Central Hypotensive Effects of the α2a-Adrenergic Receptor Subtype

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Science  09 Aug 1996:
Vol. 273, Issue 5276, pp. 801-803
DOI: 10.1126/science.273.5276.801


α2-Adrenergic receptors (α2ARs) present in the brainstem decrease blood pressure and are targets for clinically effective antihypertensive drugs. The existence of three α2AR subtypes, the lack of subtype-specific ligands, and the cross-reactivity of α2AR agonists with imidazoline receptors has precluded an understanding of the role of individual α2AR subtypes in the hypotensive response. Gene targeting was used to introduce a point mutation into the α2aAR subtype in the mouse genome. The hypotensive response to α2AR agonists was lost in the mutant mice, demonstrating that the α2aAR subtype plays a principal role in this response.

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