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Pharmacological Modulation of Brain Nicotinic Binding Sites.
Nicotinic Acetylcholine Receptors in the Nervous System, NATO ASI Series 1988;():299-316
Information was summarized concerning nicotinic acetylcholine receptor modulation following repeated exposure to anticholinesterase compounds and nicotine (54115). Several studies have examined the effects of repeated nicotine administration on brain nicotinic receptors, particularly in an attempt to determine whether alteration of these sites would be important in developing tolerance to nicotine. Most investigators determined an increase in brain nicotine receptors. Repeated treatments with nicotinic agonist cytisin increased the acetylcholine binding in rat cerebral cortex, due to an increase in the density of nicotinic binding sites with no changes in affinity. The effect of prenatal nicotine exposure was most prominent during the second postnatal week and was most persistent in the cerebellum with only minor effects in the cerebral cortex. An important aspect of receptor modulation was the correlation of the observed biochemical alterations with changes in the behavioral effects of nicotine. The enhanced behavioral effect of nicotine after repeated exposure was linked to the observed increase in brain nicotinic cholinergic receptors. According to the author, knowledge concerning the in-vivo pharmacological regulation of brain nicotinic binding sites is still limited. Such binding sites are relevant to the mechanisms underlying tolerance and dependence to nicotine.
NIOSH-Publication; NIOSH-Grant; Grants-other; Enzyme-activity; Nervous-system-disorders; Neurotransmitters; Neurotoxic-effects; Central-nervous-system
Environmental Health University of Washington Dept of Environ Hlth, SC-34 Seattle, WA 98195
Other Occupational Concerns; Grants-other; Neurotoxic Disorders; Neurotoxic-effects
Nicotinic Acetylcholine Receptors in the Nervous System, NATO ASI Series
University of Washington, Seattle, Washington
Page last reviewed: September 2, 2020
Content source: National Institute for Occupational Safety and Health Education and Information Division