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In vivo regulation of [3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs.

Publication ,  Journal Article
Schwartz, RD; Kellar, KJ
Published in: J Neurochem
August 1985

The in vivo regulation of [3H]acetylcholine [( 3H]ACh) recognition sites on nicotinic receptors in rat brain was examined by administering drugs that increase stimulation of nicotinic cholinergic receptors, either directly or indirectly. After 10 days of treatment with the cholinesterase inhibitor diisopropyl fluorophosphate, [3H]ACh binding in the cortex, thalamus, striatum, and hypothalamus was decreased. Scatchard analyses indicated that the decrease in binding in the cortex was due to a reduction in the apparent density of [3H]ACh recognition sites. In contrast, after repeated administration of nicotine (5-21 days), the number of [3H]ACh recognition sites was increased in the cortex, thalamus, striatum, and hypothalamus. Similar effects were observed in the cortex and thalamus following repeated administration of the nicotinic agonist cytisin. The nicotinic antagonists mecamylamine and dihydro-beta-erythroidine did not alter [3H]ACh binding following 10-14 days of administration. Further, concurrent treatment with these antagonists and nicotine did not prevent the nicotine-induced increase in these binding sites. The data indicate that [3H]ACh recognition sites on nicotinic receptors are subject to up- and down-regulation, and that repeated administration of nicotine results in a signal for up-regulation, probably through protracted desensitization at the recognition site.

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Published In

J Neurochem

DOI

ISSN

0022-3042

Publication Date

August 1985

Volume

45

Issue

2

Start / End Page

427 / 433

Location

England

Related Subject Headings

  • Thalamus
  • Receptors, Muscarinic
  • Receptors, Cholinergic
  • Rats, Inbred Strains
  • Rats
  • Quinuclidinyl Benzilate
  • Quinolizines
  • Nicotine
  • Neurology & Neurosurgery
  • Mecamylamine
 

Citation

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Schwartz, R. D., & Kellar, K. J. (1985). In vivo regulation of [3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs. J Neurochem, 45(2), 427–433. https://doi.org/10.1111/j.1471-4159.1985.tb04005.x
Schwartz, R. D., and K. J. Kellar. “In vivo regulation of [3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs.J Neurochem 45, no. 2 (August 1985): 427–33. https://doi.org/10.1111/j.1471-4159.1985.tb04005.x.
Schwartz, R. D., and K. J. Kellar. “In vivo regulation of [3H]acetylcholine recognition sites in brain by nicotinic cholinergic drugs.J Neurochem, vol. 45, no. 2, Aug. 1985, pp. 427–33. Pubmed, doi:10.1111/j.1471-4159.1985.tb04005.x.
Journal cover image

Published In

J Neurochem

DOI

ISSN

0022-3042

Publication Date

August 1985

Volume

45

Issue

2

Start / End Page

427 / 433

Location

England

Related Subject Headings

  • Thalamus
  • Receptors, Muscarinic
  • Receptors, Cholinergic
  • Rats, Inbred Strains
  • Rats
  • Quinuclidinyl Benzilate
  • Quinolizines
  • Nicotine
  • Neurology & Neurosurgery
  • Mecamylamine