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Gene Review

GALR1  -  galanin receptor 1

Homo sapiens

Synonyms: GAL1-R, GALNR, GALNR1, GALR-1, Galanin receptor type 1
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Disease relevance of GALR1


Psychiatry related information on GALR1


High impact information on GALR1

  • Delineation of the peptide binding site of the human galanin receptor [9].
  • To determine which amino acids of the recently cloned seven-transmembrane domain-type human galanin receptor are involved in the high-affinity binding of the endogenous peptide ligand, we performed a mutagenesis study [9].
  • Major challenges in this field include linking the receptor clones with each of the known physiological actions of galanin and evaluating the evidence for additional galanin receptor subtypes [10].
  • We report here the isolation of a cDNA coding for a human galanin receptor from a Bowes melanoma cell line cDNA expression library, by using a radioligand binding strategy [11].
  • Furthermore, studies with the inhibitory antibody and U0126, the MAPK inhibitor, show that GALR1 inhibits proliferation in immortalized and malignant keratinocytes by inactivating the MAPK pathway [1].

Chemical compound and disease context of GALR1


Biological context of GALR1


Anatomical context of GALR1

  • In this study, the expression, mitogenic function, and signaling mechanism of GALR1 are investigated in normal and malignant oral epithelial cells. mRNA expression was determined via reverse transcriptase-PCR [1].
  • Upon competitive inhibition of GALR1, proliferation was up-regulated in immortalized and malignant keratinocytes [1].
  • The presence of 5'-guanylylimidodiphosphate (GppNHp) or NaCl reduced the agonist labeling of hGALR in ENT membranes [17].
  • Autoradiograms revealed intense GALR labeling, mainly in the substantia innominata, hypothalamus, the bed nucleus of the stria terminalis and within layers 2 and 4 of the ENT [17].
  • These effects appear to be related to activation of GAL-R1 (ventral hippocampus) and GAL-R2 (dorsal hippocampus) receptors, respectively [18].

Associations of GALR1 with chemical compounds

  • In addition, pre-treatment with guanine nucleotides may provide a more accurate measurement of GALR density since it would avoid the masking of GALRs by residual binding of endogenous GAL [5].
  • Subsequent studies supported this hypothesis, showing that the effects on 5-HT release in vivo are most likely mediated by a galanin receptor in the dorsal raphe [18].
  • The galanin receptor, a glycoprotein with a molecular mass of 54-60 kDa, was initially identified and characterized by radioligand binding studies with membranes prepared from tissues and cell lines [19].
  • We conclude that GAL receptor stimulation exerts an inhibitory effect on basal and insulin-induced hypoglycemia-stimulated release of norepinephrine [20].
  • 5. Powerful inhibitory effects of galanin on the electrical (and secretory) activity of magnocellular neurons and complex presynaptic actions of galanin on the synaptic release of glutamate in the arcuate nucleus in vitro suggest an active role for multiple galanin receptor subtypes in the regulation of these hypothalamic systems in vivo [21].

Regulatory relationships of GALR1

  • We previously showed that Gal1-R expression was transcriptionally regulated by the transcription factor NF-kappa B. Consistent with this transcription factor being activated in a number of inflammatory conditions, we show increased colonic Gal1-R expression in patients with colitis due to a variety of causes [22].
  • Galanin enhances corticosterone secretion from dispersed rat adrenocortical cells through the activation of GAL-R1 and GAL-R2 receptors coupled to the adenylate cyclase-dependent signaling cascade [23].

Other interactions of GALR1

  • Discrimination of galanin receptor subtypes in RINm5F cells by structurally different galanin radioligands [24].
  • The structural organization of GALNR1 suggests convergent evolution for this gene and represents a structural organization that is unique among genes encoding G-protein-coupled receptors [25].
  • We have generated a model of the human GALR1 galanin receptor subtype (hGALR1) based on the alpha carbon maps of frog rhodopsin and investigated the significance of potential contact residues suggested by the model using site-directed mutagenesis [26].
  • Gal1-R activation resulted in a dose-dependent increase in Cl- secretion; whereas infection of T84 cells with pathogens known to activate NF-kappa B augmented Gal1-R expression and Cl- secretion [22].
  • In contrast, the effect of galanin on PRL is mediated via the pituitary-specific galanin receptor GAL-R(W), at which galanin-(3-29) is fully active [27].

Analytical, diagnostic and therapeutic context of GALR1


  1. Galanin receptor 1 has anti-proliferative effects in oral squamous cell carcinoma. Henson, B.S., Neubig, R.R., Jang, I., Ogawa, T., Zhang, Z., Carey, T.E., D'Silva, N.J. J. Biol. Chem. (2005) [Pubmed]
  2. Human galanin (GAL) and galanin 1 receptor (GALR1) variations are not involved in fat intake and early onset obesity. Schäuble, N., Reichwald, K., Grassl, W., Bechstein, H., Müller, H.C., Scherag, A., Geller, F., Utting, M., Siegfried, W., Goldschmidt, H., Blundell, J., Lawton, C., Alam, R., Whybrow, S., Stubbs, J., Platzer, M., Hebebrand, J., Hinney, A. J. Nutr. (2005) [Pubmed]
  3. Expression of galanin and the GALR1 galanin receptor subtype in the colon of children with paradoxical fecal incontinence. Engelis, A., Mozgis, D.Z., Pine, K.A., Shine, J., Iismaa, T.P., Pilmane, M. Ann. N. Y. Acad. Sci. (1998) [Pubmed]
  4. Galanin and galanin receptors in human gliomas. Berger, A., Santic, R., Almer, D., Hauser-Kronberger, C., Huemer, M., Humpel, C., Stockhammer, G., Sperl, W., Kofler, B. Acta Neuropathol. (2003) [Pubmed]
  5. Increased galanin receptor occupancy in Alzheimer's disease. McMillan, P.J., Peskind, E., Raskind, M.A., Leverenz, J.B. Neurobiol. Aging (2004) [Pubmed]
  6. Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders. Ogren, S.O., Kuteeva, E., Hökfelt, T., Kehr, J. CNS drugs. (2006) [Pubmed]
  7. Minireview. Galanin-acetylcholine interactions: relevance to memory and Alzheimer's disease. Crawley, J.N. Life Sci. (1996) [Pubmed]
  8. The role of galanin in feeding behavior. Crawley, J.N. Neuropeptides (1999) [Pubmed]
  9. Delineation of the peptide binding site of the human galanin receptor. Kask, K., Berthold, M., Kahl, U., Nordvall, G., Bartfai, T. EMBO J. (1996) [Pubmed]
  10. Galanin receptor subtypes. Branchek, T.A., Smith, K.E., Gerald, C., Walker, M.W. Trends Pharmacol. Sci. (2000) [Pubmed]
  11. Molecular cloning of a functional human galanin receptor. Habert-Ortoli, E., Amiranoff, B., Loquet, I., Laburthe, M., Mayaux, J.F. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
  12. Galanin receptor in the rat pancreatic beta cell line Rin m 5F. Molecular characterization by chemical cross-linking. Amiranoff, B., Lorinet, A.M., Laburthe, M. J. Biol. Chem. (1989) [Pubmed]
  13. Galanin receptor subtype GalR2 mediates apoptosis in SH-SY5Y neuroblastoma cells. Berger, A., Lang, R., Moritz, K., Santic, R., Hermann, A., Sperl, W., Kofler, B. Endocrinology (2004) [Pubmed]
  14. Pharmacological characterization and tissue distribution of the human and rat GALR1 receptors. Sullivan, K.A., Shiao, L.L., Cascieri, M.A. Biochem. Biophys. Res. Commun. (1997) [Pubmed]
  15. Galanin receptor expression in cultured human keratinocytes and in normal human skin. Dallos, A., Kiss, M., Polyánka, H., Dobozy, A., Kemény, L., Husz, S. J. Peripher. Nerv. Syst. (2006) [Pubmed]
  16. Molecular identification and coexpression of galanin and GalR-1 galanin receptor in the human ocular ciliary epithelium: differential modulation of their expression by the activation of alpha2- and beta2-adrenergic receptors in cultured ciliary epithelial cells. Ortego, J., Coca-Prados, M. J. Neurochem. (1998) [Pubmed]
  17. Characterization and localization of galanin receptors in human entorhinal cortex. Deecher, D.C., Mash, D.C., Staley, J.K., Mufson, E.J. Regul. Pept. (1998) [Pubmed]
  18. Modulation of acetylcholine and serotonin transmission by galanin. Relationship to spatial and aversive learning. Ogren, S.O., Schött, P.A., Kehr, J., Yoshitake, T., Misane, I., Mannström, P., Sandin, J. Ann. N. Y. Acad. Sci. (1998) [Pubmed]
  19. Galanin receptor subtypes. Wang, S., Gustafson, E.L. Drug News Perspect. (1998) [Pubmed]
  20. Effect of human galanin on the response of circulating catecholamines to hypoglycemia in man. degli Uberti, E.C., Ambrosio, M.R., Bondanelli, M., Trasforini, G., Valentini, A., Rossi, R., Margutti, A., Campo, M. Eur. J. Endocrinol. (1995) [Pubmed]
  21. Distribution, regulation and role of hypothalamic galanin systems: renewed interest in a pleiotropic peptide family. Gundlach, A.L., Burazin, T.C., Larm, J.A. Clin. Exp. Pharmacol. Physiol. (2001) [Pubmed]
  22. Galanin causes Cl- secretion in the human colon. Potential significance of inflammation-associated NF-kappa B activation on galanin-1 receptor expression and function. Benya, R.V., Matkowskyj, K.A., Danilkovich, A., Hecht, G. Ann. N. Y. Acad. Sci. (1998) [Pubmed]
  23. Galanin enhances corticosterone secretion from dispersed rat adrenocortical cells through the activation of GAL-R1 and GAL-R2 receptors coupled to the adenylate cyclase-dependent signaling cascade. Andreis, P.G., Malendowicz, L.K., Rebuffat, P., Spinazzi, R., Ziolkowska, A., Nussdorfer, G.G. Int. J. Mol. Med. (2007) [Pubmed]
  24. Discrimination of galanin receptor subtypes in RINm5F cells by structurally different galanin radioligands. Deecher, D.C., López, F.J. Peptides (2002) [Pubmed]
  25. Structural organization and chromosomal localization of three human galanin receptor genes. Iismaa, T.P., Fathi, Z., Hort, Y.J., Iben, L.G., Dutton, J.L., Baker, E., Sutherland, G.R., Shine, J. Ann. N. Y. Acad. Sci. (1998) [Pubmed]
  26. Molecular modelling and site-directed mutagenesis of human GALR1 galanin receptor defines determinants of receptor subtype specificity. Church, W.B., Jones, K.A., Kuiper, D.A., Shine, J., Iismaa, T.P. Protein Eng. (2002) [Pubmed]
  27. The differential effects of galanin-(1-30) and -(3-30) on anterior pituitary hormone secretion in vivo in humans. Todd, J.F., Edwards, C.M., Ghatei, M.A., Bloom, S.R. Am. J. Physiol. Endocrinol. Metab. (2000) [Pubmed]
  28. Molecular cloning and pharmacological characterization of a new galanin receptor subtype. Wang, S., Hashemi, T., He, C., Strader, C., Bayne, M. Mol. Pharmacol. (1997) [Pubmed]
  29. Galanin receptor plasticity within the nucleus basalis in early and late Alzheimer's disease: an in vitro autoradiographic analysis. Mufson, E.J., Deecher, D.C., Basile, M., Izenwasse, S., Mash, D.C. Neuropharmacology (2000) [Pubmed]
  30. ADP ribosylation by cholera toxin identifies three G-proteins that are activated by the galanin receptor. Studies with RINm5F cell membranes. Gillison, S.L., Sharp, G.W. Diabetes (1994) [Pubmed]
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