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Gene Review

Adra2a  -  adrenoceptor alpha 2A

Rattus norvegicus

Synonyms: Alpha-2A adrenergic receptor, Alpha-2A adrenoceptor, Alpha-2A adrenoreceptor, Alpha-2AAR, Alpha-2D adrenergic receptor, ...
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Disease relevance of Adra2a


Psychiatry related information on Adra2a


High impact information on Adra2a

  • Basal activity of PLD in membranes was reduced in RG20, a PC12 cell line overexpressing the human alpha2A-adrenergic receptor [2].
  • As internal applications of anti-phosphatidylinositol and anti-alpha q/alpha 11 antibodies had no effect on the alpha 2A-adrenoreceptor-induced enhancement of calcium channel current, these findings suggest that phosphatidylinositol hydrolysis and Gq/G11-protein are not involved in the alpha 2A-adrenoreceptor-induced coupling process [6].
  • Both alpha 1A- and alpha 2A-adrenoreceptor subtypes stimulate voltage-operated L-type calcium channels in rat portal vein myocytes. Evidence for two distinct transduction pathways [6].
  • A protein kinase C inhibitor, GF 109203X, and a long term (24 h) treatment with phorbol dibutyrate to decrease the activity of protein kinase C blocked the alpha 1A- and alpha 2A-adrenoreceptor-induced stimulation of calcium channels as well as that stimulation induced by phorbol dibutyrate [6].
  • In competition binding studies the potency order of competing ligands for RG20 is phentolamine greater than idazoxan greater than yohimbine greater than rauwolscine greater than prazosin [7].

Biological context of Adra2a


Anatomical context of Adra2a


Associations of Adra2a with chemical compounds

  • However, in contrast to RG20, [3H] rauwolscine exhibits a KD of 2 nM for the C-10 receptor, and the potency order for competing ligands is rauwolscine greater than or equal to yohimbine greater than idazoxan greater than phentolamine greater than prazosin [7].
  • The blockade in free water clearance by prazosin indicated a possible role of the alpha 2b-adrenoceptor subtype whereas the alpha 2a-adrenoceptor subtype was considered as the site mediating the clonidine-induced increase in osmolar clearance [13].
  • Our results also show that low concentrations of oxymetazoline (10-300 nM), an alpha 2A-adrenoceptor subtype-selective drug, cause profound inhibition of neuronal activity in the locus coeruleus [14].
  • We examined the effect of intrathecal (i.t.) administration of the non-selective alpha 2-adrenoceptor agonist clonidine and the alpha 2A-adrenoceptor selective agonist guanfacine on flexor reflex excitability in decerebrate, spinalized, unanesthetized rats before and after unilateral section of the sciatic nerve [15].
  • However, the competition curves for guanoxabenz were definitely biphasic and resolved into two site fits, indicating that guanoxabenz was binding to both high affinity (Kd = 35 nmol/l) and low affinity (Kd = 8900 nmol/l) alpha 2A-adrenoceptor sites in the proportions 57% and 43%, respectively [16].

Other interactions of Adra2a


Analytical, diagnostic and therapeutic context of Adra2a


  1. ATP-sensitive K+ channels mediate alpha 2D-adrenergic receptor contraction of arteriolar smooth muscle and reversal of contraction by hypoxia. Tateishi, J., Faber, J.E. Circ. Res. (1995) [Pubmed]
  2. Phospholipase D activity in PC12 cells. Effects of overexpression of alpha2A-adrenergic receptors. Ella, K.M., Qi, C., McNair, A.F., Park, J.H., Wisehart-Johnson, A.E., Meier, K.E. J. Biol. Chem. (1997) [Pubmed]
  3. A negative regulatory element in the promoter region of the rat alpha 2A-adrenergic receptor gene overlaps an SP1 consensus binding site. Handy, D.E., Zanella, M.T., Kanemaru, A., Tavares, A., Flordellis, C., Gavras, H. Biochem. J. (1995) [Pubmed]
  4. Depalmitoylation of rhodopsin with hydroxylamine. Pepperberg, D.R., Morrison, D.F., O'Brien, P.J. Meth. Enzymol. (1995) [Pubmed]
  5. Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats. Birnbaum, S.G., Podell, D.M., Arnsten, A.F. Pharmacol. Biochem. Behav. (2000) [Pubmed]
  6. Both alpha 1A- and alpha 2A-adrenoreceptor subtypes stimulate voltage-operated L-type calcium channels in rat portal vein myocytes. Evidence for two distinct transduction pathways. Leprêtre, N., Mironneau, J., Morel, J.L. J. Biol. Chem. (1994) [Pubmed]
  7. Isolation of rat genomic clones encoding subtypes of the alpha 2-adrenergic receptor. Identification of a unique receptor subtype. Lanier, S.M., Downing, S., Duzic, E., Homcy, C.J. J. Biol. Chem. (1991) [Pubmed]
  8. Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist. Michel, A.D., Loury, D.N., Whiting, R.L. Br. J. Pharmacol. (1990) [Pubmed]
  9. Alpha-2A adrenergic receptor subtype gene expression in the intestines of cocaine-exposed rat embryos. Ward, L.P., Hill, J.M., McCune, S.K. Pediatr. Res. (2002) [Pubmed]
  10. Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors. O'Rourke, M.F., Iversen, L.J., Lomasney, J.W., Bylund, D.B. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  11. Alpha 2-adrenergic receptor subtypes in rat dorsal root and superior cervical ganglion neurons. Gold, M.S., Dastmalchi, S., Levine, J.D. Pain (1997) [Pubmed]
  12. Differences between the alpha 2-adrenoceptor in rat submaxillary gland and the alpha 2A-and alpha 2B-adrenoceptor subtypes. Michel, A.D., Loury, D.N., Whiting, R.L. Br. J. Pharmacol. (1989) [Pubmed]
  13. Clonidine-induced increase in osmolar clearance and free water clearance via activation of two distinct alpha 2-adrenoceptor sites. Intengan, H.D., Smyth, D.D. Br. J. Pharmacol. (1996) [Pubmed]
  14. Action of dexmedetomidine on rat locus coeruleus neurones: intracellular recording in vitro. Chiu, T.H., Chen, M.J., Yang, Y.R., Yang, J.J., Tang, F.I. Eur. J. Pharmacol. (1995) [Pubmed]
  15. The effect of intrathecal guanfacine and clonidine on the flexor reflex in rats with intact and sectioned sciatic nerves. Xu, X.J., Wikberg, J.E., Wiesenfeld-Hallin, Z. Eur. J. Pharmacol. (1993) [Pubmed]
  16. Evidence for the existence of two forms of alpha 2A-adrenoceptors in the rat. Uhlén, S., Xia, Y., Chhajlani, V., Lien, E.J., Wikberg, J.E. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  17. Pharmacological characterization of rat alpha 2-adrenergic receptors. Harrison, J.K., D'Angelo, D.D., Zeng, D.W., Lynch, K.R. Mol. Pharmacol. (1991) [Pubmed]
  18. Enhancement of the expression of the alpha 2-adrenoreceptor protein and mRNA by a direct effect of androgens in white adipocytes. Pecquery, R., Dieudonne, M.N., Cloix, J.F., Leneveu, M.C., Dausse, J.P., Giudicelli, Y. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
  19. Alpha-2 adrenergic agonism stimulates islet glucagon release from perfused rat pancreas: possible involvement of alpha-2A adrenergic receptor subtype. Hirose, H., Maruyama, H., Itoh, K., Koyama, K., Kido, K., Saruta, T. Acta Endocrinol. (1992) [Pubmed]
  20. Dexmedetomidine enhances analgesic action of nitrous oxide: mechanisms of action. Dawson, C., Ma, D., Chow, A., Maze, M. Anesthesiology (2004) [Pubmed]
  21. Different alpha-adrenoceptor subtypes mediate constriction of arterioles and venules. Leech, C.J., Faber, J.E. Am. J. Physiol. (1996) [Pubmed]
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