JPET Assistant Professor of Medicine (Clinician-Educator)

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Right arrow Citation Map
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Daly, C. J.
Right arrow Articles by Mcgrath, J. C.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Daly, C. J.
Right arrow Articles by Mcgrath, J. C.

Vol. 286, Issue 2, 984-990, August 1998

Cellular Localization and Pharmacological Characterization of Functioning Alpha-1 Adrenoceptors by Fluorescent Ligand Binding and Image Analysis Reveals Identical Binding Properties of Clustered and Diffuse Populations of Receptors1

C. J. Daly, C. M. Milligan, G. Milligan, J. F. Mackenzie and J. C. Mcgrath

Clinical Research Initiative and Division of Neuroscience and Biomedical Systems (C.J.D., J.F.M., J.C.M.) and Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology (G.M.), Institute of Biomedical and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, and Quintiles Scotland Ltd., Inchwood, Bathgate, Scotland (C.M.M.)

A fluorescent quinazoline derivative was shown to retain high affinity for, and act as a competitive antagonist at, alpha-1 adrenoceptors. This allowed it to be used in live cells to localize receptors and to quantify receptor binding characteristics. The technique was demonstrated and validated on fibrobasts transfected with a recombinant alpha-1d adrenoceptor. Using confocal laser scanning microscopy and image analysis methods both diffuse and clustered binding sites were found: their binding characteristics were assessed and found comparable to radioligand binding on membrane preparations. This approach should have widespread applicability in nonradioactive assays determining the location, quantity and binding properties of receptors and other biological molecules on live tissue.

0022-3565/98/2862-0984$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 1998 by The American Society for Pharmacology and Experimental Therapeutics


This article has been cited by other articles:


Home page
 Mol Hum ReprodHome page
M. T.C.C. Patrao, D. B.C. Queiroz, G. Grossman, P. Petrusz, M. d. F. M. Lazari, and M. C. W. Avellar
Cloning, expression and immunolocalization of {alpha}1-adrenoceptor in different tissues from rhesus monkey and human male reproductive tract
Mol. Hum. Reprod., February 1, 2008; 14(2): 85 - 96.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
M. M. Shafaroudi, M. McBride, C. Deighan, A. Wokoma, J. Macmillan, C. J. Daly, and J. C. McGrath
Two "Knockout" Mouse Models Demonstrate That Aortic Vasodilatation Is Mediated via {alpha}2A-Adrenoceptors Located on the Endothelium
J. Pharmacol. Exp. Ther., August 1, 2005; 314(2): 804 - 810.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
M. A. Uberti, C. Hague, H. Oller, K. P. Minneman, and R. A. Hall
Heterodimerization with {beta}2-Adrenergic Receptors Promotes Surface Expression and Functional Activity of {alpha}1D-Adrenergic Receptors
J. Pharmacol. Exp. Ther., April 1, 2005; 313(1): 16 - 23.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
J. D. Pediani, J. F. Colston, D. Caldwell, G. Milligan, C. J. Daly, and J. C. McGrath
{beta}-Arrestin-Dependent Spontaneous {alpha}1a-Adrenoceptor Endocytosis Causes Intracellular Transportation of {alpha}-Blockers via Recycling Compartments
Mol. Pharmacol., April 1, 2005; 67(4): 992 - 1004.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
D. P. Morris, R. R. Price, M. P. Smith, B. Lei, and D. A. Schwinn
Cellular Trafficking of Human {alpha}1a-Adrenergic Receptors Is Continuous and Primarily Agonist-Independent
Mol. Pharmacol., October 1, 2004; 66(4): 843 - 854.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
D. Ramsay, I. C. Carr, J. Pediani, J. F. Lopez-Gimenez, R. Thurlow, M. Fidock, and G. Milligan
High-Affinity Interactions between Human {alpha}1A-Adrenoceptor C-Terminal Splice Variants Produce Homo- and Heterodimers but Do Not Generate the {alpha}1L-Adrenoceptor
Mol. Pharmacol., August 1, 2004; 66(2): 228 - 239.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
M. A. Uberti, R. A. Hall, and K. P. Minneman
Subtype-Specific Dimerization of {alpha}1-Adrenoceptors: Effects on Receptor Expression and Pharmacological Properties
Mol. Pharmacol., December 1, 2003; 64(6): 1379 - 1390.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
J. F. Mackenzie, C. J. Daly, J. D. Pediani, and J. C. McGrath
Quantitative Imaging in Live Human Cells Reveals Intracellular alpha 1-Adrenoceptor Ligand-Binding Sites
J. Pharmacol. Exp. Ther., August 1, 2000; 294(2): 434 - 443.
[Abstract] [Full Text]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1998 by the American Society for Pharmacology and Experimental Therapeutics.