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[3H]acetylcholine binding sites in brain. Effect of disulfide bond modification.

Publication ,  Journal Article
Schwartz, RD; Kellar, KJ
Published in: Mol Pharmacol
November 1983

Nicotinic cholinergic receptor recognition sites have been measured in rat brain using [3H]acetylcholine. Modification of these sites in vitro with the disulfide bond reducing agent, dithiothreitol, resulted in a decrease in the density (Bmax) of [3H]acetylcholine binding sites while the affinity of these sites was unaltered. Reoxidation of the reduced sites with 5,5'-dithiobis(2-nitrobenzoic acid) reversed the effects of dithiothreitol. The reoxidation effect was partially prevented by p-chloromercuribenzoic acid, which generates thiol complexes with exposed sulfhydryl groups. Reduction of disulfide bonds had no effect on the ability of nicotinic cholinergic agonists or antagonists to compete for the remaining [3H]acetylcholine binding sites. In addition, pretreatment of cortical homogenates with acetylcholine or nicotine did not alter the effects of dithiothreitol on [3H] acetylcholine binding, suggesting that the disulfide bonds which are critical for [3H] acetylcholine binding are not located directly at the recognition site.

Duke Scholars

Published In

Mol Pharmacol

ISSN

0026-895X

Publication Date

November 1983

Volume

24

Issue

3

Start / End Page

387 / 391

Location

United States

Related Subject Headings

  • Receptors, Cholinergic
  • Rats, Inbred Strains
  • Rats
  • Pharmacology & Pharmacy
  • Parasympathomimetics
  • Parasympatholytics
  • Male
  • In Vitro Techniques
  • Dithiothreitol
  • Dithionitrobenzoic Acid
 

Citation

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MLA
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Schwartz, R. D., & Kellar, K. J. (1983). [3H]acetylcholine binding sites in brain. Effect of disulfide bond modification. Mol Pharmacol, 24(3), 387–391.
Schwartz, R. D., and K. J. Kellar. “[3H]acetylcholine binding sites in brain. Effect of disulfide bond modification.Mol Pharmacol 24, no. 3 (November 1983): 387–91.
Schwartz RD, Kellar KJ. [3H]acetylcholine binding sites in brain. Effect of disulfide bond modification. Mol Pharmacol. 1983 Nov;24(3):387–91.
Schwartz, R. D., and K. J. Kellar. “[3H]acetylcholine binding sites in brain. Effect of disulfide bond modification.Mol Pharmacol, vol. 24, no. 3, Nov. 1983, pp. 387–91.
Schwartz RD, Kellar KJ. [3H]acetylcholine binding sites in brain. Effect of disulfide bond modification. Mol Pharmacol. 1983 Nov;24(3):387–391.

Published In

Mol Pharmacol

ISSN

0026-895X

Publication Date

November 1983

Volume

24

Issue

3

Start / End Page

387 / 391

Location

United States

Related Subject Headings

  • Receptors, Cholinergic
  • Rats, Inbred Strains
  • Rats
  • Pharmacology & Pharmacy
  • Parasympathomimetics
  • Parasympatholytics
  • Male
  • In Vitro Techniques
  • Dithiothreitol
  • Dithionitrobenzoic Acid