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 receptors

Daly, C.J. , Milligan, C.M., Milligan, G. , Mackenzie, J.F. and McGrath, J.C. (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 receptors. Journal of Pharmacology and Experimental Therapeutics, 286(2), pp. 984-990.

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Publisher's URL: http://jpet.aspetjournals.org/content/286/2/984.abstract

Abstract

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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:McGrath, Professor John and Daly, Dr Craig and Milligan, Professor Graeme
Authors: Daly, C.J., Milligan, C.M., Milligan, G., Mackenzie, J.F., and McGrath, J.C.
College/School:College of Medical Veterinary and Life Sciences > Institute of Molecular Cell and Systems Biology
College of Medical Veterinary and Life Sciences > School of Life Sciences
Journal Name:Journal of Pharmacology and Experimental Therapeutics
Publisher:American Society for Pharmacology and Experimental Therapeutics
ISSN:0022-3565
ISSN (Online):1521-0103

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