Structure-activity relationships of 1,2,3-benzothiadiazoles as synergists for carbaryl against the house fly (Musca domestica)

Fifty six 1,2,3-benzothiadiazoles and related compounds were evaluated as carbaryl synergists against the house fly (Musca domestica). Many of these were excellent synergists, the most active being those containing various combinations of halogen, alkyl, or alkoxy substituents in the 5- and/or 6-positions of the ring.Regression analysis on the data from 14 compounds for which substituents constants were available established that synergistic activity can be satisfactorily described by equations in terms of the hydrophobic bonding constant (π) and the homolytic free radical constant (σ ·).The results with compounds related to the 1,2,3-benzothiadiazoles suggest that synergistic activity is associated primarily with the diazosulfide moiety.     

The effect of phosphine on the absorption and circular dichroic spectra of cytochrome c and cytochrome oxidase

The interaction of phosphine with purified cytochrome c and cytochrome oxidase was studied by absorption and circular dichroic spectrometry. Treatment of cytochrome oxidase with phosphine yielded absorption spectra in both the visible and Soret region that were similar to that produced by dithionite. Striking changes in the circular dichroic spectra were also recorded, sugesting that a valence change of the heme iron was accompanied by a conformation change of the prosthetic group.Phosphine treatment of cytochrome c also yielded spectra similar to those produced by reduction with dithionite suggesting a valence change of the heme iron. However, both the time necessary for complete reduction and the concentration of phosphine necessary for this effect suggest that, in comparison with cytochrome oxidase, cytochrome c was relatively insensitive. Reduction of cytochrome oxidase by phosphine had only a very minor effect on the intrinsic dichroic spectrum suggesting little effect on the polypeptide chains.The persistence of a component after reduction by phosphine and the subsequent reduction of this component by dithionite suggests that phosphine primarily reduced only one comonent of the cytochrome aa₃ complex. The failure of EDTA and fluoride, which are known ligands of cytochrome a₃ to affect the reduction of cytochrome aa₃ by phosphine, as well as the occurrence of a 436-nm isosbestic point of the ferric-ferrous absorption spectra suggests that phosphine reduced primarily cytochrome a. However, it is argued that a slow reduction of cytochrome a₃ cannot be ruled out.     

Isomerization and Beckmann rearrangement reactions in the metabolism of methomyl in rats

Methomyl {S-methyl-N-[(methylcarbamoyl)oxy]thioacetimidate}, also known as Lannate, may exist in two geometric configurations but the more stable syn isomer is the form applied as an insecticide. In the rat, syn[¹⁴CN]methomyl [CH₃S(CH₃)CNOC(O)NHCH₃] was metabolized to respiratory ¹⁴CO₂ and $\text{CH}{}_3{}^{14}\text{CN}$ in a ratio of about 2 to 1. Studies with the anti isomer showed that it was metabolized predominately to $\text{CH}{}_3{}^{14}\text{CN}$. These and other data are presented supporting the contention that syn methomyl is partially isomerized to the anti isomer in the animal prior to the hydrolysis of the ester linkage. After hydrolysis, the syn oxime [CH₃S(CH₃)¹⁴CNOH] is further metabolized to ¹⁴CO₂ while the anti oxime is metabolized to $\text{CH}{}_3{}^{14}\text{CN}$. Proposed immediate precursors to the carbon dioxide and acetonitrile, formed by Beckmann rearrangement of the syn and anti oximes, are CH₃S¹⁴C(O)NHCH₃ and $\text{[}\text{CH}{}_3{}^{\mathrm{14\oplus }}\text{CNSCH}{}_3\text{]x}{}^{\mathrm{?}}$, respectively.     

The "barker" (neonatal respiratory distress) syndrome in the pig: its occurrence in the field.

A new syndrome, characterised by acute respiratory distress and by abnormalities of the skin, hair and thyroid, was the apparent cause of neonatal death in 35 (24 per cent) of 146 piglets sired by a large white boar in four small commercial pig units. The syndrome appears to be of genetic origin, inherited as an autosomal recessive trait. Its similarities with the respiratory distress syndrome (RDS) of the newborn infant and the "barker" syndrome of the newborn foal are discussed.     

Seasonal activity of EPTC for Cyperus rotundus L. control in a tropical climate*

Four experiments were conducted at six week intervals to determine the seasonal activity and persistence of soil-incorporated EPTC (5-ethyl N,N-dipropyl(thiocarbamate)) for Cyperus rotundus L. control and tolerance of okra (Hibiscus esculentus L.), cucumber (Cucumis sativus L.), lettuce (Lactuca sativa L.), red beet (Beta vulgaris L.) and carrot (Daucus carota L.) during the dry and wet seasons in Viçosa, Brazil. Satisfactory control of C. rotundus was obtained at 2 kg/ha EPTC during the dry season and 4 kg/ha or more during the wet season. Only red beet and carrot tolerated these doses of EPTC when the crops were planted five days after application. However, selective control of C. rotundus was obtained when the planting date of lettuce was delayed for three or six weeks after EPTC application. EPTC controlled C. rotundus at half the dose that was required to control three species of annual grass that germinated near the soil surface. EPTC persisted longer when applied to air dry soil and incorporated with a rototiller than when incorporated into moist or wet soil.     

Distinguishing between carbamate and organophosphate insecticide poisoning in house flies by symptomology

Three criteria, latency to convulsions, still period, and recovery are used to distinguish between carbamate and phosphate insecticide poisoning in house flies, Musca domestica. Because of shorter latencies with carbamate-treated flies, the central nervous system was considered more sensitive to the presence of carbamates than phosphates. Recovery from carbamate-induced tetany was considered correlated with reactivation of carbamylated cholinesterase. There appeared to be a fundamental difference between the insecticidal actions of carbamates and phosphates not wholly explainable by cholinesterase inhibition. Tethered or held house flies were less susceptible to poisoning than unrestrained flies.     

Spectral interactions of insecticide synergists with microsomal cytochrome P-450 from insecticide-resistant and susceptible house flies

The spectral interactions of 45 insecticide synergists and related compounds with oxidized and reduced cytochrome P-450 from microsomes of insecticide-resistant and -susceptible house flies were investigated. The type III interaction typical of piperonyl butoxide was the most common spectral interaction for the compounds studied. In addition to this, several other varients of the type III interaction were noted. In general these responses with house fly microsomes were similar to those reported for mammals, although some minor species and strain differences were observed. The cytochrome P-450 from susceptible house flies, although reported previously not to exhibit type I difference spectra with many xenobiotics, was found to elicit this spectral response with several methylenedioxyphenyl compounds.