrate that the above compounds do not show any acute lethal action when administered before the 9th day of incubation; on the other hand, the administration is regularly followed by death after the 9th day of incubation. The doses are comparable to those causing death in hatched chicks. It has also been observed that no appreciable difference exists in DFP uptake from the yolk before and after the 9th day of incubation and that drug-induced cholinesterase inhibition is of the same order of magnitude at any developmental stage; the compound pyridine-2-aldoxime methanesulfonate (2-PAM) was a good antidote against DFP acute lethality. It seems likely that between the 8th and the 9th day of incubation the target system of organophosphorus inhibitors, that is, the cholinesterase enzymatic system, reaches a new point of maturation.

Animals↗
PubMed1977

Cholinergic involvement in cobalt-induced epilepsy in the rat.

In rats with cobalt implanted in the right frontal cerebral cortex, acetylcholine (ACh) levels were depressed in the visually non-necotic, surrounding cortex at 7 and 14 days after surgery in comparison with values for controls treated with glass. At 21 days post-implantation, ACh levels were not different for glass and cobalt treatments. Effects of drugs affecting cholinergic function on electro-corticographic (ECoG) epileptiform activity were determined in rats implanted bilaterally with cobalt. The cholinesterase inhibitors, physostigmine and diisopropylfluorophosphate reduced both seizure activity and interictal spiking in these cobalt-treated rats. Hemicholinium-3 (HC-3), given subacutely initially inhibited seizures, but seizure frequency increased later during treatment. HC-3 did not appear to inhibit interictal spiking. These results suggest an involvement of brain cholinergic system in chronic cobalt experimental epilepsy. Seven days after cobalt implantation, HC-3 was less effective in depleting ACh in cerebral cortex adjacent to the cobalt-lesion than in similar tissue from rats with no cobalt implants. This suggests that the cholinergic neurons adjacent to the implant are not highly active at a time when seizure frequency is maximal.

Acetylcholine↗
PubMed1977

Improved assay of neurotoxic esterase for screening organophosphates for delayed neurotoxicity potential.

The assay of neurotoxic esterase (NTE) in brains taken from dosed hens enables potential neurotoxicity of organophosphate pesticides, plasticers, etc. to be assessed. The original assay [Johnson, M.K. Biochem. J. 114, 711-717 (1969)] has been simplified to eliminate centrifugation and transfer steps and both the selectivity and the sensitivity have been increased. The procedures necessary to obtain stable reagent stocks are described.

Animals↗
PubMed1978

The anomalous behaviour of dimethyl phosphates in the biochemical test for delayed neurotoxicity.

Several dimethyl phosphate behave anomalously in tests for delayed neurotoxicity. Doses given to hens caused high inhibition of brain neurotoxic esterase (NTE) but no ataxia. Less inhibition of NTE was seen in spinal cord than in brain. Di-isopropyl phosphorofluoridate caused equal inhibition of NTE in brain and cord. When dosing with dimethyl phosphates was repeated NTE inhibition in cord increased and pair-dosed birds became ataxic. In vitro brain and cord NTE were indistinguishable but the in vivo discrepancy between inhibition of brain and cord NTE was matched by a similar discrepancy in inhibition of AChE. It appears that ataxia arises from inhibition of spinal cord NTE and that only in the present cases (among about 200) was the effect in brain not a perfect biochemical monitor.

Animals↗
PubMed1976

Therapeutic effects of some cholinolytics in organophosphate intoxications.

The therapeutic effects of pipethanate (sycotrol) and two newly synthetized cholinolytics, DPX-8 and ANC-51, were compared with atropine in mice poisoned by DDVP, fluostigmine, phospholine, and paraoxon. The antagonistic activotagonistic activity of tested drugs against acetylcholine-induced contraction of rat ileum and oxotremorine-induced salivation and tremor in the mouse was also studied. The anticholinergic activity of pipethanate, DPX-8, and ANC-51 was weaker than that of atropine. However,the therapeutic effect of pipethanate was higher than that of atropine in mice poisoned by the organophosphates. DPX-8 and ANC-51 afforded a better antidotal effect than atropine only in DDVP-poisoned mice.

Animals↗
PubMed1979

Human serum and epithelial spread in tissue culture.

The dependence of epithelial spread on human serum in culture has been studied. Using measured pieces of mouse ear skin epithelial outgrowth about floating explants (epiboly) and from adherent explants was studied. Where compared directly the two systems show similar results. Because of its ease of quantitation, the adherent explant culture was studied in greater detail. In this system in the presence of serum appreciable spread was found only after 48 h but spread continued for at least the next 4 days. In the absence of serum only minimal epithelial spread occurred. Adding serum to deficient media enhanced spreading and removing serum from media depressed spreading. The extent of spread appeared independent of mouse age for the first 4-10 weeks though 2-week-old mouse skin showed quantitatively greater spreading. The activity in human serum responsible for epithelial spread acts under conditions of minimal DNA synthesis and is not reproduced by bovine serum albumin, fetuin, or serum that had been exposed to 100 degrees C for 5 min. The activity is not dialyzable and it is resistant to the protease inhibitors DFP and PMSF. These studies suggest that a specific serum component(s) serves to support epithelial spread in vitro.

Age Factors↗
PubMed1977

Development and disappearance of subsensitivity to pilocarpine following a single administration of the irreversible anticholinesterase angent, DFP.

The present study examined the possibility that subsensitivity to pilocarpine might occur following a single injection of the irreversible anticholinesterase agent, DFP. In one experiment male Sprague-Dawley rats were trained to drink from experimental drinking chambers for 1/2 h per day. After establishment of baselines, pilocarpine hydrochloride (8 mg/kg) was injected i.p. 5 min before the drinking session. One week later DFP or the arachis oil vehicle (1 mg/kg) was injected intramuscularly and injections of pilocarpine were given at varying times thereafter. The suppression of water intake by this dose of pilocarpine was unaffected by pretreatment with arachis oil, but was markedly attenuated by pretreatment with DFP. This subsensitivity was first observed on the second day but had largely disappeared by the 14th day. DFP was found to have comparable effects on water intake and brain acetylcholinesterase activity when the injections were separated by 20 days. In a second experiment the hypothermic effects of pilocarpine were found to be reduced in rats acutely treated with DFP. These data establish that subsensitivity to pilocarpine occurs following a single administration of DFP. This subsensitivity could reflect a reduced sensitivity of postsynaptic receptors to acetylcholine, which may partially account for the behavioural recovery of the rats while acetylcholinesterase activity is still markedly depressed.

Acetylcholinesterase↗
PubMed1979

Development of behavioral tolerance: a search for subcellular mechanisms.

Development of behavioral tolerance is one of the processes by which living organisms adjust to changes in their internal and external environments. The search for neurochemical mechanisms underlying such processes requires the testing of many hypotheses. The present study was designed to examine the possible involvement of certain subcellular events. The concentrations of acetylcholine (ACh) and choline (Ch), the high-affinity transport of Ch, and the rate of synthesis of ACh were measured in synaptosomes prepared from the brains of rats. The assays were made at critical times during the acute changes in behavior induced by administration of the anticholinesterase, di-isopropylfluorophosphate, and during the development of behavioral tolerance to this compound as chronicity of administration continued. No statistically significant differences were found among treatment groups in the total concentration of ACh or Ch, the synthesis of ACh, or the high-affinity transport of Ch. These results, plus evidence from previous experiments, indicate that the development of behavioral tolerance does not relate to the factors studied. Consequently, alternative mechanisms should be considered. In addition to changes in cholinergic (muscarinic) receptors already shown to occur concomitantly with the development of behavioral tolerance, it is suggested that the possible involvement of mechanisms controlling release of ACh should be studied.

Acetylcholine↗
PubMed1977

Expression of esterases during ontogenesis of the flour beetle Tribolium castaneum (Tenebrionidae; Coleoptera).

Two electrophoretically fast-migrating, nonspecific esterases were detected in two strains of the flour beetle Tribolium castaneum and designated F (fast) and S (slow) according to their relative migration distances. Both isozymes are associated with the alimentary canal and display ontogenetic changes. Their activity is very low in the egg stage, increases in the larva, and declines dramatically in the pharate pupa and pupa. The overall activity in the pupal stage is low, yet increases gradually throughout this period. In the adult, the activity of the esterases rises sharply. The larval and adult F and S isozymes were found to hydrolyze alpha- and beta-naphthylacetate and alpha-naphthylpropionate with almost equal capacity. alpha-Naphthyl laurate was cleaved by the F enzyme of both larvae and adults. The F and S were insensitive to inhibitors of arylesterases and cholinesterases and were markedly inhibited by the organophosphate di-isopropylphosphorofluoridate (DFP) and could be classified as carboxylesterases. Differential sensitivities of larval and adult esterases to urea and heat treatment as well as to DFP may indicate the expression of different genes during metamorphosis.

Animals↗
PubMed1978

The multiple forms of brain acetylcholinesterase. II. A suggestion of their functional importance.

The pattern of the multiple forms of the acetylocholinesterase (AChE, E.C. 3.1.1.7) of the rat brain is investigated using polyacrylamide gradient micro-gel electrophoresis with regard to a possible functional importance of this individual forms. The patterns of the AChE-forms of selected regions of the CNS are compared and certain differences could be shown. After increased cholinergic input (into the hippocampus by electrical stimulation of the nc. septi medialis) an aggregation of AChE subunits is detectable. Subletal intoxication with an irreversible inhibitor of AChE is followed by a faster recovery of the smaller forms. A suggestion of a possible functional role of the multiple forms of AChE is discussed.

Acetylcholinesterase↗
PubMed1979

The multiple forms of brain acetycholinesterase. III. Implications for the histochemical demonstration of acetylcholinesterase.

The multiple forms of acetylcholinesterase (AChE, E.C. 3.1.1.7) have been investigated with regard to their histochemical demonstrability. Their pattern is influenced by buffer treatment, fixation, and by incubation conditions causing aggregation and disaggregation as well as loss or inactivation of individual forms. The standard histochemical method for AChE preferentially demonstrates the high molecular forms. Most of the oligomer forms are washed out or inactivated. A selective demonstration of the highly aggregated forms is possible either by inhibition of the oligomers with diisopropylfluoridate (DFP) or by specifically dissolving them out. No reason could be found for the selective demonstration of the low molecular weight forms.

Acetylcholinesterase↗