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Vol. 57, Issue 4, 659-666, April 2000
1B- and 1D-Adrenoceptors by
Agonists and Inverse Agonists
The Department of Pharmacology (S.E.E., D.F.M., J.R.O., M.T.P.) and
the Vascular Biology Research Group (S.E.E., D.F.M., J.R.O., M.T.P.,
G.R.P., B.A.W.), The University of Kentucky College of Medicine, The
Division of Pharmaceutical Sciences (G.R.P., B.A.W.), The University of
Kentucky College of Pharmacy, Lexington, Kentucky; and The Department
of Molecular Cardiology, Lerner Research Institute, The Cleveland
Clinic Foundation, Cleveland, Ohio (D.M.P., D.J.J.W.)
The regulation of the cellular distribution and intracellular signaling
properties of the 
1B- and 1D-
adrenoceptor (1-AR) subtypes was examined in stably
transfected Rat 1 fibroblasts. In unstimulated cells,
1B-AR expression was noted primarily on the cell
surface. Treatment with phenylephrine induced internalization of the
1B-AR and promoted association with arrestin 2. The
internalized 1B-AR colocalized with the transferrin
receptor, an endosomal marker. In unstimulated fibroblasts, the
1D-AR was detected in a perinuclear orientation and was
colocalized with arrestin 2 in a compartment also containing the
transferrin receptor. After treatment with prazosin, which exhibits
inverse agonist properties, the 1D-AR was redistributed
from intracellular sites to the cellular periphery and was no longer
associated with the transferrin receptor or arrestin 2. 1D-AR-expressing cells exhibited a high degree of basal
activity for both inositol phosphate formation and extracellular signal
regulated kinase (ERK), which was reduced by treatment with prazosin.
In these cells, phenylephrine induced a dose-dependent increase in
inositol phosphate formation but had no effect on ERK activity. In
1B -AR-expressing cells, phenylephrine stimulated both
inositol phosphate formation and ERK activity. These data show that: 1)
there are differences in the cellular localization of the
1-AR subtypes; 2) the 1B-AR exhibits
expected G protein-coupled receptor activity regarding cellular
localization, agonist-mediated internalization, and coupling to second
messengers; and 3) the 1D-AR is constitutively active
and, as a result, is localized to intracellular compartments involved
in receptor recycling.
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