Db. Bylund et al., CHARACTERIZATION OF ALPHA-2D ADRENERGIC-RECEPTOR SUBTYPES IN BOVINE OCULAR TISSUE-HOMOGENATES, The Journal of pharmacology and experimental therapeutics, 281(3), 1997, pp. 1171-1177
The alpha-2 adrenergic receptors are known to be present in the mammal
ian eye and to mediate the effects of alpha-2 agonists used in the tre
atment of glaucoma. Little is known, however, regarding the relative d
ensities of the three alpha-2 subtypes in the various tissues of the e
ye. We used receptor binding experiments with the radioligand [H-3]RX8
21002 to characterize the alpha-2 adrenergic receptors in three tissue
s of the bovine eye, the ciliary body, retinal pigment epithelium/chor
iocapillaris and iris. The K-D values in the three tissues were simila
r (0.12-0.14 nM), and the B-max values ranged from 100 fmol/mg of prot
ein for the ciliary body and retinal pigment epithelium/choriocapillar
is to 200 fmol/mg of protein for the iris. The pharmacological charact
eristics of the alpha-2 receptors in all three tissues of the bovine e
ye, as assessed by competition studies, were essentially identical and
were similar to the characteristics of the alpha-2A/D receptors of th
e bovine neurosensory retina. The correlation coefficients between the
logarithms of the K-i values for the three tissues and the neurosenso
ry retina for nine adrenergic agents were .98 to .99. We conclude that
the alpha-2 adrenergic receptors in the ciliary body, iris and retina
l pigment epithelium/choriocapillaris of the bovine eye are mainly alp
ha-2D.