Expression of three α2-adrenergic receptor subtypes in rat tissues: Implications for α2 receptor classification

W. Lorenz, J. W. Lomasney, S. Collins, J. W. Regan, M. G. Caron, R. J. Lefkowitz

Research output: Contribution to journalArticlepeer-review

130 Scopus citations


Based on biochemical and ligand binding studies in various tissues and species, evidence for several α2-adrenergic receptor subtypes has accumulated. The current α2-adrenergic receptor classification (α(2A), α(2B), α(2C)) is based exclusively on pharmacological criteria. The molecular cloning of three distinct genes for human α2-adrenergic receptors has confirmed the existence of multiple α2-adrenergic receptor subtypes. According to their localization on different human chromosomes, the receptor genes were termed α2-C10, α2-C4, and α2-C2. The relationship, however, between the pharmacologically characterized α2-adrenergic receptors and the isolated genes has yet to be clarified. Using Northern blot hybridization, we analyzed the expression of the three cloned α2-adrenergic receptor genes in 13 rat tissues, as well as in cell lines previously described as model systems for the pharmacologically defined α2-adrenergic receptor subtypes. The α2-C10 receptor corresponds to the α(2A) subtype and is expressed in rat brainstem, cerebral cortex, hippocampus, pituitary gland, cerebellum, kidney, aorta, skeletal muscle, spleen, and lung. Messenger RNA coding for the α2-C4 receptor was detected only in brain regions, not in peripheral tissues, whereas the α2-C2 message was found only in liver and kidney. Hybridization experiments with RNA derived from tissues and cells from which the pharmacological α2-receptor classification has been developed lead to the conclusion that the α(2B) subtype represents two distinct receptor molecules, the α2-C4 and a subtype previously undetected by classical ligand binding approaches. Furthermore, our results suggest that the α(2C) subtype characterized in opossum kidney cells is an interspecies variation of α2-C4 rather than a separate subtype. Finally, the cloned α2-C2 receptor was found to be 'α(2B)-like' and not covered by the current pharmacological classification.

Original languageEnglish (US)
Pages (from-to)599-603
Number of pages5
JournalMolecular pharmacology
Issue number5
StatePublished - 1990

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology


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