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Covalent labeling of the cerebral cortex α1-adrenergic receptor with a new high affinity radioiodinated photoaffinity probe

Leeb-Lundberg, L. M.Fredrik LU ; Dickinson, Kenneth E.J. ; Heald, Sarah L. ; Wikberg, Jarl E.S. ; DeBernardis, John F. ; Winn, Marty ; Arendsen, David L. ; Lefkowitz, Robert J. and Caron, Marc G. (1983) In Biochemical and Biophysical Research Communications 115(3). p.946-951
Abstract

A novel high affinity radioiodinated photoaffinity probe, 4-amino-6,7-dimethoxy-2[4-[5(3-[125I]iodo-4-azidophenyl)pentanoyl]-1-piperazinyl]- quinazoline, structurally related to the potent α1-adrenergic antagonist prazosin, was developed and used to covalently label the rat cerebral cortex α1-adrenergic receptor. In the absence of light, this ligand binds to cortex plasma membranes with a dissociation constant of 308 pM and with a maximal number of binding sites of 200 fmol/mg protein. Upon photolysis, the ligand incorporates irreversibly into plasma membrane proteins. Autoradiograms of such membrane samples subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis reveal a major... (More)

A novel high affinity radioiodinated photoaffinity probe, 4-amino-6,7-dimethoxy-2[4-[5(3-[125I]iodo-4-azidophenyl)pentanoyl]-1-piperazinyl]- quinazoline, structurally related to the potent α1-adrenergic antagonist prazosin, was developed and used to covalently label the rat cerebral cortex α1-adrenergic receptor. In the absence of light, this ligand binds to cortex plasma membranes with a dissociation constant of 308 pM and with a maximal number of binding sites of 200 fmol/mg protein. Upon photolysis, the ligand incorporates irreversibly into plasma membrane proteins. Autoradiograms of such membrane samples subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis reveal a major specifically labeled polypeptide at Mr = 79,000. The covalent incorporation into the peptide at Mr = 79,000 can be inhibited by several adrenergic receptor ligands with a typical α1-adrenergic receptor specificity and stereoselectivity.

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author
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publishing date
type
Contribution to journal
publication status
published
subject
in
Biochemical and Biophysical Research Communications
volume
115
issue
3
pages
946 - 951
publisher
Elsevier
external identifiers
  • pmid:6313003
  • scopus:0020627571
ISSN
0006-291X
DOI
10.1016/S0006-291X(83)80026-6
language
English
LU publication?
no
id
3c00b4a5-baa8-4e75-aa5e-aff8042cd402
date added to LUP
2019-06-12 11:53:08
date last changed
2024-01-01 09:55:39
@article{3c00b4a5-baa8-4e75-aa5e-aff8042cd402,
  abstract     = {{<p>A novel high affinity radioiodinated photoaffinity probe, 4-amino-6,7-dimethoxy-2[4-[5(3-[<sup>125</sup>I]iodo-4-azidophenyl)pentanoyl]-1-piperazinyl]- quinazoline, structurally related to the potent α<sub>1</sub>-adrenergic antagonist prazosin, was developed and used to covalently label the rat cerebral cortex α<sub>1</sub>-adrenergic receptor. In the absence of light, this ligand binds to cortex plasma membranes with a dissociation constant of 308 pM and with a maximal number of binding sites of 200 fmol/mg protein. Upon photolysis, the ligand incorporates irreversibly into plasma membrane proteins. Autoradiograms of such membrane samples subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis reveal a major specifically labeled polypeptide at M<sub>r</sub> = 79,000. The covalent incorporation into the peptide at M<sub>r</sub> = 79,000 can be inhibited by several adrenergic receptor ligands with a typical α<sub>1</sub>-adrenergic receptor specificity and stereoselectivity.</p>}},
  author       = {{Leeb-Lundberg, L. M.Fredrik and Dickinson, Kenneth E.J. and Heald, Sarah L. and Wikberg, Jarl E.S. and DeBernardis, John F. and Winn, Marty and Arendsen, David L. and Lefkowitz, Robert J. and Caron, Marc G.}},
  issn         = {{0006-291X}},
  language     = {{eng}},
  month        = {{09}},
  number       = {{3}},
  pages        = {{946--951}},
  publisher    = {{Elsevier}},
  series       = {{Biochemical and Biophysical Research Communications}},
  title        = {{Covalent labeling of the cerebral cortex α<sub>1</sub>-adrenergic receptor with a new high affinity radioiodinated photoaffinity probe}},
  url          = {{http://dx.doi.org/10.1016/S0006-291X(83)80026-6}},
  doi          = {{10.1016/S0006-291X(83)80026-6}},
  volume       = {{115}},
  year         = {{1983}},
}