Discovery of novel (N-aryl-4-methylpiperidinyl)pyrazoles: a new class of potent lepidopteran insecticides.

Background: Insects of the order Lepidoptera are among the most destructive global pests, causing billions of dollars in damage annually. A new class of N-arylpyrazole-4-methylpiperidines with potent activity on lepidopteran species has been discovered.

Results: In a high-throughput insecticide screen compound 1 was identified to possess modest activity on the lepidopteran insect Plutella xylostella.

Pyrrole-2 carboxamides - A novel class of insect ryanodine receptor activators.

The ryanodine receptor (RyR) is an intracellular calcium channel critical to the regulation of insect muscle contraction and the target site of diamide insecticides such as chlorantraniliprole, cyantraniliprole and flubendiamide. To-date, diamides are the only known class of synthetic molecules with high potency against insect RyRs. Target-based screening of an informer library led to discovery of a novel class of RyR activators, pyrrole-2-carboxamides.

Mesoionic insecticides: a novel class of insecticides that modulate nicotinic acetylcholine receptors.

Background: As the world population grows towards 9 billion by 2050, it is projected that food production will need to increase by 60%. A critical part of this growth includes the safe and effective use of insecticides to reduce the estimated 20-49% loss of global crop yields owing to pests. The development of new insecticides will help to sustain this protection and overcome insecticide resistance.

Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide.

A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program which led to the discovery of triflumezopyrim as a highly potent insecticide controlling various hopper species. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biological activity evaluation are also presented.

Insecticidal quinoline and isoquinoline isoxazolines.

A series of quinoline and isoquinoline isoxazolines have been designed as pesticides for crop protection. Herein we reported the chemical synthesis, biological activity and structure-activity relationships. The isoquinoline derivative, such as 3i, is discovered as potent new class of isoxazoline insecticide which is competitive with commercial insecticide Indoxacarb.

Movement of cyantraniliprole in plants after foliar applications and its impact on the control of sucking and chewing insects.

Background: Given the physical properties of insecticides, there is often some movement of these compounds within crop plants following foliar application. In this context, movement of two formulations of cyantraniliprole, an anthranilic diamide, was characterized for translocation to new growth, distribution within a leaf and penetration through the leaf cuticle.

Results: Upward movement of cyantraniliprole to new plant growth via the xylem was confirmed using (14) C-radiolabeled cyantraniliprole and from Helicoverpa zea mortality on tomato leaves that had not been directly treated.

Discovery, synthesis, and evaluation of N-substituted amino-2(5H)-oxazolones as novel insecticides activating nicotinic acetylcholine receptors.

N-Substituted amino-2(5H)-oxazolones A are a novel class of insecticides acting as nicotinic acetylcholine receptor (nAChR) agonists and show potent activity against hemipteran insect species. Here we report the discovery and preparation of this class of chemistry. Our efforts in SAR elucidation, biological activity evaluation, as well as mode-of-action studies are also presented.

Discovery of cyantraniliprole, a potent and selective anthranilic diamide ryanodine receptor activator with cross-spectrum insecticidal activity.

Anthranilic diamides are an exceptionally active class of insect control chemistry that selectively activates insect ryanodine receptors causing mortality from uncontrolled release of calcium ion stores in muscle cells. Work in this area led to the successful commercialization of chlorantraniliprole for control of Lepidoptera and other insect pests at very low application rates. In search of lower logP analogs with improved plant systemic properties, exploration of cyano-substituted anthranilic diamides culminated in the discovery of a second product candidate, cyantraniliprole, having excellent activity against a wide range of pests from multiple insect orders.

4-Azolylphenyl isoxazoline insecticides acting at the GABA gated chloride channel.

Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides.

Seasonal abundance, life history, and parasitism of Caloptilia porphyretica (Lepidoptera: Gracillariidae), a leafminer of highbush blueberry.

The leafminer Caloptilia porphyretica Braun (Lepidoptera: Gracillariidae), has become a frequent pest in commercial highbush blueberries, Vaccinium corymbosum L., in New Jersey, but little is known about its seasonal abundance, life history, and parasitism rates. Monitoring programs were conducted from 2003 to 2006 on seven blueberry farms to determine the relative abundance of this leafminer by using pheromone-baited traps and by sampling vegetative and flower/fruit clusters and new shoot growth.

Optimization of pheromone deployment for effective mating disruption of oriental beetle (Coleoptera: Scarabaeidae) in commercial blueberries.

Cost is a potential limiting factor in the adoption of mating disruption to control oriental beetle, Anomala orientalis (Waterhouse) (Coleoptera: Scarabaeidae). A 3-yr study was conducted in 1-ha blueberry, Vaccinium corymbosum L., plots to test the possibility of lowering cost by reducing the number of point-source dispensers and pheromone [(Z)-7-tetradecen-2-one] concentrations, while maintaining mating disruption.

New and selective ryanodine receptor activators for insect control.

Diamide insecticides have emerged as one of the most promising new classes of insecticide chemistry owing to their excellent insecticidal efficacy and high margins of mammalian safety. Chlorantraniliprole and flubendiamide, the first two insecticides from this class, demonstrate exceptional activity across a broad range of pests in the order Lepidoptera. This chemistry has been confirmed to control insects via activation of ryanodine receptors which leads to uncontrolled calcium release in muscle.

A randomized controlled trial comparing treatment regimens for acute pain for topical oleoresin capsaicin (pepper spray) exposure in adult volunteers.

Objective: Several topical therapies have been proposed to treat acute pain from exposure to oleoresin capsaicin (OC). The purpose of this study was to determine the most beneficial topical treatment for relieving contact dermatitis pain caused by OC exposure.

Methods: We performed a single-blind, randomized human experiment evaluating the effectiveness of five different regimens for the treatment of topical facial OC exposure.

Synthesis of insecticidal fluorinated anthranilic diamides.

A series of highly active fluorinated anthranilic diamide insecticides have been prepared and their biological activity assessed on two aphid species in the search for systemically active compounds that control Hemiptera. In addition, we have demonstrated a new synthesis of N-aryl 3-fluoropyrazoles.

Effectiveness of protein baits on melon fly and oriental fruit fly (Diptera: Tephritidae): attraction and feeding.

Attraction and feeding responses of oriental fruit fly, Bactrocera dorsalis (Hendel), and melon fly, Bactrocera cucurbitae (Coquillett), were determined for different protein baits. In separate choice attraction assays for each species, significantly more flies arrived at stations with bait than water, but no differences existed among baits of GF-120 Fruit Fly Bait, GF-120 NF Naturalyte Fruit Fly Bait, Provesta 621 autolyzed yeast extract, and Mazoferm E802. In comparison with B.

Vasopressin treatment for cyclic antidepressant overdose.

Due to neurotransmitter reuptake inhibition, peripheral alpha receptor blocking effects, and sodium channel blockade, severe cyclic antidepressant poisoning may lead to intractable hypotension. We report a case of severe amitriptyline toxicity, with hypotension unresponsive to direct alpha receptor agonists after pH manipulation, but improved with intravenous vasopressin. Vasopressin use in the setting of cyclic antidepressant toxicity has not been previously reported.

Comparative effectiveness of different insecticides for organic management of blueberry maggot (Diptera: Tephritidae).

Laboratory and field assays using insecticides for organic pest management were conducted on the blueberry maggot, Rhagoletis mendax Curran. Topical exposure of flies to spinosad (Entrust), pyrethrum (PyGanic 1.4 EC), azadirachtin (Aza-Direct), and phosmet (Imidan 70-W) resulted in significantly higher mortality compared with the water control after 2 and 24 h.

Rattlesnake envenomation to the face of an infant.

Background: Mortality from rattlesnake envenomation in the United States is rare. Despite approximately 8000 crotaline (pit vipers) bites annually, it is estimated that only 10 to 15 deaths occur. Besides direct intravascular envenomation and anaphylaxis, bites to the head and neck may account for some of these rare fatalities.

Evaluation of traps and toxicants in an attract-and-kill system for Rhagoletis mendax (Diptera: Tephritidae).

A series of laboratory and field assays were performed to evaluate new methods for an attract-and-kill approach to control blueberry maggot, Rhagoletis mendax Curran. In laboratory assays, fly mortality was similar among insecticide-treated matted paper, plastic, and biodegradable sphere traps. Plastic and biodegradable traps baited with ammonium acetate captured significantly more flies than baited matted paper traps in field assays, whereas fly captures were similar in baited matted paper traps and unbaited plastic sphere traps.

Phenology and infestation patterns of plum curculio (Coleoptera: Curculionidae) on four highbush blueberry cultivars.

The plum curculio, Conotrachelus nenuphar (Herbst), is a well known pest in apple and peach orchards, but it also is capable of having an economic impact in highbush blueberries. Host phenology and plum curculio oviposition patterns were determined on four highbush blueberry cultivars differing in fruit maturation period. Numbers of oviposition scars were higher on early- ('Weymouth') and mid-season ('Duke' and 'Bluecrop') blueberries than on late-season 'Elliott' in 2001, 2002, and 2003.

Recapture of sterile Mediterranean fruit flies (Diptera: Tephritidae) in California's Preventative Release Program.

In southern California, the sterile insect technique has been used since 1994 to prevent establishment of the Mediterranean fruit fly, Ceratitis capitata (Wiedemann). This method involves the continual mass release of sterile flies, which suppress or eliminate any introduced wild fly populations. In addition, Jackson traps baited with trimedlure are deployed throughout the preventative release region for the dual purpose of detecting wild flies and monitoring released sterile flies.

Feeding activity and attraction of blueberry maggot (Diptera: Tephritidae) to protein baits, ammonium acetate, and sucrose.

Attraction and feeding assays were conducted on blueberry maggot, Rhagoletis mendax Curran, to three protein baits, ammonium acetate, and sucrose. Flies fed significantly longer on concentrations of 25 and 50% SolBait than they did on any of the concentrations tested for Nu-Lure, AY50% (Mauri Yeast Australia), or a water control. The number of flies arriving at SolBait in an attraction assay was significantly higher than for Nu-Lure and a water control but was not different from AY50%.

Effectiveness of GF-120 fruit fly bait spray applied to border area plants for control of melon flies (Diptera: Tephritidae).

In a field study in Hawaii, color-marked protein-deprived and protein-fed female melon flies, Bactrocera cucurbitae Coquillett, were released within canopies of unsprayed sorghum plants (a nonhost of melon flies) outside of a border area of unsprayed or bait-sprayed sorghum plants or open space that surrounded cucumbers, a favored host of melon flies. Application of bait spray to sorghum or sugarcane surrounding host plants of melon flies is a common practice for melon fly control in Hawaii. GF-120 Fruit Fly Bait spray proved very effective in preventing protein-deprived females from alighting on cucumbers (23% of released females were observed dead on bait-sprayed sorghum; 0% were observed alive on cucumbers), but proved less effective in suppressing protein-fed females (14% of released females were observed dead on bait-sprayed sorghum; 11% were observed alive on cucumbers).

Feeding and foraging of wild and sterile Mediterranean fruit flies (Diptera: Tephritidae) in the presence of spinosad bait.

The sterile insect technique (SIT) is used to control wild Mediterranean fruit fly introductions in California and Florida in the U.S. In the past, bait sprays containing malathion proved invaluable in treating new outbreaks or large populations before the use of SIT.

Effects of irradiation on Mediterranean fruit flies (Diptera: Tephritidae): emergence, survivorship, lure attraction, and mating competition.

Irradiation of puparia in Mediterranean fruit fly, Ceratitis capitata (Wiedemann), sterile insect release programs can negatively affect adult fly performance. Emergence, survivorship, lure attraction, and mating competition tests were performed on irradiated and unirradiated Mediterranean fruit flies in Hawaii. Unirradiated flies of the Vienna-7 (tsl) strain had higher emergence, flight ability, and survivorship compared with irradiated flies.