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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1985-8-9
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pubmed:abstractText |
Alpha adrenergic receptors are subdivided into alpha-1 and alpha-2 subtypes on the basis of their pharmacologic properties. An evaluation of data from radioligand binding and functional experiments indicates that the receptors classified as alpha-2 are not a homogeneous group. The best example of this heterogeneity is the differences in the pharmacologic properties of alpha-2 receptors in rodent and non-rodent mammalian species. Prazosin generally has a high affinity for rodent alpha-2 receptors, but a low affinity for non-rodent alpha-2 receptors, while oxymetazoline is more potent at non-rodent alpha-2 receptors. A definition of alpha-2 adrenergic receptor subtypes is proposed with prazosin having a lower affinity (200-300 nM) at alpha-2A receptors and a higher affinity (5-10 nM) at alpha-2B receptors. Using this definition, the human platelet appears to have only the alpha-2A subtype, while all the receptors in the neonatal rat lung are of the alpha-2B subtype. The rat brain has roughly equal amounts of alpha-2A and -2B receptors while in the rat submandibular gland, about 85% of the receptors are alpha-2A. The ability to pharmacologically define putative alpha-2 adrenergic receptor subtypes should promote the development of additional subtype selective drugs which will increase our understanding of adrenergic pharmacology and may provide new therapeutic approaches.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Oxymetazoline,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0091-3057
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
22
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
835-43
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:2989948-Animals,
pubmed-meshheading:2989948-Blood Platelets,
pubmed-meshheading:2989948-Brain,
pubmed-meshheading:2989948-Cerebral Cortex,
pubmed-meshheading:2989948-Clonidine,
pubmed-meshheading:2989948-Corpus Striatum,
pubmed-meshheading:2989948-Dogs,
pubmed-meshheading:2989948-Guinea Pigs,
pubmed-meshheading:2989948-Humans,
pubmed-meshheading:2989948-Oxymetazoline,
pubmed-meshheading:2989948-Prazosin,
pubmed-meshheading:2989948-Radioligand Assay,
pubmed-meshheading:2989948-Rats,
pubmed-meshheading:2989948-Receptors, Adrenergic, alpha,
pubmed-meshheading:2989948-Species Specificity,
pubmed-meshheading:2989948-Submandibular Gland,
pubmed-meshheading:2989948-Yohimbine
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pubmed:year |
1985
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pubmed:articleTitle |
Heterogeneity of alpha-2 adrenergic receptors.
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pubmed:publicationType |
Journal Article,
Review
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