Abstract
A series of 3-substituted, 3-(4-pyridinylmethyl)-1,3-dihydro-1-phenyl-2H-indol-2-ones was synthesized and found to enhance the stimulus-induced release of neurotransmitter acetylcholine (AcCh), and by doing so, might be useful in treating cognitive disorders where the level of this neurotransmitter may be diminished in the brain, as in Alzheimer's disease. An attempt has been made to correlate the structure of the 3-substitution with the ability of the compounds to enhance the release of AcCh from the striatum region of rat brain preparations.
MeSH terms
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Acetylcholine / metabolism*
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Alzheimer Disease / drug therapy
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Amnesia / etiology
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Amnesia / physiopathology
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Animals
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Avoidance Learning / drug effects
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Avoidance Learning / physiology
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Corpus Striatum / drug effects
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Corpus Striatum / metabolism
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Hypoxia
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology
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Male
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Rats
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Rats, Wistar
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Indoles
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Pyridines
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2,3-dihydro-2-oxo-1-phenyl-3-(4-pyridinylmethyl)-1H-indole-3-butanoic acid ethyl ester
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2,3-dihydro-2-oxo 1-phenyl-3-(4-pyridinylmethyl)-1H-indole-3-pentanenitrile
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linopirdine
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Acetylcholine