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Gene Review

Adra2b  -  adrenergic receptor, alpha 2b

Mus musculus

Synonyms: Adra-2b, Alpha-2B adrenergic receptor, Alpha-2B adrenoceptor, Alpha-2B adrenoreceptor, Alpha-2BAR, ...
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Disease relevance of Adra2b


Psychiatry related information on Adra2b

  • In the alpha2B AR and alpha2C AR knock-out mice, Dex produced a dose-dependent reduction in spontaneous locomotor activity with ED50 values of 29.1+/-6.4 (P>0.05 vs WT control) and 57.5+/-11.3 (P>0.05 vs WT control) microg kg(-1), respectively [2].

High impact information on Adra2b

  • Our results show that the alpha 1 and alpha 2A domains of the H-2Kk antigen can constitute target molecules for alloimmune anti-Kk T cells, whereas the alpha 2B region, when exchanged for Kd or Kb sequences, plays only a limited role [3].
  • Although alpha2-adrenoceptors (alpha2-ARs) have been suggested to have a modulatory role in these disorders, the specific roles of each alpha2-AR subtype (alpha2A, alpha2B, and alpha2C) are largely unknown [4].
  • The third intracellular loops of the alpha 2A, alpha 2B, and alpha 2C-AR subtypes interact with spinophilin, a multidomain protein that, like the three alpha 2-AR subtypes, is enriched at the basolateral surface of MDCKII cells [5].
  • Here, we have analyzed and compared the performance of three nuclear genes (von Willebrand Factor, interphotoreceptor retinoid-binding protein, and Alpha 2B adrenergic receptor) for a large taxonomic sampling, covering the whole rodent and placental diversity [6].
  • The unglycosylated alpha 2B subtype of the alpha 2-adrenergic receptor found in NG-108-15 cells possesses allosteric regulation of adrenergic ligand binding by monovalent cations and 5-amino-substituted amiloride analogs [7].

Biological context of Adra2b

  • The selective expression of alpha2B in brain as indexed by beta-galactosidase, under the direction of this promoter region, may be traced in situ by using X-gal staining [8].
  • No bands were seen for HT29, NG108 and OK cells when hybridized with a third alpha 2-adrenoceptor human genomic DNA probe which is localized in chromosome 2 (alpha 2-C2) [9].
  • In the alpha2B AR and alpha2C AR knock-out mice, Dex produced a dose-dependent reduction in body temperature with ED50 values of 28.4+/-4.8 (P>0.05 vs WT control) and 54.1+/-8.0 (P>0.05 vs WT control) microg kg(-1), respectively [2].
  • CONCLUSIONS: These results indicate that etomidate acts as an agonist at alpha2-adrenoceptors, which appears in vivo primarily as an alpha2B-receptor-mediated increase in blood pressure [10].
  • The deduced amino acid sequence of the M alpha 2-2H shows 82% and 96% identity to the human alpha 2-C2 and the rat RNG alpha 2 adrenergic receptors, respectively [11].

Anatomical context of Adra2b


Associations of Adra2b with chemical compounds

  • Which of the three alpha2-adrenoceptor subtypes of alpha2A, alpha2B, or alpha2C mediates the neuroprotective effect of dexmedetomidine was examined in cell culture as well as in an in vivo model of neonatal asphyxia [16].
  • When expressed in Spodoptera frugiperda Sf9 cells the alpha2A subtype showed only inhibition of forskolin-stimulated cAMP production when activated by norepinephrine (NE), whereas the alpha2B subtype displayed a biphasic dose-response curve with inhibition at low concentrations of NE and a potentiation at higher concentrations [17].
  • The alpha-2B preferential antagonists ARC-239, prazosin or chlorpromazine failed to block the modifications in both glycemic and insulin levels induced by alpha-2 adrenoceptor stimulation [18].
  • 2. Comparing the effects of the GlyR agonists, glycine, beta-alanine and taurine, on the GlyR alpha2 isoforms, revealed a significant increase in potency for all three agonists at the alpha2B variant [19].
  • 6-chloro-9-[(3-methyl-2-butenyl)oxy]-3-methyl-1H-2,3,4,5-tetrahydro-3- benzazepine (SK&F 104078) did not differentiate between the alpha-2A and alpha-2B receptor subtypes [20].

Other interactions of Adra2b

  • Expression levels of Adra2a and Adra2b mRNA in brain and kidney are not altered by the Adra2c knockout [21].
  • Radioligand binding studies showed that the alpha 2-adrenoceptor expressed in HT29, NG108 and OK cells represent the pharmacological alpha 2A, alpha 2B and alpha 2C subtypes respectively [9].
  • Activation of the wild-type alpha2B AR-Galpha15 fusion protein in CHO-K1 cells by (-)-adrenaline induced a time- and concentration-dependent (pEC50 = 7.37+/-0.13) increase in the intracellular Ca2+ concentration, which could be antagonized by RX 811059 (pK(B) = 7.55+/-0.15) [22].

Analytical, diagnostic and therapeutic context of Adra2b


  1. Factors determining the specificity of signal transduction by guanine nucleotide-binding protein-coupled receptors. III. Coupling of alpha 2-adrenergic receptor subtypes in a cell type-specific manner. Duzic, E., Lanier, S.M. J. Biol. Chem. (1992) [Pubmed]
  2. Assessment of the role of alpha2-adrenoceptor subtypes in the antinociceptive, sedative and hypothermic action of dexmedetomidine in transgenic mice. Hunter, J.C., Fontana, D.J., Hedley, L.R., Jasper, J.R., Lewis, R., Link, R.E., Secchi, R., Sutton, J., Eglen, R.M. Br. J. Pharmacol. (1997) [Pubmed]
  3. Different structural constraints for recognition of mouse H-2Kd and -Kk antigens by alloimmune cytolytic T lymphocytes. Schøller, J., Shimonkevitz, R., MacDonald, H.R., Kvist, S. J. Exp. Med. (1986) [Pubmed]
  4. Adrenergic alpha2C-receptors modulate the acoustic startle reflex, prepulse inhibition, and aggression in mice. Sallinen, J., Haapalinna, A., Viitamaa, T., Kobilka, B.K., Scheinin, M. J. Neurosci. (1998) [Pubmed]
  5. Spinophilin stabilizes cell surface expression of alpha 2B-adrenergic receptors. Brady, A.E., Wang, Q., Colbran, R.J., Allen, P.B., Greengard, P., Limbird, L.E. J. Biol. Chem. (2003) [Pubmed]
  6. Rodent phylogeny and a timescale for the evolution of Glires: evidence from an extensive taxon sampling using three nuclear genes. Huchon, D., Madsen, O., Sibbald, M.J., Ament, K., Stanhope, M.J., Catzeflis, F., de Jong, W.W., Douzery, E.J. Mol. Biol. Evol. (2002) [Pubmed]
  7. Monovalent cation and amiloride analog modulation of adrenergic ligand binding to the unglycosylated alpha 2B-adrenergic receptor subtype. Wilson, A.L., Seibert, K., Brandon, S., Cragoe, E.J., Limbird, L.E. Mol. Pharmacol. (1991) [Pubmed]
  8. Regulated expression of alpha2B adrenoceptor during development. Wang, G.S., Chang, N.C., Wu, S.C., Chang, A.C. Dev. Dyn. (2002) [Pubmed]
  9. Northern blot and ribonuclease protection study of alpha 2-adrenoceptor subtypes in cultured cell lines. Sun, L., Umemura, S., Chun, M., Pettinger, W.A. Eur. J. Pharmacol. (1992) [Pubmed]
  10. Activation of alpha 2B-adrenoceptors mediates the cardiovascular effects of etomidate. Paris, A., Philipp, M., Tonner, P.H., Steinfath, M., Lohse, M., Scholz, J., Hein, L. Anesthesiology (2003) [Pubmed]
  11. Cloning and expression of the mouse homolog of the human alpha 2-C2 adrenergic receptor. Chruscinski, A.J., Link, R.E., Daunt, D.A., Barsh, G.S., Kobilka, B.K. Biochem. Biophys. Res. Commun. (1992) [Pubmed]
  12. Linkage mapping of alpha-2 adrenergic receptor genes to mouse chromosomes 2 and 5. Link, R.E., Kobilka, B.K., Barsh, G.S. Mamm. Genome (1993) [Pubmed]
  13. Occurrence, pharmacology and function of presynaptic alpha2-autoreceptors in alpha2A/D-adrenoceptor-deficient mice. Trendelenburg, A.U., Hein, L., Gaiser, E.G., Starke, K. Naunyn Schmiedebergs Arch. Pharmacol. (1999) [Pubmed]
  14. Gene substitution/knockout to delineate the role of alpha 2-adrenoceptor subtypes in mediating central effects of catecholamines and imidazolines. Hein, L., Limbird, L.E., Eglen, R.M., Kobilka, B.K. Ann. N. Y. Acad. Sci. (1999) [Pubmed]
  15. Factors determining the specificity of signal transduction by guanine nucleotide-binding protein-coupled receptors. I. Coupling of alpha 2-adrenergic receptor subtypes to distinct G-proteins. Duzic, E., Coupry, I., Downing, S., Lanier, S.M. J. Biol. Chem. (1992) [Pubmed]
  16. Dexmedetomidine produces its neuroprotective effect via the alpha 2A-adrenoceptor subtype. Ma, D., Hossain, M., Rajakumaraswamy, N., Arshad, M., Sanders, R.D., Franks, N.P., Maze, M. Eur. J. Pharmacol. (2004) [Pubmed]
  17. The second intracellular loop of the alpha2-adrenergic receptors determines subtype-specific coupling to cAMP production. Näsman, J., Jansson, C.C., Akerman, K.E. J. Biol. Chem. (1997) [Pubmed]
  18. Involvement of alpha-2 adrenergic receptor subtypes in hyperglycemia. Angel, I., Niddam, R., Langer, S.Z. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  19. Differential agonist sensitivity of glycine receptor alpha2 subunit splice variants. Miller, P.S., Harvey, R.J., Smart, T.G. Br. J. Pharmacol. (2004) [Pubmed]
  20. Ability of SK&F 104078 and SK&F 104856 to identify alpha-2 adrenoceptor subtypes in NCB20 cells and guinea pig lung. Gleason, M.M., Hieble, J.P. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  21. Targeted inactivation of the gene encoding the mouse alpha 2c-adrenoceptor homolog. Link, R.E., Stevens, M.S., Kulatunga, M., Scheinin, M., Barsh, G.S., Kobilka, B.K. Mol. Pharmacol. (1995) [Pubmed]
  22. Ligand-receptor interactions as controlled by wild-type and mutant Thr(370)Lys alpha2B-adrenoceptor-Galpha15 fusion proteins. Pauwels, P.J., Tardif, S., Finana, F., Wurch, T., Colpaert, F.C. J. Neurochem. (2000) [Pubmed]
  23. Distribution of mRNA encoding three alpha 2-adrenergic receptor subtypes in the developing mouse embryo suggests a role for the alpha 2A subtype in apoptosis. Wang, R.X., Limbird, L.E. Mol. Pharmacol. (1997) [Pubmed]
  24. Effect of alpha2B-adrenoceptor polymorphism on peripheral vasoconstriction in healthy volunteers. Talke, P., Stapelfeldt, C., Lobo, E., Brown, R., Scheinin, M., Snapir, A. Anesthesiology (2005) [Pubmed]
  25. Viable AC-2, a new adult bovine serum- and colostrum-based supplement for the culture of mammalian cells. Viander, B., Ala-Uotila, S., Jalkanen, M., Pakkanen, R. BioTechniques (1996) [Pubmed]
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