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Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling.

Publication ,  Journal Article
Dickinson, KE; Leeb-Lundberg, LM; Strasser, RH; Caron, MG; Lefkowitz, RJ
Published in: J Neurochem
April 1986

The adrenergic receptors of rat pineal gland were investigated using radiolabeled ligand binding and photoaffinity labeling techniques. 125I-2-[beta-(4-hydroxyphenyl)ethylaminomethyl]tetralone (125I-HEAT) and 125I-cyanopindolol (125I-CYP) labeled specific sites on rat pineal gland membranes with equilibrium dissociation constants (KD) of 48 (+/- 5) pM and 30 (+/- 5) pM, respectively. Binding site maxima were 481 (+/- 63) and 1,020 (+/- 85) fmol/mg protein. The sites labeled by 125I-HEAT had the pharmacological characteristics of alpha 1-adrenergic receptors. 125I-CYP-labeled beta-adrenergic receptors were characterized as a homogeneous population of beta 1-adrenergic receptors. The alpha 1- and beta 1-adrenergic receptors were covalently labeled with the specific photoaffinity probes 4-amino-6,7-dimethoxy-2-(4-[5-(4-azido-3-[125I]iodophenyl) pentanoyl]-1-piperazinyl) quinazoline (125I-APDQ) and 125I-p-azidobenzylcarazolol (125I-pABC). 125I-APDQ labeled an alpha 1-adrenergic receptor peptide of Mr = 74,000 (+/- 4,000), which was similar to peptides labeled in rat cerebral cortex, liver, and spleen. 125I-pABC labeled a single beta 1-adrenergic receptor peptide with a Mr = 42,000 (+/- 1,500), which differed from the 60-65,000 peptide commonly seen in mammalian tissues. Possible reasons for these differences are discussed.

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Published In

J Neurochem

DOI

ISSN

0022-3042

Publication Date

April 1986

Volume

46

Issue

4

Start / End Page

1153 / 1160

Location

England

Related Subject Headings

  • Tetralones
  • Spleen
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, alpha
  • Rats
  • Propanolamines
  • Pineal Gland
  • Pindolol
  • Photochemistry
  • Phenethylamines
 

Citation

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Dickinson, K. E., Leeb-Lundberg, L. M., Strasser, R. H., Caron, M. G., & Lefkowitz, R. J. (1986). Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling. J Neurochem, 46(4), 1153–1160. https://doi.org/10.1111/j.1471-4159.1986.tb00630.x
Dickinson, K. E., L. M. Leeb-Lundberg, R. H. Strasser, M. G. Caron, and R. J. Lefkowitz. “Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling.J Neurochem 46, no. 4 (April 1986): 1153–60. https://doi.org/10.1111/j.1471-4159.1986.tb00630.x.
Dickinson KE, Leeb-Lundberg LM, Strasser RH, Caron MG, Lefkowitz RJ. Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling. J Neurochem. 1986 Apr;46(4):1153–60.
Dickinson, K. E., et al. “Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling.J Neurochem, vol. 46, no. 4, Apr. 1986, pp. 1153–60. Pubmed, doi:10.1111/j.1471-4159.1986.tb00630.x.
Dickinson KE, Leeb-Lundberg LM, Strasser RH, Caron MG, Lefkowitz RJ. Identification of the subunit structure of rat pineal adrenergic receptors by photoaffinity labeling. J Neurochem. 1986 Apr;46(4):1153–1160.
Journal cover image

Published In

J Neurochem

DOI

ISSN

0022-3042

Publication Date

April 1986

Volume

46

Issue

4

Start / End Page

1153 / 1160

Location

England

Related Subject Headings

  • Tetralones
  • Spleen
  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic, alpha
  • Rats
  • Propanolamines
  • Pineal Gland
  • Pindolol
  • Photochemistry
  • Phenethylamines