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Summary: insight review articles
206 NATURE | VOL 415 | 10 JANUARY 2002 | www.nature.com
T
he family of G-protein-coupled receptors
(GPCRs) contain a conserved structure of seven
transmembrane -helices. Of these receptors, the
adrenergic receptors and muscarinic cholinergic
receptors are particularly important for the heart
because they function in the homeostatic regulation of the
cardiovascular system. The adrenergic receptors have been
well studied and are the targets for many pharmaceuticals,
such as the - and -blockers that are used widely to treat
hypertension and myocardial diseases1
.
At least nine subtypes of adrenergic receptors have been
cloned, including three 1-, three 2- and three -adrener-
gic receptors (ARs)1
. In the heart, the 1-AR is the most
predominant subtype, comprising 7580% of total -ARs;
in contrast, there are only a small number of -ARs, with a
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