Abstract
Chemical and biological strategies have provided evidence for alpha(2)-receptor heterogeneity, to date classified in three different subtypes, alpha(2A), alpha(2B), and alpha(2C). These are widely distributed throughout the body and mediate numerous effects; therefore, the potential therapeutic indications of agonists and antagonists are numerous. Nevertheless, the lack of subtype-selectivity of the well-known compounds represents a major limit for their use. SAR studies may help to design new and more selective drugs.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Adrenergic alpha-2 Receptor Agonists*
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Adrenergic alpha-2 Receptor Antagonists*
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Adrenergic alpha-Agonists / chemistry
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Adrenergic alpha-Agonists / metabolism
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Adrenergic alpha-Agonists / pharmacology*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / metabolism
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Adrenergic alpha-Antagonists / pharmacology*
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Animals
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Humans
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Receptors, Adrenergic, alpha-2 / classification
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Receptors, Adrenergic, alpha-2 / metabolism
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Adrenergic alpha-2 Receptor Agonists
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Adrenergic alpha-2 Receptor Antagonists
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Adrenergic alpha-Agonists
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Adrenergic alpha-Antagonists
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Receptors, Adrenergic, alpha-2