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(Investigative Ophthalmology and Visual Science. 1999;40:2299-2306.)
© 1999 by The Association for Research in Vision and Ophthalmology, Inc.

Characterization of {alpha}2 Adrenergic Receptor Subtypes in Human Ocular Tissue Homogenates

David B. Bylund1 and David M. Chacko2

From the Departments of 1 Pharmacology and 2 Ophthalmology, University of Nebraska Medical Center, Omaha.

Abstract

PURPOSE. To determine the predominant {alpha}2 adrenergic receptor subtypes present in the human eye.

METHODS. Saturation- and competition-receptor–binding experiments were performed with the radioligand [3H]RX821002 in human ciliary body, retinal pigmented epithelium–choriocapillaris, iris, and neurosensory retina. The affinities of various adrenergic antagonists in these ocular tissues were compared with their affinities for the cloned {alpha}2A, {alpha}2B, and {alpha}2C adrenergic receptor subtypes.

RESULTS. The density of {alpha}2 adrenergic receptors was highest in the iris (440 femtomoles/mg protein), lowest in the neurosensory retina (14 femtomoles/mg protein), and intermediate in the other two tissues (approximately 90 fmol/mg protein). The drug affinities in all four human ocular tissues were highly correlated (correlation coefficients between 0.94 and 0.97) with the affinities for the human {alpha}2A adrenergic receptor subtype and poorly correlated (correlation coefficients between 0.15 and 0.66) with the {alpha}2B and {alpha}2C subtypes.

CONCLUSIONS. In agreement with previous studies in several animal species, the {alpha}2 adrenergic receptors in the human ciliary body, retinal pigmented epithelium–choriocapillaris, iris, and neurosensory retina are predominately of the {alpha}2A subtype.




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