Genomes and Genes
Summary: A family of G-protein-coupled receptors that are specific for GALANIN and galanin peptides. They are generally considered to be coupled to the GI, INHIBITORY G-PROTEIN to meditate the neurological effects of galanin. Several subtypes of galanin receptors occur with differing specificities for the full length galanin, galanin peptide fragments, and galanin-like peptide.
- Berger A, Santic R, Hauser Kronberger C, Schilling F, Kogner P, Ratschek M, et al. Galanin and galanin receptors in human cancers. Neuropeptides. 2005;39:353-9 pubmed..This study summarizes our current knowledge on the expression of galanin peptide and galanin receptors in different human neuroendocrine tumors...
- Kolakowski L, O Neill G, Howard A, Broussard S, Sullivan K, Feighner S, et al. Molecular characterization and expression of cloned human galanin receptors GALR2 and GALR3. J Neurochem. 1998;71:2239-51 pubmed..GALR3 mRNA was highly expressed in human testis and was detectable in adrenal gland and pancreas. The genes for human GALR2 and 3 were localized to chromosomes 17q25 and 22q12.2-13.1, respectively. ..
- Schmidt W, Kratzin H, Eckart K, Drevs D, Mundkowski G, Clemens A, et al. Isolation and primary structure of pituitary human galanin, a 30-residue nonamidated neuropeptide. Proc Natl Acad Sci U S A. 1991;88:11435-9 pubmed..Synthetic hGal possesses full biological activity on isolated rat fundus muscle strips. ..
- Sun Y, Li J, Yang B, Yu L. Antinociceptive effects of galanin in the rat tuberomammillary nucleus and the plasticity of galanin receptor 1 during hyperalgesia. J Neurosci Res. 2004;77:718-22 pubmed..a putative galanin receptor antagonist, suggesting that the antinociceptive effect of galanin is mediated by galanin receptors. Moreover, there was abundant galanin receptor 1 (GalR1) in the TM, and the number of GalR1-positive neurons ..
- Dungan H, Clifton D, Steiner R. Minireview: kisspeptin neurons as central processors in the regulation of gonadotropin-releasing hormone secretion. Endocrinology. 2006;147:1154-8 pubmed..Together, these observations demonstrate that kisspeptin-GPR54 signaling in the brain serves as an important conduit for controlling GnRH secretion in the developing and adult animal. ..
- Mulvaney J, Merriam L, Parsons R. Galantide distinguishes putative subtypes of galanin receptors in mudpuppy parasympathetic neurons. Eur J Pharmacol. 1995;287:97-100 pubmed..One interpretation of these observations is that different galanin receptors mediate the different effects of galanin on the mudpuppy parasympathetic neurons.
- Liu Z, Xu Y, Wu L, Zhang S. Evolution of galanin receptor genes: insights from the deuterostome genomes. J Biomol Struct Dyn. 2010;28:97-106 pubmed..We also proposed that Galr3 genes were the products of Galr2 duplication during evolution, while Galr2 genes may evolve from Galr1. ..
- Mickael M, Rajput A, Steyn J, Wiemerslage L, Burglin T. An optimised phylogenetic method sheds more light on the main branching events of rhodopsin-like superfamily. Comp Biochem Physiol Part D Genomics Proteomics. 2016;20:85-94 pubmed publisher..Our analysis indicated that basal receptors might be playing a role in early evolution of the nervous system. This is evident in Trichoplax adhaerens genome, where we located histamine receptors and adenosine receptors. ..
- Dallos A, Kiss M, Polyanka H, Dobozy A, Kemeny L, Husz S. Galanin receptor expression in cultured human keratinocytes and in normal human skin. J Peripher Nerv Syst. 2006;11:156-64 pubmed..GAL treatment of the keratinocytes resulted in an increase in cytosolic Ca2+ concentration, suggesting that GALR2 is a functional receptor. Further studies are necessary to clarify the biological effects of GAL in the skin. ..
- Seminara S, Dipietro M, Ramaswamy S, Crowley W, Plant T. Continuous human metastin 45-54 infusion desensitizes G protein-coupled receptor 54-induced gonadotropin-releasing hormone release monitored indirectly in the juvenile male Rhesus monkey (Macaca mulatta): a finding with therapeutic implications. Endocrinology. 2006;147:2122-6 pubmed..e. precocious puberty, endometriosis, uterine fibroids, and prostate cancer). ..
- Sollenberg U, Bartfai T, Langel U. Galnon--a low-molecular weight ligand of the galanin receptors. Neuropeptides. 2005;39:161-3 pubmedGalnon is a low-molecular weight galanin receptor ligand, with affinity towards the three galanin receptors in the micromolar range...
- Ruczyński J, Konstanski Z, Cybal M, Petrusewicz J, Wojcikowski C, Rekowski P, et al. Synthesis and biological properties of new chimeric galanin analogue GAL(1-13)-[Ala10,11]ET-1(6-21)-NH2. J Physiol Pharmacol. 2005;56:273-85 pubmed..This chimera was previously shown to be a moderate-affinity ligand to hypothalamic galanin receptors with a K(D) value of 205 nM. However, its biological action has been unknown so far...
- Simoneaux D, Leach R, O Connell P. Galanin receptor 1 gene (Galnr1) is tightly linked to the myelin basic protein gene on chromosome 18 in mouse. Mamm Genome. 1997;8:875 pubmed
- Volkoff H, Peter R. Interactions between orexin A, NPY and galanin in the control of food intake of the goldfish, Carassius auratus. Regul Pept. 2001;101:59-72 pubmed..In addition, the effects of OXA are mediated, in part, by the NPY pathway. This suggests a functional interdependence between these three peptidergic systems in the control of energy balance in goldfish. ..
- Mensah E, Blanco A, Donini A, Unniappan S. Brain and intestinal expression of galanin-like peptide (GALP), galanin receptor R1 and galanin receptor R2, and GALP regulation of food intake in goldfish (Carassius auratus). Neurosci Lett. 2017;637:126-135 pubmed publisher..These observations form the first report on the presence of GALP in the fish brain and gut, and also on its modulatory role on fish feeding behavior. GALP, as in mammals, appears to be a functional neuropeptide in goldfish. ..
- Fang P, Yu M, He B, Guo L, Huang X, Kong G, et al. Central injection of GALR1 agonist M617 attenuates diabetic rat skeletal muscle insulin resistance through the Akt/AS160/GLUT4 pathway. Mech Ageing Dev. 2017;162:122-128 pubmed publisher..in skeletal muscle of rats, there is no literature available regarding to the effect of type 1 of galanin receptors (GALR1) on insulin resistance in skeletal muscle of type 2 diabetic rats...
- Weinshenker D, Holmes P. Regulation of neurological and neuropsychiatric phenotypes by locus coeruleus-derived galanin. Brain Res. 2016;1641:320-37 pubmed publisher..This article is part of a Special Issue entitled SI: Noradrenergic System. ..
- Walli R, Schafer H, Morys Wortmann C, Paetzold G, Nustede R, Schmidt W. Identification and biochemical characterization of the human brain galanin receptor. J Mol Endocrinol. 1994;13:347-56 pubmed..Receptors bound to 125I-labelled hGal could be specifically adsorbed to wheat germ agglutinin and ricinus communis agglutinin, suggesting that receptor glycosylation involves N-acetyl glucosamine and galactose respectively. ..
- Barreto S, Carati C, Schloithe A, Toouli J, Saccone G. Galanin potentiates supramaximal caerulein-stimulated pancreatic amylase secretion via its action on somatostatin secretion. Am J Physiol Gastrointest Liver Physiol. 2009;297:G1268-73 pubmed publisher..Taken together, these data suggest that, at supramaximal caerulein concentrations, galanin acts via its receptors to further increase caerulein-stimulated amylase secretion by inhibiting the caerulein-induced release of somatostatin. ..
- Bloch G, Butler P, Eckersell C, Mills R. Gonadal steroid-dependent GAL-IR cells within the medial preoptic nucleus (MPN) and the stimulatory effects of GAL within the MPN on sexual behaviors. Ann N Y Acad Sci. 1998;863:188-205 pubmed
- Ceide S, Trembleau L, Haberhauer G, Somogyi L, Lu X, Bartfai T, et al. Synthesis of galmic: a nonpeptide galanin receptor agonist. Proc Natl Acad Sci U S A. 2004;101:16727-32 pubmed..Few nonpeptide ligands, capable of activating galanin receptors, are available today...
- Li S, Huo M, Wu X, Huang Y, Wang L, Zhang X, et al. Involvement of galanin and galanin receptor 1 in nociceptive modulation in the central nucleus of amygdala in normal and neuropathic rats. Sci Rep. 2017;7:15317 pubmed publisher..These results illustrated that galanin induced antinociception in CeA in normal rats and rats with neuropathy, and there is an up-regulation of GalR1 expression in rats with neuropathy. ..
- Fitzgerald L, Patterson J, Conklin D, Horlick R, Largent B. Pharmacological and biochemical characterization of a recombinant human galanin GALR1 receptor: agonist character of chimeric galanin peptides. J Pharmacol Exp Ther. 1998;287:448-56 pubmed..These observations suggest that the antagonist effects in vivo of M40, and perhaps other chimeric peptides, are not mediated via direct interactions with the galanin receptor 1 receptor. ..
- Cui J, Chen Q, Yue X, Jiang X, Gao G, Yu L, et al. Galanin protects against intracellular amyloid toxicity in human primary neurons. J Alzheimers Dis. 2010;19:529-44 pubmed publisherGalanin and galanin receptors are upregulated in the brain regions associated with Alzheimer's disease (AD). However, the consequence of this overexpression is still unknown, particularly in human neurons...
- Tyszkiewicz J, Fong T, Dong Y. GABAB receptors are required for galanin modulation of membrane properties of neurons in the arcuate nucleus of rats. Brain Res. 2008;1191:63-8 pubmed..The galanin action is mediated by the galanin receptors (GAL1/2/3R)...
- Tortorella C, Neri G, Nussdorfer G. Galanin in the regulation of the hypothalamic-pituitary-adrenal axis (Review). Int J Mol Med. 2007;19:639-47 pubmed..There is also evidence that galanin plays a role in the modulation of HPA-axis response to stress, as well as in the pathogenesis of pituitary adenomas and perhaps of pheochromocytomas. ..
- Zhang M, Wang H, Fu F, Yu L. Involvement of galanin and galanin receptor 2 in nociceptive modulation in anterior cingulate cortex of normal rats and rats with mononeuropathy. Sci Rep. 2017;7:45930 pubmed publisher..And there may be plastic changes in the expression of galanin and galanin receptor 2 in rats with mononeuropathy, as well as in the galanin-induced antinociception. ..
- Boudaka A, Wörl J, Shiina T, Shimizu Y, Takewaki T, Neuhuber W. Galanin modulates vagally induced contractions in the mouse oesophagus. Neurogastroenterol Motil. 2009;21:180-8 pubmed publisher..These data suggest that galanin from co-innervating enteric neurons co-operates with nitric oxide in modulating vagally induced contractions in the mouse oesophagus. ..
- Hawes J, Picciotto M. Characterization of GalR1, GalR2, and GalR3 immunoreactivity in catecholaminergic nuclei of the mouse brain. J Comp Neurol. 2004;479:410-23 pubmedThe distribution of immunoreactivity for the three identified neuropeptide galanin receptors, GalR1, GalR2, and GalR3, was determined in areas of the mouse brain involved in drug addiction, including the ventral tegmental area (VTA), ..
- Lu X, Sharkey L, Bartfai T. The brain galanin receptors: targets for novel antidepressant drugs. CNS Neurol Disord Drug Targets. 2007;6:183-92 pubmed..b>Galanin receptors are expressed in brain structures that are involved in the regulation of mood such as frontal cortex, ..
- Mahoney S, Hosking R, Farrant S, Holmes F, Jacoby A, Shine J, et al. The second galanin receptor GalR2 plays a key role in neurite outgrowth from adult sensory neurons. J Neurosci. 2003;23:416-21 pubmed..These results demonstrate that adult sensory neurons are dependent, in part, on galanin for neurite extension and that this crucial physiological process is mediated by activation of the GalR2 receptor in a PKC-dependent manner. ..
- Ma X, Tong Y, Schmidt R, Brown W, Payza K, Hodzic L, et al. Effects of galanin receptor agonists on locus coeruleus neurons. Brain Res. 2001;919:169-74 pubmed..These results suggest that it mainly is the GALR1 receptor that mediates hyperpolarization of LC neurons. ..
- Blakeman K, Hao J, Xu X, Jacoby A, Shine J, Crawley J, et al. Hyperalgesia and increased neuropathic pain-like response in mice lacking galanin receptor 1 receptors. Neuroscience. 2003;117:221-7 pubmed..The results provide some evidence for an inhibitory function for the neuropeptide galanin acting on galanin receptor 1 (GALR1) in nociception and neuropathic pain after peripheral nerve injury in mice. ..
- Podlasz P, Jakimiuk A, Chmielewska Krzesinska M, Kasica N, Nowik N, Kaleczyc J. Galanin regulates blood glucose level in the zebrafish: a morphological and functional study. Histochem Cell Biol. 2016;145:105-17 pubmed publisher..The present findings suggest that, like in mammals, in the zebrafish galanin is involved in the regulation of blood glucose level. However, further studies are needed to elucidate the exact mechanism of the galanin action. ..
- Metcalf C, Smith M, Klein B, McDougle D, Zhang L, Bulaj G. Preclinical Analgesic and Safety Evaluation of the GalR2-preferring Analog, NAX 810-2. Neurochem Res. 2017;42:1983-1994 pubmed publisher..Similarly, 8 mg/kg (twice daily, 5 days) of NAX 810-2 did not increase growth hormone levels. These results demonstrate that NAX 810-2 possesses a favorable pre-clinical profile as a novel and first-in-class analgesic. ..
- Lerner J, Sankar R, Mazarati A. Galanin and epilepsy. Cell Mol Life Sci. 2008;65:1864-71 pubmed publisher..attenuated seizure responses under conditions of animal models of epilepsy; pharmacological blocking of galanin receptors exerted proconvulsant effects...
- Anselmi L, Lakhter A, Hirano A, Tonini M, Sternini C. Expression of galanin receptor messenger RNAs in different regions of the rat gastrointestinal tract. Peptides. 2005;26:815-9 pubmed..The differential regional distribution of GalRs suggests that the complex effects of galanin in the gut are the result of activating multiple receptor subtypes, whose density, subtype and signaling vary along the gastrointestinal tract. ..
- Smith K, Walker M, Artymyshyn R, Bard J, Borowsky B, Tamm J, et al. Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels. J Biol Chem. 1998;273:23321-6 pubmed..Multiple galanin receptors are predicted to mediate its effects, but only two functionally coupled receptors have been reported...
- Rezaei K, Xu I, Wu W, Shi T, Soomets U, Land T, et al. Intrathecal administration of PNA targeting galanin receptor reduces galanin-mediated inhibitory effect in the rat spinal cord. Neuroreport. 2001;12:317-20 pubmed..Thus, unmodified PNA applied i.t. appears to function as an effective antisense reagent in rat spinal cord in vivo. ..
- Odorizzi M, Fernette B, Angel E, Burlet C, Tankosic P, Burlet A. Galanin receptor antagonists decrease fat preference in Brattleboro rat. Neuropharmacology. 2002;42:134-41 pubmed
- Lin C, Zhang M, Huang T, Yang L, Fu H, Zhao L, et al. Spexin Enhances Bowel Movement through Activating L-type Voltage-dependent Calcium Channel via Galanin Receptor 2 in Mice. Sci Rep. 2015;5:12095 pubmed publisher..Our findings provide evidence for important physiological roles of spexin in GI functions. Selective action on spexin pathway might have therapeutic effects on GI diseases with motility disorders. ..
- Sullivan K, Shiao L, Cascieri M. Pharmacological characterization and tissue distribution of the human and rat GALR1 receptors. Biochem Biophys Res Commun. 1997;233:823-8 pubmed..The galanin receptors expressed in CHP-212 cells, like GALR1 have high affinity for galanin (Kd = 0...
- Saar K, Mazarati A, Mahlapuu R, Hallnemo G, Soomets U, Kilk K, et al. Anticonvulsant activity of a nonpeptide galanin receptor agonist. Proc Natl Acad Sci U S A. 2002;99:7136-41 pubmed..No nonpeptide ligands, capable of activating galanin receptors, are available today...
- Kask K, Berthold M, Kahl U, Jureus A, Nordvall G, Langel U, et al. Mutagenesis study on human galanin receptor GalR1 reveals domains involved in ligand binding. Ann N Y Acad Sci. 1998;863:78-85 pubmed
- Gajewska A, Zielińska Górska M, Wasilewska Dziubinska E, Baran M, Kotarba G, Gorski K. Pituitary galaninergic system activity in female rats: the regulatory role of gonadal steroids. J Physiol Pharmacol. 2016;67:423-9 pubmed..Furthermore, the results revealed that progesterone regulates the activity of the pituitary galaninergic system by facilitating estradiol-induced galanin synthesis in the female rat anterior pituitary gland. ..
- Wang S, Hashemi T, He C, Strader C, Bayne M. Molecular cloning and pharmacological characterization of a new galanin receptor subtype. Mol Pharmacol. 1997;52:337-43 pubmed..The identification of galanin(2-29) as a receptor-specific ligand should enhance the understanding of specificity of galanin-receptor interactions. ..
- Ogren S, Kuteeva E, Hokfelt T, Kehr J. Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders. CNS Drugs. 2006;20:633-54 pubmed..This inhibitory effect is related to activation of the galanin receptors located on the dorsal raphe neurons...
- SchrÃ¶dl F, Kaser Eichberger A, Trost A, Strohmaier C, Bogner B, Runge C, et al. Distribution of galanin receptors in the human eye. Exp Eye Res. 2015;138:42-51 pubmed publisher..Presence of GALR1 in ciliary body epithelium and GALR3 in ciliary vessels indicates involvement in aqueous humor production, whereas retinal GALR distribution might contribute to signal transduction. ..
- Xia C, Yuan C, Yuan C. Galanin inhibits the proliferation of glial olfactory ensheathing cells. Neuropeptides. 2005;39:453-9 pubmed..Moreover, the influence can be blocked by M35, a nonspecific antagonist of GAL receptors. It is suggested that GAL is an inhibitory factor in regulating OECs proliferation. ..
- Pham T, Guerrini S, Wong H, Reeve J, Sternini C. Distribution of galanin receptor 1 immunoreactivity in the rat stomach and small intestine. J Comp Neurol. 2002;450:292-302 pubmed