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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
1996-1-22
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pubmed:abstractText |
1. A class of compounds, 9-aminoacridines, have long been known to be reversible inhibitors of acetylcholinesterase (AChE-EC 3.1.1.7), the most familiar of which is 9-amino-1,2,3,4-tetrahydroacridine (Tacrine). 2. A novel aminoacridine was synthesised: -2-tertiary-butyl-9-amino-1,2,3,4- tetrahydroacridine (2tBuTHA). 3. In vitro comparisons of the acetylcholinesterase inhibitory potential and neurotoxicity compared to Tacrine were performed using a chemically differentiated neuroblastoma cell line (Neuro 2A). 2tBuTHA, but not Tacrine, was cytotoxic to the neural cell following 20 h exposure, despite being the least potent AChE inhibitor (IC80 AChE 12.53 microM +/- 1.14 s.e.m., Neutral Red Uptake IC50 9.53 microM +/- 0.98 s.e.m., MTT Reduction IC80 14.6 microM +/- 1.43 s.e.m.). 4. In vivo studies used a novel application of a five arm radial maze to assess neuropharmacological effects on working memory in control and Scopolamine (1 mg kg-1 i.p.) treated mice. There was an impairment of short term cognitive function with 2tBuTHA (15 mg kg-1 i.p.), but not Tacrine (10 mg kg-1 i.p.) which improved the Scopolamine deficit as expected. 5. This combined in vitro and in vivo data infers a neurotoxic property for the novel compound 2tBuTHA, a close structural analogue of Tacrine.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aminoacridines,
http://linkedlifedata.com/resource/pubmed/chemical/Cholinesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Metallothionein,
http://linkedlifedata.com/resource/pubmed/chemical/Neurotoxins,
http://linkedlifedata.com/resource/pubmed/chemical/Neutral Red,
http://linkedlifedata.com/resource/pubmed/chemical/Scopolamine Hydrobromide,
http://linkedlifedata.com/resource/pubmed/chemical/Tacrine
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0960-3271
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
469-74
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:8519521-Aminoacridines,
pubmed-meshheading:8519521-Analysis of Variance,
pubmed-meshheading:8519521-Animals,
pubmed-meshheading:8519521-Behavior, Animal,
pubmed-meshheading:8519521-Cholinesterase Inhibitors,
pubmed-meshheading:8519521-Exploratory Behavior,
pubmed-meshheading:8519521-Memory,
pubmed-meshheading:8519521-Metallothionein,
pubmed-meshheading:8519521-Mice,
pubmed-meshheading:8519521-Neuroblastoma,
pubmed-meshheading:8519521-Neurotoxins,
pubmed-meshheading:8519521-Neutral Red,
pubmed-meshheading:8519521-Oxidation-Reduction,
pubmed-meshheading:8519521-Scopolamine Hydrobromide,
pubmed-meshheading:8519521-Structure-Activity Relationship,
pubmed-meshheading:8519521-Tacrine,
pubmed-meshheading:8519521-Tumor Cells, Cultured
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pubmed:year |
1995
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pubmed:articleTitle |
Potential neurotoxicity of a novel aminoacridine analogue.
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pubmed:affiliation |
CellTox Centre, University of Hertfordshire, Hatfield, Herts, UK.
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pubmed:publicationType |
Journal Article,
Comparative Study
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