A Galanin Receptor Subtype 1 Specific Agonist

Lundström, Linda; Sollenberg, Ulla; Brewer, Ariel; Kouya, Poli Francois; Zheng, Kang; Xu, Xiao‐Jun; Sheng, Xia; Robinson, John K.; Wiesenfeld‐Hallin, Zsuzsanna; Xu, Zhi‐Qing David; Hökfelt, Tomas; Bartfai, Tamás; Langel, Ülo

doi:10.1007/s10989-004-1717-z

Cited by 47 publications

(37 citation statements)

References 36 publications

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“…Neither M617 nor M871 were yet tested with respect to the GalR3 receptor subtype. Both in vitro and in vivo studies support the view that M617 acts as GalR1 agonist, and M871 is an antagonist at the GalR2 receptor (Lundström et al, 2005;Sollenberg et al, 2006). Galanin (2-12), AR-M1896, was first described as a high affinity GalR2 selective agonist with a nanomolar affinity (Liu et al, 2001).…”

Section: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 78%

“…A microinfusion pump (CMA/Microdialysis) and Hamilton syringe (25 ml) were used to infuse rat galanin (3 nmol per rat), the GalR1 agonist M617 (3 nmol), the GalR2(R3) agonist AR-M1896 (1 nmol) or the GalR2 antagonist M871 (3 nmol), or aCSF for the control group (see Figure 1 for the details). The dose of galanin was based on earlier in vivo results in the FST (Kuteeva et al, 2007), and the selection of doses for the galanin receptor-selective peptides was based on their relative in vitro affinity for the galanin receptors compared to galanin itself (Lundström et al, 2005;Sollenberg et al, 2006). The aCSF and peptide solutions (dissolved in aCSF) were freshly made and coded before the i.c.v.…”

Section: Stereotaxic Surgerymentioning

confidence: 99%

“…In vitro studies have indicated that M617 exhibits a 25-fold subtype specificity for GalR1 vs GalR2 (Lundström et al, 2005), while M871 binds to the GalR2 with a 32-fold higher affinity than to GalR1 (Sollenberg et al, 2006). Neither M617 nor M871 were yet tested with respect to the GalR3 receptor subtype.…”

Section: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 99%

“…Recently, both peptidergic and non-peptidergic compounds with relatively high selectivity for galanin receptor subtypes have been developed (Lundström et al, 2005;Swanson et al, 2005;Barr et al, 2006;Sollenberg et al, 2006), allowing studies on selective involvement of galanin receptor subtypes in regulation of physiological functions. For instance, newly developed non-peptide GalR3 antagonists, when given by systemic routes, were shown to have an antidepressant-like activity in behavioral models of anxiety and depression (Swanson et al, 2005;Barr et al, 2006).…”

Section: Introductionmentioning

confidence: 99%

“…The purpose of the present study was to assess the role of galanin receptor subtypes in depression-like behavior, using selective peptide ligands for the GalR1 and GalR2 receptors (Liu et al, 2001;Lundström et al, 2005;Sollenberg et al, 2006). As stress is involved in the pathogenesis of depression, the effects of forced swim on the endogenous galanin systems of the LC and DR was studied by in situ hybridization.…”

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: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 78%

Section: Stereotaxic Surgerymentioning

confidence: 99%

Section: Galanin Receptor Selectivity Of the Peptidergic Ligandsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

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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Antinociceptive roles of galanin receptor 1 in nucleus accumbens of rats in a model of neuropathic pain

Duan

Zhang

et al. 2015

J of Neuroscience Research

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It has been reported that galanin and its receptors might be involved in the modulation and transmission of nociception in the central nervous system. Our previous research has also demonstrated that galanin induces antinociception in the nucleus accumbens (NAc) of intact rats. However, the interaction between galanin and its receptors in the NAc and the underlying mechanism of suppressing pain transmission remain unclear. The present study seeks to determine the antinociception induced by galanin receptor (GalR)-1 stimulation in the NAc of rats with neuropathic pain. The left sciatic nerve of rats was ligated to mimic a neuropathic pain model. Western blots showed that the expression of GalR1 was significantly upregulated in the NAc of rats with neuropathic pain. Intra-NAc injection of GalR1 agonist M617 induced a dose-dependent increase in hindpaw withdrawal latency (HWL) to noxious thermal and mechanical stimulations in rats with neuropathic pain. Also, the effect of M617 was attenuated by M35, a GalR1/2 antagonist; at the same time, M35 reduced the galanin-induced antinociception, suggesting that GalR1 mediates antinociception induced by galanin in the NAc of rats with neuropathic pain. Furthermore, we found that M617-induced antinociception in rats with neuropathic pain was stronger than the antinociception in intact rats. We also found that injections of M617 and galanin each induced significant increases in HWL, but the galanin-induced antinociception was stronger than that of M617. All these results suggest that GalR1 plays an important role in antinociception and that other GalRs also are involved in pain modulation induced by galanin in the NAc of rats with neuropathic pain.

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