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Vol. 282, Issue 3, 1632-1642, 1997
Department of Physiology and Pharmacology, and Center for
Investigative Neuroscience, Bowman Gray School of Medicine, Wake Forest
University, Winston-Salem, North Carolina
Cannabinoid receptor activation of G-proteins can be measured by WIN
55212-2-stimulated [35S]GTP
S binding.
Receptor/transducer amplification factors, interpreted as the number of
G-proteins activated per occupied receptor, are the ratio of the
apparent Bmax of net agonist-stimulated
[35S]GTPS binding to the Bmax
of receptor binding. The present study examined whether amplification
factors for cannabinoid receptors differ among various rat brain
regions. In autoradiographic studies with [3H]WIN
55212-2 and WIN 55212-2-stimulated [35S]GTPS
binding, some regions displayed different relative levels of
agonist-stimulated [35S]GTPS binding than receptor
binding. To quantify amplification factors, membranes from different
brain regions were assayed by saturation binding analysis of
net WIN 55212-2-stimulated [35S]GTPS,
[3H]SR141716A (antagonist) and [3H]WIN
55212-2 (agonist) binding. For [3H]SR141716A binding,
amplification factors varied significantly from 2.0 (frontal cortex) to
7.5 (hypothalamus). For [3H]WIN 55212-2 binding,
amplification factors ranged from 2.4 (hippocampus) to 5.5 (thalamus).
Comparison of receptor binding and G-protein activation at
subsaturating concentrations of WIN 55212-2 indicated that
amplification factors may vary with receptor occupancy in some regions
like cerebellum. Ratios between high-affinity [3H]WIN
55212-2 Bmax and [3H]SR141716A
Bmax also differed significantly among brain
regions. These results demonstrate that G-protein coupling by
cannabinoid receptors differs among brain regions, and therefore
depends on the cellular environment.
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