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Adra2c  -  adrenergic receptor, alpha 2c

Mus musculus

Synonyms: Adra-2c, Alpha-2 adrenergic receptor subtype C4, Alpha-2C adrenergic receptor, Alpha-2C adrenoceptor, Alpha-2C adrenoreceptor, ...
 
 
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Disease relevance of Adra2c

 

Psychiatry related information on Adra2c

  • The effects of dexmedetomidine, a subtype-nonselective alpha 2-AR agonist, on monoamine turnover in brain and on locomotor activity were similar in mice with targeted inactivation of the alpha 2C-AR gene and in their controls, but the hypothermic effect of the alpha 2-AR agonist was significantly attenuated by the receptor gene inactivation [2].
 

High impact information on Adra2c

  • Alpha2-adrenergic receptors are known to have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system; however, the individual roles of the three highly homologous alpha2-adrenergic-receptor subtypes (alpha2A, alpha2B, alpha2C) in this process are not known [1].
  • A chimera consisting of 81% and 19% of the alpha1 N terminus and alpha2 C terminus, respectively, behaves like alpha2 and coprecipitates with the beta2 ectodomain [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].
  • 90% of the NIH-3T3 alpha2C-AR transfectants expressed receptor mRNA, but only 14% of the clonal cell lines expressed receptor protein [5].
  • The alpha2C-AR mRNA with the longer 3'-UTR underwent translational initiation as it was found in the polysome fraction, indicating that the lack of receptor protein was due to impaired translational elongation or termination [5].
 

Biological context of Adra2c

 

Anatomical context of Adra2c

 

Associations of Adra2c with chemical compounds

  • In striatal slices from Adra2c+/+ mice, the alpha2 adrenoceptor antagonist RX821002 facilitated forskolin-stimulated cyclic AMP accumulation in a concentration-dependent manner [11].
  • Genetic alteration of alpha 2C-adrenoceptor expression in mice: influence on locomotor, hypothermic, and neurochemical effects of dexmedetomidine, a subtype-nonselective alpha 2-adrenoceptor agonist [2].
  • Very similar data were obtained for two other Gi-coupled receptors, the D2 dopamine receptor and the alpha2C adrenergic receptor [12].
  • In vivo, deletion of sympathetic or adrenal feedback control led to increased plasma and urine norepinephrine (alpha 2A-knockout) and epinephrine levels (alpha 2C-knockout), respectively [10].
  • The alpha2A and alpha2C adrenergic receptor (AR) subtypes mediate antinociception when activated by the endogenous ligand norepinephrine [13].
 

Other interactions of Adra2c

  • 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 [14].
 

Analytical, diagnostic and therapeutic context of Adra2c

References

  1. Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission. Hein, L., Altman, J.D., Kobilka, B.K. Nature (1999) [Pubmed]
  2. Genetic alteration of alpha 2C-adrenoceptor expression in mice: influence on locomotor, hypothermic, and neurochemical effects of dexmedetomidine, a subtype-nonselective alpha 2-adrenoceptor agonist. Sallinen, J., Link, R.E., Haapalinna, A., Viitamaa, T., Kulatunga, M., Sjöholm, B., Macdonald, E., Pelto-Huikko, M., Leino, T., Barsh, G.S., Kobilka, B.K., Scheinin, M. Mol. Pharmacol. (1997) [Pubmed]
  3. Isoform-specific interactions of Na,K-ATPase subunits are mediated via extracellular domains and carbohydrates. Schmalzing, G., Ruhl, K., Gloor, S.M. Proc. Natl. Acad. Sci. U.S.A. (1997) [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. The 3'-untranslated region of the alpha2C-adrenergic receptor mRNA impedes translation of the receptor message. Yang, Q., McDermott, P.J., Duzic, E., Pleij, C.W., Sherlock, J.D., Lanier, S.M. J. Biol. Chem. (1997) [Pubmed]
  6. 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]
  7. Characterization of the regulatory region of Adra2c, the gene encoding the murine alpha2C adrenoceptor subtype. Chen, W.K., Chang, N.C., Chang, Y.H., Chang, K.L., Wu, S.C., Yang, T.S., Wu, S.M., Chang, A.C. J. Biomed. Sci. (2004) [Pubmed]
  8. Selective irreversible binding of chloroethylclonidine at alpha 1- and alpha 2-adrenoceptor subtypes. Michel, M.C., Kerker, J., Branchek, T.A., Forray, C. Mol. Pharmacol. (1993) [Pubmed]
  9. Expression of alpha 2-adrenergic receptor subtypes in the mouse brain: evaluation of spatial and temporal information imparted by 3 kb of 5' regulatory sequence for the alpha 2A AR-receptor gene in transgenic animals. Wang, R., Macmillan, L.B., Fremeau, R.T., Magnuson, M.A., Lindner, J., Limbird, L.E. Neuroscience (1996) [Pubmed]
  10. Differential control of adrenal and sympathetic catecholamine release by alpha 2-adrenoceptor subtypes. Brede, M., Nagy, G., Philipp, M., Sorensen, J.B., Lohse, M.J., Hein, L. Mol. Endocrinol. (2003) [Pubmed]
  11. alpha2C adrenoceptors inhibit adenylyl cyclase in mouse striatum: potential activation by dopamine. Zhang, W., Klimek, V., Farley, J.T., Zhu, M.Y., Ordway, G.A. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  12. G-protein-coupled receptor-mediated activation of rap GTPases: characterization of a novel Galphai regulated pathway. Weissman, J.T., Ma, J.N., Essex, A., Gao, Y., Burstein, E.S. Oncogene (2004) [Pubmed]
  13. Transcutaneous electrical nerve stimulation activates peripherally located alpha-2A adrenergic receptors. King, E.W., Audette, K., Athman, G.A., Nguyen, H.O., Sluka, K.A., Fairbanks, C.A. Pain (2005) [Pubmed]
  14. 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]
  15. 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]
  16. Alpha 2C-adrenoceptor mediated regulation of cortical EEG arousal. Puoliväli, J., Björklund, M., Holmberg, M., Ihalainen, J.A., Scheinin, M., Tanila, H. Neuropharmacology (2002) [Pubmed]
  17. 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]
 
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