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At least 19 recordsLinked to original sources
PubMed1984

Involvement of adrenergic and serotonergic nervous mechanisms in allethrin-induced tremors in mice.

Oral or intravenous administration of allethrin, a synthetic derivative of the pirethrin-based insecticides, produces neurotoxic symptoms consisting of mild salivation, hyperexcitability, tremors and convulsions which result in death. Intracerebroventricular injection of allethrin to mouse at about one-nineth the dose of intravenous administration, produced qualitatively identical but less prominent symptoms, indicating that at least some of the symptoms may be originated in the central nervous system. To investigate the mechanism of action of the compound, we studied the ability of agents which alter neurotransmission to prevent or potentiate the effect of convulsive doses of technical grade (15.5% cis, 84.5% trans) allethrin. Intraperitoneal pretreatment with drugs which block noradrenergic receptors or norepinephrine synthesis, such as pentobarbital, chlorpromazine, phentolamine, phenoxybenzamine and reserpine, depressed the tremor induced by allethrin. The inhibitory effect of reserpine was reversed by phenylephrine. Both the serotonergic blocker, methysergide, and the serotonin depletor, rho-chlorphenylalanine, potentiated the effect of allethrin. The potentiating effect of methysergide was antagonized by 5-hydroxytryptamine. However, intracerebroventricular administration of methysergide was ineffective in potentiating the effect of allethrin. alpha 2- and beta-adrenoceptor blockers, muscarinic antagonists, GABA mimenergics and morphine had no effect. These results suggest that allethrin produces its neurotoxic responses in mice by acting on the brain and spinal levels. Furthermore, adrenergic excitatory and serotonergic inhibitory mechanisms may be involved in the neural pathway through which the allethrin-induced tremor is evoked.

Allethrins↗
PubMed1994

Interactions of the pyrethroid insecticide allethrin with liposomes.

The action of allethrin, a pyrethroid with an alkenylmethylcyclopentenolone group, on the thermotropic properties of lipid vesicles has been investigated. Application of turbidimetry and differential scanning calorimetry to liposomes made with dimyristoyl- (DMPC), dipalmitoyl- (DPPC), and distearoyl- (DSPC) phosphatidycholine, containing variable concentrations of allethrin, showed that the pyrethroid lowers the temperature at which the phase transition of the phospholipid occurs. Furthermore, allethrin produces a broadening of the peak which marks the gel to liquid-crystalline phase transition. The appearance of a second peak as the allethrin concentration in the membranes rises indicates a limited miscibility of the pyrethroid in lipids. Incorporation of allethrin in carboxyfluorescein-trapped unilamellar liposomes, followed by incubation at several temperatures, enhances carboxyfluorescein release in allethrin-containing vesicles. The results are discussed in terms of a preferential localization of allethrin in an extended orientation in the bilayer with the carbonyl group of the alkenylmethylcyclopentenolone residue in the lipid water interface and the cyclopropanecarboxylate moiety between the hydrocarbon acyl chain of the phospholipids.

Allethrins↗
PubMed2003

Mammalian voltage-gated calcium channels are potently blocked by the pyrethroid insecticide allethrin.

Pyrethroids are commonly used insecticides for both household and agricultural applications. It is generally reported that voltage-gated sodium channels are the primary target for toxicity of these chemicals to humans. The phylogenetic and structural relatedness between sodium channels and voltage-gated calcium (Ca) channels prompted us to examine the effects of the type 1 pyrethroid allethrin on the three major classes of mammalian calcium channels exogenously expressed in human embryonic kidney 293 cells. We report that all classes of mammalian calcium channels are targets for allethrin at concentrations very similar to those reported for interaction with sodium channels. Allethrin caused blockade with IC(50) values of 7.0 microM for T-type alpha(1G) (Ca(v)3.1), 6.8 microM for L-type alpha(1C) (Ca(v)1.2), and 6.7 microM for P/Q-type alpha(1A) (Ca(v)2.1) channels. Mechanistically, the blockade of calcium channels was found to be significantly different than the prolonged opening of mammalian sodium channels caused by pyrethroids. In all calcium channel subtypes tested, allethrin caused a significant acceleration of the inactivation kinetics and a hyperpolarizing shift in the voltage dependence of inactivation. The high-voltage-activated P/Q- and L-type channels showed a frequency of stimulation-dependent increase in block by allethrin, whereas the low-voltage-activated alpha(1G) subtype did not. Allethrin did not significantly modify the deactivation kinetics or current-voltage relationships of any of the calcium channel types. Our study indicates that calcium channels are another primary target for allethrin and suggests that blockade of different types of calcium channels may underlie some of the chronic effects of low-level pyrethroid poisoning.

Allethrins↗
PubMed2005

Biodegradation of allethrin, a pyrethroid insecticide, by an acidomonas sp.

Allethrin is a major mosquito repellent agent. To degrade allethrin present in used mats and the environment, a bacterium capable of utilizing allethrin was isolated. This isolate, an Acidomonas sp., grew in minimal medium with 16 mM: allethrin as sole source of carbon and degraded >70% of it in 72 h, with negligible residual metabolites in the medium. Culture filtrates collected after 48 h and 72 h showed presence of (i) cyclopropanecarboxylic acid, 2,2-dimethyl-3-(2-methyl-1-propenyl), (ii) 2-ethyl-1,3-dimethyl-cyclopent-2-ene-carboxylic acid (iii) chrysanthemic acid and (iv) allethrolone [2-cyclopenten-l-one, 4-hydroxy-3-methyl-2(-2-propenyl)] as the major metabolites with 2 minor metabolites. Allethrin is thus metabolized by a hydrolytic pathway followed by oxidation and dehydrogenation.

Acetobacteraceae↗
PubMed1999

Time course and temperature dependence of allethrin modulation of sodium channels in rat dorsal root ganglion cells.

Key effects of the pyrethroid insecticide allethrin, delivered to or washed out from cells at 10 or 100 microM in 0.1% DMSO, on neuronal Na(+) channel currents were studied in rat dorsal root ganglion (DRG) cells under whole-cell patch clamp. Tetrodotoxin-resistant (TTX-R) Na(+) channels were more responsive to allethrin than tetrodotoxin-sensitive (TTX-S) Na(+) channels. On application of 10 or 100 microM allethrin to cells with TTX-R Na(+) channels, the Na(+) tail current during repolarization developed a large slowly decaying component within 10 min. This slow tail developed multiphasically, suggesting that allethrin gains access to Na(+) channels by a multiorder process. On washout (with 0.1% DMSO present), the slow tail current disappeared monophasically (exponential tau=188+/-44 s). Development and washout rates did not depend systematically on temperature (12 degrees, 18 degrees, or 27 degrees C), but washout was slowed severely if DMSO was absent. As the duration of a depolarizing pulse was increased (range 0.32-10 ms), the amplitude of the slow component of the succeeding tail conductance first increased then decreased. Tail current amplitude had the same dependence on preceding pulse duration (at 18 degrees ) at 10 or 100 microM, consistent with allethrin modification of Na(+) channels at rest before opening. At 10 microM, slow tail conductance was at maximum 40% of the peak conductance during the previous depolarization, independent of temperature; evidently, the fraction of open modified channels did not change. However, at low temperature, the tail is more prolonged, bringing more Na(+) ions into a cell. In functioning neurons, this Na(+) influx would cause a larger depolarizing afterpotential, a condition favoring the repetitive discharges, which are signatory of pyrethroid intoxication.

Allethrins↗
PubMed1983

Involvement of cholinergic mechanism in the action of allethrin in insect CNS.

Allethrin had a stimulating action on spontaneous discharges in the cockroach sixth abdominal ganglion superfused with an insect saline solution. This action at a low concentration (5 X 10(-8) M) of allethrin was abolished by either of d-tubocurarine, hexamethonium or atropine at 5 X 10(-4) M. It was also abolished by the treatment of ganglia with hemicholinium-3 or by low-calcium-high magnesium insect saline solution. However, treatment of these blocked ganglia with allethrin at more than 5 X 10(-7) M overcame the block, producing increased spontaneous activity. Allethrin had no effect on insect cholinesterase activity. These results may suggest that the stimulating action at a low concentration of allethrin may be mediated by the release of ACh from cholinergic terminals in ganglia.

Acetylcholine↗
PubMed1995

Effect of the pyrethroid insecticide allethrin on membrane fluidity.

Allethrin is a widely used pyrethroid insecticide with an alkenylmethylcyclopentenolone group in its structure. We have analyzed its interaction with model and native membranes using DPH and its polar derivative TMA-DPH fluorescence polarization. Allethrin modified the bilayer order in the temperature range of the phase transition when incorporated into liposomes made with dimyristoyl-(DMPC), dipalmitoyl-(DPPC) and distearoyl-(DSPC) phosphatidylcholine. In DMPC: allethrin mixtures the pyrethroid decreased the bilayer order in the gel phase, without altering the liquid-crystalline one. In native membranes, DPH and TMA-DPH fluorescence polarization remained unchanged after incubation with allethrin. The release of hemoglobin was notably facilitated by the incorporation of allethrin into human erythrocytes. The results are discussed in terms of a possible aggregation of the insecticide in the lipid bilayer to create special domains with a consequent increase in membrane instability.

1,2-Dipalmitoylphosphatidylcholine↗
PubMedDate not supplied

Lack of changes in brain muscarinic receptor and motor activity of mice after neonatal inhalation exposure to d-allethrin.

Synthetic pyrethroids are among the most common pesticides and insecticides currently in worldwide use. Eriksson and co-workers postulated that oral exposure of mice to pyrethroids during a neonatal brain growth spurt induces permanent disturbance in the cerebral muscarinic cholinergic receptor (MAChR) and behaviour. However, the scientific basis for these phenomena is now under discussion. The present study was performed to determine whether the experimental findings of Eriksson's study could be reproduced in newborn mice by inhalation. Male and female NMRI mice were exposed to d-allethrin by whole-body inhalation for 6 h per day between postnatal days 10 and 16. Actual concentrations of d-allethrin were 0.43, 1.35, 3.49 and 74.2 mg m(-3) (equivalent to 0.70, 2.2, 5.7 and 120.2 mg kg(-1) day(-1), respectively), and the mass median aerodynamic diameter and geometric log-standard deviation of mist particles ranged from 2.58 to 2.98 micro m and from 1.58 to 2.09 micro m for all groups, respectively. The highest exposure level in the present study (74.2 mg m(-3)) was ca. 13,000 times as high as the concentration used in practice. The MAChR in the three brain areas (cortex, hippocampus and striatum) and motor activity were examined at the ages of 17 days and 4 months. In addition, a water-maze test was performed at the age of 11 months. There was no systemic toxicity interfering with the interpretation of assay results. The neonatal exposure to d-allethrin by inhalation did not induce effects either on the brain MAChR density and motor activity at 17 days and 4 months or on performance in the learning/memory test at the age of 11 months. The effects of allethrins on developmental neurotoxicity that Eriksson and co-workers reported previously were not reproduced in the present study.

Administration, Inhalation↗
PubMed1993

Differential sensitivity of tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels to the insecticide allethrin in rat dorsal root ganglion neurons.

The pyrethroid insecticides are known to modify neuronal sodium channels to cause a prolongation of whole cell current. The sodium channels expressed in the dorsal root ganglion neurons of the rat are of two types, one highly sensitive to tetrodotoxin and the other highly resistant to tetrodotoxin. The pyrethroid allethrin exerted profound effects on tetrodotoxin-resistant sodium channels while causing minimal effects on tetrodotoxin-sensitive sodium channels. Currents derived from tetrodotoxin-resistant sodium channels were greatly prolonged during a step depolarization; the tail currents upon repolarization were also augmented and prolonged. In the tetrodotoxin-sensitive sodium channel currents, these changes caused by allethrin were much smaller or negligible. The activation and inactivation voltages of tetrodotoxin-resistant peak sodium currents were not significantly altered by allethrin. The differential action of allethrin on the two types of sodium channels would be important not only in identifying the target molecular structure but also in interpreting the symptoms of poisoning in mammals.

Allethrins↗
PubMed1982

Allethrin interactions with the nicotinic acetylcholine receptor channel.

Interactions of the synthetic pyrethroid allethrin with the nicotinic acetylcholine (ACh) receptor/channel were studied in membranes from Torpedo electric organ. Allethrin did not inhibit binding of [3H]ACh to the receptor sites, but inhibited noncompetitively binding of [3H]perhydrohistrionicotoxin ([3H]H12-HTX) to the ionic channel sites in a dose-dependent manner. The inhibition constant (Ki) of [3H]H12-HTX binding in absence of receptor agonist was 30 micro M, while in presence of 100 micro M carbamylcholine it was 4 micro M. This inhibitory effect of allethrin had a negative temperature coefficient. The high affinity binding of allethrin to the channel sites of the nicotinic ACh-receptor may be indicative of a postsynaptic site of action for pyrethroids, in addition to their known action on the sodium channel.

Acetylcholine↗
PubMed2000

Point mutations in domain III of a Drosophila neuronal Na channel confer resistance to allethrin.

Voltage-gated sodium channels are the presumed site of action of pyrethroid insecticides and DDT. We screened several mutant sodium channel Drosophila lines for resistance to type I pyrethroids. In insecticidal bioassays the para(74) and para(DN7) fly lines showed greater than 4-fold resistance to allethrin relative to the allethrin sensitive Canton-S control line. The amino acid substitutions of both mutants are in domain III. The point mutation associated with para(74) lies within the S6 transmembrane region and the amino acid substitution associated with para(DN7) lies within the S4-S5 linker region. These sites are analogous to the mutations in domain II underlying knockdown resistance (kdr) and super-kdr, naturally occurring forms of pyrethroid resistance found in houseflies and other insects. Electrophysiological studies were performed on isolated Drosophila neurons from wild type and para(74) embryos placed in primary culture for three days to two weeks. The mutant para(74) sodium currents were kinetically similar to wild type currents, in activation, inactivation and time to peak. The only observed difference between para(74) and wild-type neurons was in the affinity of the type I pyrethroid, allethrin. Application of 500 nM allethrin caused removal of inactivation and prolonged tail currents in wild type sodium channels but had little or no effect on para(74) mutant sodium channels.

Allethrins↗
PubMed1996

Bioefficacy of mosquito mat, coil and dispenser formulations containing allethrin group of synthetic pyrethroids against mosquito vectors.

The bioefficacy of mats, coils and dispensers containing allethrin group of synthetic pyrethroids was studied against laboratory strains of Culex quinquefasciatus, Aedes aegypti and Anopheles stephensi. Except esbiothrin in the mat formulation which was 100 and 178 times more effective against Cx. quinquefasciatus than against Ae. aegypti and An. stephensi with KT50 of 0.005, 0.5 and 0.89 min. respectively, all the three allethrins in mat or coil formulations were equally effective against the three vector mosquitoes. When compared to mat formulations of d-allethrin and bioallethrin, mat formulation of esbiothrin was 156 and 144 times more effective against Cx. quinquefasciatus. It was 162 times more effective against Cx. quinquefasciatus than in the coil formulation. Dispenser containing d-allethrin was the least effective against Cx. quinquefasciatus (KT50: 2.65 min.) and Ae. aegypti (KT50: 4.68 min.) but as effective as coil against An. stephensi. When mat and dispenser heated or coil burnt continuously for 10 hours the knockdown was consistently above 60% in all the three vector species but mortality was not consistently > 60% in Ae. aegypti. Repellent effect of the formulations ranged from 0.0 to 80.3%, 0 to 57.3% and 59.2 to 78.3% against Cx. quinquefasciatus Ae. aegypti and An. stephensi respectively. Repellency was more against An. stephensi than against the other two species. Mats and coils deterred > 50% of the mosquitoes from feeding on the chicken (range: 50 to 99.52%) but in case of dispenser the effect was only 14.72 to 65.01%. The use of these formulations as a control tools in reducing man-vector contact is discussed.

Allethrins↗
PubMed2001

Monitoring of allethrin, deltamethrin, esbiothrin, prallethrin and transfluthrin in air during the use of household mosquito repellents.

Three types of mosquito repellent [two different mosquito coils containing allethrin 0.1% w/w and transfluthrin 0.03% w/w, an aerosol sample containing a combination of two pyrethroid molecules (deltamethrin 0.02% w/w + allethrin 0.13% w/w) and two different mosquito mats containing esbiothrin 2.0% w/w and prallethrin 1.5% w/w as active ingredients] were individually subjected to use in a closed room. Air samples from the room were drawn at different time intervals (15, 30 and 45 min, and 1, 2, 4, 6 and 8 h) uniformly from three different positions in the room (top, middle and bottom) with the pyrethroid contents analysed using gas chromatography-electron capture detection (GC-ECD). Analysis of air samples showed maximum concentrations of the pyrethroid residues allethrin (0.0120 ppm), transfluthrin (0.0134 ppm), deltamethrin (0.0057 ppm), allethrin (0.080 ppm), esbiothrin (0.015 ppm) and prallethrin (0.0138 ppm) within 30-45 min of use. The drop in residue content was significant with time. At the end of a 6 h period, most of the residues had dissipated to below 0.0001 ppm. Further significant differences were observed in the residue contents tested at different points within the room. Studies were compared with the experimental results obtained when the mosquito repellents were tested with air circulation in the room.

Air Movements↗
PubMed2005

Liquid chromatography-tandem mass spectrometry for the identification of impurities in d-allethrin samples.

A previous GC/MS study highlighting the impurity profile of the synthetic pesticide d-allethrin is extended here to validate and confirm the impurities identity through the development of soft ionisation HPLC-MS methods. To accomplish this, we developed a reverse phase LC-MS analysis in gradient elution with two distinct soft ionisation techniques, the atmospheric pressure ionisation with electrospray source (API-ESI) and the chemical ionisation (APCI). A single quadrupole and an ion trap, which allowed the simultaneous determination of the molecular masses and structural information of the impurities by acquisition of collisionally induced (CID) product ions spectrum and in-source fragmentation, were employed as analysers. Single quadrupole and ion trap analysers resulted perfectly matching in the d-allethrin impurity fragmentation patterns. All the main impurities over 0.1% identified by GC/MS were confirmed. Results indicate that the proposed HPLC/MS method was found appropriate to confirm the presence of impurities such as chrysolactone, chloro allethrin derivatives, allethrolone and chrysanthemic acid, excluding their formation under GC/MS strong ionisation condition.

Allethrins↗
PubMed2005

Neuromechanical effects of pyrethroids, allethrin, cyhalothrin and deltamethrin on the cholinergic processes in rat brain.

Our previous microdialysis study of freely moving rats demonstrated that 3 pyrethroids, allethrin (type I), cyhalothrin (type II) and deltamethrin (type II) differentially modulate acetylcholine (ACh) release in the hippocampus. To better understand the mechanisms of their modulatory effects and also other effects on the cholinergic system in the brain, the activities of ACh hydrolyzing enzyme acetylcholinesterase (AChE), ACh synthesizing enzyme choline acetyltransferase (ChAT) and ACh synthesizing rate-limiting step, high-affinity choline uptake (HACU) were examined in the present study. The pyrethroids studied had no effect on AChE activity in the cortex, hippocampus and striatum. These pyrethroids had no significant effect on ChAT in the cortex and hippocampus, but striatal ChAT was increased at higher dosage (60 mg/kg) by all three compounds. Lineweaver-Burk analysis of hippocampal HACU revealed that the pyrethroids did not alter the Michaelis-Menten constant (Km) value but caused alteration of maximal velocity (Vmax). Allethrin (60 mg/kg) and cyhalothrin (20 and 60 mg/kg) decreased while deltamethrin (60 mg/kg) increased the Vmax for HACU. In vitro study showed that at higher concentrations (> or = 10(-) (6) M) allethrin and cyhalothrin reduced the hippocampal HACU but deltamethrin increased it. These results suggest that mechanisms of ACh synthesis are involved in the modulatory effects of the pyrethroids on ACh release and other cholinergic activities.

Acetylcholine↗
PubMed1998

Aliphatic aldehydes and allethrin in mosquito-coil smoke.

Presence of aliphatic aldehydes and allethrin in the smoke produced by two brands of mosquito-coil was determined by high performance liquid chromatography. It was observed that burning mosquito-coil produces a greater amount of formaldehyde, acetaldehyde and acrolein in the gaseous phase, whereas lesser amount of particulate-bounded aldehydes. Aldehydes bounded in particulates were, however, enriched in terms of concentration. Allethrin was found to occur only in particulates of 0.1-1.0 micron size. The results reveal that allethrin may not be capable of attacking the mosquitoes effectively.

Air Pollutants↗
PubMed2002

Impact of long-term exposure to mosquito coils: residual deposition and dissipation of D-trans-allethrin in a room.

A D-trans-allethrin-based mosquito repellent coil formulation was used continuously in a room for 30 d. Two different experiments were conducted and the deposition of residues on different surfaces of the room was determined. Studies were conducted continuously for a period of 30 d in a fully closed room and in another room kept open for 14 h per day. The residues deposited on different surfaces, ceiling, side walls and floor, were measured. The results showed the accumulation of high concentrations of allethrin on all the surfaces of the room when the room was in a fully closed condition. Samples collected from the ceiling showed residues of D-trans-allethrin of 6.34-148.63 microg m(-2) during the 30 d study, the side walls 4.68-170.72 microg m(-2) and the floor 20.00-184.52 microg m(-2) Maximum residues were observed in 30 d samples collected from the ceiling and floor. The residual concentrations were nearly 10 times higher in samples collected from the closed room. Discontinuation of the use of the mosquito repellent after 30 d led to a gradual decrease in the concentrations of residues on all the surfaces. The influence of environmental parameters on the dissipation of residues was also studied.

Allethrins↗
PubMed2000

Management of endemic outbreaks of scabies with allethrin, permethrin, and ivermectin.

BACKGROUND: At three residences for the elderly, recurrent scabies infestations became out of control. Due to the failure of repeated, nonsynchronized therapeutic efforts with conventional external anti-scabies treatments, an eradication program had to be developed. We describe a protocol for the management of outbreaks of scabies. METHODS: According to the clinical examination and microscopically identified mites, all individuals of the population (IOP: patients, staff, and family members) were divided into two groups: (a) healthy and infested IOP; and (b) cases with crusted scabies. The first group was treated simultaneously once with external scabicides (allethrin or permethrin). All others were hospitalized and treated either with systemic ivermectin or with the latter in combination with permethrin. RESULTS: In 252 IOP living in three residences for the elderly, clinical signs of scabies were reported in 91.5%, 78.5%, and 15.4% of the patients (age 55-97 years; mean, 80.5 years), 54.1%, 32.9%, and 16.6% of staff members, and in 7%, 3%, and 0% of family members. The infested IOP showed crusted scabies (index cases) in 5.3%, 5.0%, and 1.7%, common scabies in 43.1%, 36.7%, and 7.1%, and postscabiotic dermatitis in 10.3%, 7.6%, and 3.5%. In 99.2% of the synchronously treated IOP in group (a) (n = 240), the conventional treatment with permethrin cream 5% or allethrin spray was effective. Group (b) (n=12) received ivermectin (12 mg) once (n=5) or twice (n= 7) after an interval of 8 days. One index case received permethrin three times. CONCLUSIONS: Outbreaks of scabies in populations of elderly people require special management for disease control. Synchronous treatment with external permethrin cream 5% or allethrin spray, including all IOP once, and close control offers a time-saving, cheap, and reliable method. Crusted scabies should be treated by oral administration of ivermectin once or twice after an interval of 8 days. Additional applications of permethrin and mechanical clearing of hyperkeratotic subungual areas shorten the course.

Aged↗