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Neonatal rat pinealocytes: typical and atypical characteristics of [125I]iodohydroxybenzylpindolol binding and adenosine 3',5'-monophosphate accumulation.

Publication ,  Journal Article
Auerbach, DA; Klein, DC; Woodard, C; Aurbach, GD
Published in: Endocrinology
February 1981

Techniques are described which make it possible to study beta-adrenergic receptors on intact neuroendocrine cells. Receptors were characterized on neonatal pinealocytes using the radioligand [125I]iodohydroxybenzylpindolol ([125I]IHYP). Specific binding of [125I]IHYP, which is 4-fold greater than nonspecific binding, is concentration and temperature dependent, reversible, and saturable. [125I]IHYP binds noncooperatively (Kd = 35 pM), and Scatchard analysis indicates that only a single class of receptor sites for [125I]IHYP is present. Under the conditions used, it appears that there are about 12,000 +/- 1,100 sites/cell. Inhibition of specific [125I]IHYP binding by beta-adrenergic agonists and antagonists is stereospecific, and the relative potency of agonists is characteristic of binding to beta-adrenergic receptors. Analysis of adrenergic stimulation of intracellular cAMP accumulation indicates that similar half-maximal concentrations of antagonists inhibit [125I]IHYP binding and adrenergically stimulated cAMP accumulation. In contrast, beta-adrenergic agonists are considerably more potent in stimulating cAMP than in inhibiting [125I]IHYP binding. Unexpected differences, not previously reportd, were found in the shapes of the cAMP accumulation dose-response curves of norepinephrine and isoproterenol. The relative potencies of these two agonists appear to be partially concentration dependent. This raises the possibility that there may be distinct differences in the intrinsic effects of these compounds on the regulation of intracellular cAMP accumulation in pinealocytes. (Endocrinology 108: 559, 1981)

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Published In

Endocrinology

DOI

ISSN

0013-7227

Publication Date

February 1981

Volume

108

Issue

2

Start / End Page

559 / 567

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Rats
  • Propranolol
  • Pineal Gland
  • Pindolol
  • Phenylephrine
  • Oxprenolol
  • Norepinephrine
  • Kinetics
 

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Auerbach, D. A., Klein, D. C., Woodard, C., & Aurbach, G. D. (1981). Neonatal rat pinealocytes: typical and atypical characteristics of [125I]iodohydroxybenzylpindolol binding and adenosine 3',5'-monophosphate accumulation. Endocrinology, 108(2), 559–567. https://doi.org/10.1210/endo-108-2-559
Auerbach, D. A., D. C. Klein, C. Woodard, and G. D. Aurbach. “Neonatal rat pinealocytes: typical and atypical characteristics of [125I]iodohydroxybenzylpindolol binding and adenosine 3',5'-monophosphate accumulation.Endocrinology 108, no. 2 (February 1981): 559–67. https://doi.org/10.1210/endo-108-2-559.
Auerbach, D. A., et al. “Neonatal rat pinealocytes: typical and atypical characteristics of [125I]iodohydroxybenzylpindolol binding and adenosine 3',5'-monophosphate accumulation.Endocrinology, vol. 108, no. 2, Feb. 1981, pp. 559–67. Pubmed, doi:10.1210/endo-108-2-559.
Journal cover image

Published In

Endocrinology

DOI

ISSN

0013-7227

Publication Date

February 1981

Volume

108

Issue

2

Start / End Page

559 / 567

Location

United States

Related Subject Headings

  • Receptors, Adrenergic, beta
  • Receptors, Adrenergic
  • Rats
  • Propranolol
  • Pineal Gland
  • Pindolol
  • Phenylephrine
  • Oxprenolol
  • Norepinephrine
  • Kinetics