Galanin receptor subtypes

Branchek, Theresa A.; Smith, Kip; Gerald, Christophe; Walker, Mary W.

doi:10.1016/s0165-6147(00)01446-2

Cited by 451 publications

(320 citation statements)

References 89 publications

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“…This receptor subtype could transmit an excitatory action of galanin, which is mediated via the phospholipase C pathway (see Branchek et al, 2000), as well as by inhibition of the G-protein coupled inwardly rectifying potassium (GIRK) channels (Kerekes et al, 2003). In agreement, activation of the GalR2 receptor in the DR by local infusion of AR-M1896 was shown to increase 5-HT release in the hippocampus (Mazarati et al, 2005), contrary to the profound reduction seen after the i.c.v.…”

Section: Integrative Mechanism Of Galanininergic Regulation Of Depresmentioning

confidence: 87%

“…In contrast, infusion of AR-M1896 into the DR increased 5-HT release in the hippocampus (Mazarati et al, 2005). Since the GalR2 subtype mediates excitatory actions of galanin on neurotransmitter release (see Branchek et al, 2000), it seems likely that AR-M1896 in vivo acts mainly as an agonist at the GalR2 receptor. In the discussion, we, therefore, consider AR-M1896 as a GalR2 receptor agonist, although a potential effect on GalR3 receptor cannot be excluded.…”

Section: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 99%

“…Electrophysiological, behavioral, and neurochemical studies have shown that galanin exerts modulatory (mainly inhibitory) effects on both the noradrenergic and serotonergic systems (Seutin et al, 1989;Sevcik et al, 1993;Pieribone et al, 1995;Xu et al, 1998c;Razani et al, 2001;Kehr et al, 2002;see Ö gren et al, 2006). Moreover, in vivo galanin can modulate 5-HT 1A preand postsynaptic receptor functions in an antagonistic manner (see Fuxe et al, 1998;Misane et al, 1998; The action of galanin is mediated via three G proteincoupled receptors, GalR1-GalR3 (see Branchek et al, 2000), which are expressed in the LC, DR, and their projection areas (Xu et al, 1998b, c;O'Donnell et al, 1999;Burazin et al, 2000;Larm et al, 2003;Hawes and Picciotto, 2004;Hawes et al, 2005;Swanson et al, 2005). Among these receptors, GalR1 and GalR3 mainly activate G i/o types of G proteins mediating inhibitory actions of galanin (Habert-Ortoli et al, 1994;Burgevin et al, 1995;Parker et al, 1995;see Branchek et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

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Differential Role of Galanin Receptors in the Regulation of Depression-Like Behavior and Monoamine/Stress-Related Genes at the Cell Body Level

Kuteeva

Wardi

Lundström

et al. 2008

Neuropsychopharmacol

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The present study on rat examined the role of galanin receptor subtypes in regulation of depression-like behavior as well as potential molecular mechanisms involved in the locus coeruleus (LC) and dorsal raphe (DR). The effect of intracerebroventricular (i.c.v.) infusion of galanin or galanin receptor GalR1-and GalR2-selective ligands was studied in the forced swim test, followed by quantitative in situ hybridization studies. Naive control, non-treated (swim control), saline-and fluoxetine-treated rats were used as controls in the behavioral and in situ hybridization studies. Subchronic treatment with fluoxetine reduced immobility and climbing time. Intracerebroventricular infusion of galanin, the GalR1 agonist M617 or the GalR2 antagonist M871 increased, while the GalR2(R3) agonist AR-M1896 decreased, immobility time compared to the aCSF-treated animals. Galanin also decreased the time of climbing. Galanin mRNA levels were upregulated by the combination of injection + swim stress in the saline-and the fluoxetine-treated groups in the LC, but not in the DR. Also tyrosine hydroxylase levels in the LC were increased following injection + swim stress in the saline-and fluoxetine-treated rats. Tryptophan hydroxylase 2 and serotonin transporter mRNAs were not significantly affected by any treatment. 5-HT 1A mRNA levels were downregulated following i.c.v. galanin, M617 or AR-M1896 infusion. These results indicate a differential role of galanin receptor subtypes in depression-like behavior in rodents: GalR1 subtype may mediate 'prodepressive' and GalR2 'antidepressant' effects of galanin. Galanin has a role in behavioral adaptation to stressful events involving changes of molecules important for noradrenaline and/or serotonin transmission.

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Section: Integrative Mechanism Of Galanininergic Regulation Of Depresmentioning

confidence: 87%

Section: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Differential Role of Galanin Receptors in the Regulation of Depression-Like Behavior and Monoamine/Stress-Related Genes at the Cell Body Level

Kuteeva

Wardi

Lundström

et al. 2008

Neuropsychopharmacol

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“…In addition, it has been demonstrated that GAL act as a neurotransmitter in the NTS (Tan et al, 2004). Three GAL receptors, GalR1, GalR2 and GalR3, have currently been cloned, and they are all G -protein-coupled receptors (GPCRs) (Habert-Ortoli et al, 1994;Branchek et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

Galanin inhibits calcium channels via Gαi-protein mediated by GalR1 in rat nucleus tractus solitarius

et al. 2008

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Galanin (GAL), a 29-amino-acid neuropeptide, is involved in various neuronal functions, including the regulation of food intake, hormone secretion and central cardiovascular regulation. The nucleus tractus solitarius (NTS) is known to plays a major role in the regulation of cardiovascular, respiratory, gustatory, hepatic and swallowing functions.Voltage-dependent Ca 2+ channels (VDCCs) serve as crucial mediators of membrane excitability and Ca 2+ -dependent functions such as neurotransmitter release, enzyme activity and gene expression. The purpose of this study was to investigate the effects of GAL on VDCCs currents (ICa) carried by Ba 2+ (IBa) in the NTS using patch-clamp recording methods. An application of M617 (GalR1 specific agonist), AR-M961 (GAL receptor GalR 1/2 agonist) and GAL caused inhibition of N-and P/Q-types IBa. M617, GAL, and AR-M961 caused inhibition of IBa in a concentration-dependent manner, with IC50's of 678 nM, 325 nM and 573 nM, respectively. This inhibition was relieved, albeit incompletely, by a depolarizing prepulse. Pretreatment with M35 (GalR non-specific antagonist) attenuated the M617-induced inhibition of IBa. Intracellular dialysis of the G i-protein antibody also attenuated the Gal-induced inhibition of IBa. These results indicate that GAL inhibits N-and P/Q-types VDCCs via G i -protein subunits 3 mediated by GalR1 in NTS.

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“…Galanin activates three distinct receptor subtypes that have been cloned and characterized pharmacologically: galanin receptor 1 (GalR1), GalR2, and GalR3 [3,4]. Galanin receptor activation involves different signaling pathways.…”

Section: Introductionmentioning

confidence: 99%

Expression of galanin receptor messenger RNAs in different regions of the rat gastrointestinal tract

et al. 2005

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Galanin effects are mediated by three G-protein-coupled receptors: galanin receptor 1 (GalR1), GalR2 and GalR3. We quantified mRNA levels of GalR1, GalR2 and GalR3 in the rat stomach, small and large intestine using real-time RT-PCR. All three GalR mRNAs were detected throughout the gut at different levels. GalR1 and GalR2 mRNA levels were higher in the large than in the small intestine. GalR2 mRNA was most abundant in the stomach. GalR3 mRNA levels were generally quite low. 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.

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Galanin receptor subtypes

Cited by 451 publications

References 89 publications

Differential Role of Galanin Receptors in the Regulation of Depression-Like Behavior and Monoamine/Stress-Related Genes at the Cell Body Level

Differential Role of Galanin Receptors in the Regulation of Depression-Like Behavior and Monoamine/Stress-Related Genes at the Cell Body Level

Galanin inhibits calcium channels via Gαi-protein mediated by GalR1 in rat nucleus tractus solitarius

Expression of galanin receptor messenger RNAs in different regions of the rat gastrointestinal tract

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