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Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes. 2007

Francesco Gentili, and Maria Pigini, and Alessandro Piergentili, and Mario Giannella
Department of Chemical Sciences, University of Camerino, via S. Agostino 1, 62032 Camerino, Italy.

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.

UI MeSH Term Description Entries
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000316 Adrenergic alpha-Agonists Drugs that selectively bind to and activate alpha adrenergic receptors. Adrenergic alpha-Receptor Agonists,alpha-Adrenergic Receptor Agonists,Adrenergic alpha-Agonist,Adrenergic alpha-Receptor Agonist,Receptor Agonists, Adrenergic alpha,Receptor Agonists, alpha-Adrenergic,alpha-Adrenergic Agonist,alpha-Adrenergic Agonists,alpha-Adrenergic Receptor Agonist,Adrenergic alpha Agonist,Adrenergic alpha Agonists,Adrenergic alpha Receptor Agonist,Adrenergic alpha Receptor Agonists,Agonist, Adrenergic alpha-Receptor,Agonist, alpha-Adrenergic,Agonist, alpha-Adrenergic Receptor,Agonists, Adrenergic alpha-Receptor,Agonists, alpha-Adrenergic,Agonists, alpha-Adrenergic Receptor,Receptor Agonist, alpha-Adrenergic,Receptor Agonists, alpha Adrenergic,alpha Adrenergic Agonist,alpha Adrenergic Agonists,alpha Adrenergic Receptor Agonist,alpha Adrenergic Receptor Agonists,alpha-Agonist, Adrenergic,alpha-Agonists, Adrenergic,alpha-Receptor Agonist, Adrenergic,alpha-Receptor Agonists, Adrenergic
D000317 Adrenergic alpha-Antagonists Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma. Adrenergic alpha-Receptor Blockaders,alpha-Adrenergic Blocking Agents,alpha-Adrenergic Receptor Blockaders,alpha-Blockers, Adrenergic,Adrenergic alpha-Blockers,alpha-Adrenergic Antagonists,alpha-Adrenergic Blockers,Adrenergic alpha Antagonists,Adrenergic alpha Blockers,Adrenergic alpha Receptor Blockaders,Agents, alpha-Adrenergic Blocking,Antagonists, alpha-Adrenergic,Blockaders, Adrenergic alpha-Receptor,Blockaders, alpha-Adrenergic Receptor,Blockers, alpha-Adrenergic,Blocking Agents, alpha-Adrenergic,Receptor Blockaders, alpha-Adrenergic,alpha Adrenergic Antagonists,alpha Adrenergic Blockers,alpha Adrenergic Blocking Agents,alpha Adrenergic Receptor Blockaders,alpha Blockers, Adrenergic,alpha-Antagonists, Adrenergic,alpha-Receptor Blockaders, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D013379 Substrate Specificity A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts. Specificities, Substrate,Specificity, Substrate,Substrate Specificities
D058647 Adrenergic alpha-2 Receptor Agonists Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. Adrenergic alpha-2 Agonists,Adrenergic alpha-2 Receptor Agonist,Adrenergic alpha2-Agonists,Adrenergic alpha 2 Agonists,Adrenergic alpha 2 Receptor Agonist,Adrenergic alpha 2 Receptor Agonists,Adrenergic alpha2 Agonists,Agonists, Adrenergic alpha-2,alpha-2 Agonists, Adrenergic,alpha2-Agonists, Adrenergic
D058669 Adrenergic alpha-2 Receptor Antagonists Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS. Adrenergic alpha-2 Antagonists,Adrenergic alpha-2 Receptor Blockers,Adrenergic alpha2-Antagonists,alpha-2 Adrenergic Blocking Agents,alpha2-Adrenergic Antagonists,Adrenergic alpha 2 Antagonists,Adrenergic alpha 2 Receptor Antagonists,Adrenergic alpha 2 Receptor Blockers,Adrenergic alpha2 Antagonists,Antagonists, Adrenergic alpha-2,Antagonists, alpha2-Adrenergic,alpha 2 Adrenergic Blocking Agents,alpha-2 Antagonists, Adrenergic,alpha2 Adrenergic Antagonists,alpha2-Antagonists, Adrenergic
D018341 Receptors, Adrenergic, alpha-2 A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release. Adrenergic alpha-2 Receptors,Receptors, alpha-2 Adrenergic,alpha-2 Adrenergic Receptors,Adrenergic Receptor alpha(2C),Adrenergic Receptor alpha(2d),Adrenergic Receptor alpha-2C,Adrenergic Receptor alpha-2b,Adrenergic Receptor, alpha-2,Adrenergic alpha-2A Receptors,Adrenergic alpha-2B Receptors,Adrenergic alpha-2C Receptors,Adrenergic alpha-2D Receptors,Receptor, Adrenergic, alpha-2,Receptor, Adrenergic, alpha-2A,Receptor, Adrenergic, alpha-2B,Receptor, Adrenergic, alpha-2C,Receptor, Adrenergic, alpha-2D,Receptors, Adrenergic, alpha-2A,Receptors, Adrenergic, alpha-2B,Receptors, Adrenergic, alpha-2D,alpha 2 Adrenergic Receptors,alpha-2A Adrenergic Receptor,alpha-2B Adrenergic Receptor,alpha-2C Adrenergic Receptor,alpha-2D Adrenergic Receptor,Adrenergic Receptor alpha 2C,Adrenergic Receptor alpha 2b,Adrenergic Receptor, alpha 2,Adrenergic Receptor, alpha-2A,Adrenergic Receptor, alpha-2B,Adrenergic Receptor, alpha-2C,Adrenergic Receptor, alpha-2D,Adrenergic Receptors, alpha-2,Adrenergic alpha 2 Receptors,Adrenergic alpha 2A Receptors,Adrenergic alpha 2B Receptors,Adrenergic alpha 2C Receptors,Adrenergic alpha 2D Receptors,Receptor alpha-2C, Adrenergic,Receptor alpha-2b, Adrenergic,Receptor, alpha-2 Adrenergic,Receptor, alpha-2A Adrenergic,Receptor, alpha-2B Adrenergic,Receptor, alpha-2C Adrenergic,Receptor, alpha-2D Adrenergic,Receptors, Adrenergic alpha-2,Receptors, Adrenergic alpha-2A,Receptors, Adrenergic alpha-2B,Receptors, Adrenergic alpha-2C,Receptors, Adrenergic alpha-2D,Receptors, alpha 2 Adrenergic,alpha 2A Adrenergic Receptor,alpha 2B Adrenergic Receptor,alpha 2C Adrenergic Receptor,alpha 2D Adrenergic Receptor,alpha-2 Adrenergic Receptor,alpha-2 Receptors, Adrenergic,alpha-2A Receptors, Adrenergic,alpha-2B Receptors, Adrenergic,alpha-2C Receptors, Adrenergic,alpha-2C, Adrenergic Receptor,alpha-2D Receptors, Adrenergic,alpha-2b, Adrenergic Receptor

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