Our understanding of adrenergic function has advanced considerably in the 15
years since three adrenergic receptor books were published in The Receptors
series. In the late 1980s, many of the adrenergic subtypes had not yet been cloned.
Most of the studies during that time focused on traditional pharmacological
approaches in selected tissues and cell lines. We learned about structure–function
relationships through the manipulation of the drug, not the receptor. We
understood that there were multiple subtypes within each class of adrenergic
receptors, but the functions of the subtypes were unclear because they seemed to
control the same signal transduction and biological processes. Molecular cloning
of the receptors led to the realization that there were many different subtypes,
some not previously described by the tissue pharmacology. With the genes of
these receptors in hand, the field has now advanced with more precise experiments
and questions, but it has still suffered from the lack of highly selective
ligands and antibodies. Foreseeing that these limitations would not be overcome
any time in the near future, scientists in the adrenergic receptor field—using
modern genetic approaches—started to redirect their work to answer questions
about structure and function and the possible physiological and pathophysiological
pathways that would be regulated by adrenergic receptors. The
Adrenergic Receptors: In the 21st Century focuses on these modern approaches
and was written by the scientists who developed them to elucidate adrenergic
An authoritative review of the current state-of-the-art understanding of the structure and function of the adrenergic receptor subtypes, as well as of the role played by these receptors in physiological and pathophysiological settings. Topics range from structure-function studies and the imaging of adrenergic receptors to the use of genetically altered mouse models and pharmacogenomics. Highlights include a survey of the knockout and overexpressed mouse models, a review of the new ways that adrenergic receptors can signal, and the effects of polymorphisms on clinical outcomes and on potential gene therapy applications. The side-by-side comparison of all the adrenergic receptors (a1, a2, and b) provides the reader with an excellent survey of the field, including the rationale for designing better drugs to control blood pressure and heart function.
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