Central Hypotensive Effects of the α 2a -Adrenergic Receptor Subtype

α 2 -Adrenergic receptors (α 2 ARs) present in the brainstem decrease blood pressure and are targets for clinically effective antihypertensive drugs. The existence of three α 2 AR subtypes, the lack of subtype-specific ligands, and the cross-reactivity of α 2 AR agonists with imidazoline receptors h...

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Bibliographic Details
Published in:Science (American Association for the Advancement of Science) 1996-08, Vol.273 (5276), p.801-803
Main Authors: MacMillan, Leigh B., Hein, Lutz, Smith, Marta S., Piascik, Michael T., Limbird, Lee E.
Format: Article
Language:English
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Summary:α 2 -Adrenergic receptors (α 2 ARs) present in the brainstem decrease blood pressure and are targets for clinically effective antihypertensive drugs. The existence of three α 2 AR subtypes, the lack of subtype-specific ligands, and the cross-reactivity of α 2 AR agonists with imidazoline receptors has precluded an understanding of the role of individual α 2 AR subtypes in the hypotensive response. Gene targeting was used to introduce a point mutation into the α 2a AR subtype in the mouse genome. The hypotensive response to α 2 AR agonists was lost in the mutant mice, demonstrating that the α 2a AR subtype plays a principal role in this response.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.273.5276.801