1. The kinetics of inhibition of AChE by the carbamate inhibitor eserine sulphate were investigated in five resistant strains of Drosophila melanogaster. 2. The dissociation constant (Kd) was higher and the carbamylation constant was lower relative to the control in four of these. 3. No change was observed in the decarbamylation constants (k3) of the five strains. 4. The Vmax of AChE was higher in the five resistant stocks than in the Canton-S/TM2 controls but no change in the Km of AChE for acetylthiocholine was observed. No electrophoretic variants of AChE were detected. 5. No increase in the activity of nonspecific esterases was detected in the resistant lines. 6. These results indicate that resistance to eserine sulphate may occur in D. melanogaster by a reduction in affinity of AChE for the inhibitor.
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http://dx.doi.org/10.1016/0742-8413(88)90122-3 | DOI Listing |
Behav Brain Res
June 2021
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan; Complementary and Alternative Medicine Clinical Research and Development, Graduate School of Medicine Sciences, Kanazawa University, 13-1 Takaramachi, Kanazawa, Ishikawa 920-8640, Japan.
Deficits in olfaction are associated with neurodegenerative disorders such as Alzheimer's disease. A recent study reported that intranasal zinc sulfate (ZnSO)-treated mice show olfaction and memory deficits. However, it remains unknown whether olfaction deficit-induced learning and memory impairment is associated with the cholinergic system in the brain.
View Article and Find Full Text PDFJ Med Food
August 2019
1Department of Pharmacology II, School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Japan.
Royal jelly (RJ) is widely used as a cosmetic or dietary supplement to relieve various health disorders, such as dry skin, fatigue, and menopause. RJ has been recommended to improve constipation on a commercial basis. However, the detailed mechanisms by which RJ influences intestinal motility and whether RJ improves constipation remain unclear.
View Article and Find Full Text PDFVet Parasitol
January 2019
Department of Biology, Animal Physiology and Neurobiology Section, KU Leuven, Naamsestraat 59, box 2465, 3000 Leuven, Belgium.
Parasitic nematodes continue to cause significant economic losses in livestock globally. Given the limited number of anthelmintic drugs on the market and the currently increasing drug resistance, there is an urgent need for novel anthelmintics. Most motility assays of anthelmintic activity for parasitic nematodes are laborious and low throughput, and therefore not suitable for screening large compound libraries.
View Article and Find Full Text PDFBull Environ Contam Toxicol
January 2018
Unidad de Química en Sisal, Facultad de Química, Universidad Nacional Autónoma de México, Puerto de Abrigo s/n Sisal, 97356, Hunucma, Yucatán, Mexico.
The inhibition of cholinesterase (ChE) activity has been used as a biomarker of exposure to organophosphate and carbamate insecticides. ChE of nesting female green turtles (Chelonia mydas) were biochemically characterized using two substrates, acetylthiocholine iodide and butyrylthiocholine iodide, and three ChE inhibitors (eserine sulfate, BW284C51 and iso-OMPA). The results indicated that BChE is the predominant plasma ChE in female C.
View Article and Find Full Text PDFExp Appl Acarol
September 2017
Department of Science and Technology, Science and Engineering Research Board (SERB), New Delhi, 110070, India.
A comparative analysis of esterases in susceptible and resistant ticks revealed six types of esterases (EST-1b, EST-2b, EST-3b, EST-4b, EST-5b and EST-6b) in Rhipicephalus microplus and four types (EST-1h, EST-2h, EST-3h, EST-4h) in Hyalomma anatolicum using α-naphthyl acetate substrate. Inhibition studies with eserine sulfate, p-chloromercuribenzoate, copper sulphate and phenylmethylsulfonyl fluoride revealed a marked variation in band intensity between susceptible and resistant ticks, with the latter being more intense. Qualitative expression of EST-4b along with an extra band of EST-5b and EST-6b were indicative of deltamethrin and diazinon resistance in R.
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