In JOHNSON et al. (1981), the Caenorhabditis elegans mutant strain PR1000, homozygous for the ace-1 mutation p1000, is shown to be deficient in the class A subset of acetylcholinesterases, which comprises approximately one-half of the total C. elegans acetylcholinesterase activity. Beginning with this strain, we have isolated 487 new behavioral and morphological mutant strains. Two of these, in...

The aim of this work was to evaluate, in vitro, the effect of L-alanine (Ala) on suckling rat brain acetylcholinesterase (AChE) and on eel Electrophorus electricus pure AChE inhibited by L-phenylalanine (Phe) as well as to investigate whether Phe or Ala is a competitive inhibitor or an effector of the enzyme. AChE activity was determined in brain homogenates and in the pure enzyme after 1 h pre...

A series of indolinone-based compounds bearing benzylpyridinium moiety was designed as dual-binding inhibitors of acetylcholinesterase (AChE). The target compounds 3a-u were synthesized by condensation of oxindole and pyridin-4-carbalehyde, and subsequent N-benzylation. The anti-cholinesterase activity evaluation of synthesized compounds revealed that most of them had very potent inhibitory act...

Dugesia tigrina is a non-parasitic platyhelminth, which has been recently utilized in pharmacological models, regarding the nervous system, as it presents a wide sensitivity to drugs. Our trials aimed to propose a model for an in vivo screening of substances with inhibitory activity of the enzyme acetylcholinesterase. Trials were performed with four drugs commercialized in Brazil: donepezil, ta...

Cyto- and myeloarchitectonics as well as acetylcholinesterase activity of the nucleus limitans thalami--an important part of the nociceptive system--were studied in insectivora (Sorex araneus, Erinaceus europaeus, Talpa europaeus), rat, rabbit, cat, monkey and man. Our results suggest that nucleus limitans is phylogenetically a rather new structure. In insectivora and in the rat we could not fi...

Seventeen lactones including eight territrem derivatives (1-8) and nine butyrolactone derivatives (9-17) were isolated from a marine-derived fungus Aspergillus terreus SCSGAF0162 under solid-state fermentation of rice. Compounds 1-3 and 9-10 were new, and their structures were elucidated by spectroscopic analysis. The acetylcholinesterase inhibitory activity and antiviral activity of compounds ...

The morphine-induced changes in the activity of enzymes involved in the metabolism of neurotransmitters in specific areas of the brain of rats made tolerant to morphine have been investigated. The activities of choline acetyl transferase (E.G.2.3.1.6.), acetylcholinesterase (E.C.3.1.1.7.) and monoamine oxidase (E.G. 1.4.3.4.) were determined in the hippocampus, thalamus, hypothalamus, cerebral ...