Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction

Sollenberg, Ulla; Runesson, Johan; Sillard, Rannar; Langel, Ülo

doi:10.1007/s10989-009-9197-9

Cited by 18 publications

(12 citation statements)

References 26 publications

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“…[151] Gal 1 --16 GWTLNSAGYLLGPHAI-amide 4.8 5.7 50 [77] Gal 2 --29 WTLNSAGYLLGPHAIDNHRSFSDKHGLT-amide 85 1.9 12 [77] Gal 3 --29 TLNSAGYLLGPHAIDNHRSFSDKHGLT-amide > 1000 > 1000 > 1000 [77] M15 GWTLNSAGYLLGPQQFFGLM-amide 0.65 1 1 [152] M35 GWTLNSAGYLLGPPPGFSPFR-amide 0.325 3.24 2.09 [152] M40 GWTLNSAGYLLGPPPALALA-amide 6.76 3.55 79.4 [152] M617 GWTLNSAGYLLGPQPGFSPFR-amide 0.23 (h) 5.7 (h) 49 (h) [143,145] M871 WTLNSAGYLLGPEHPPPALALA-amide 420 (h) 13 (h) > 10,000 (h) [144,145] Gal-B2 (Sar)WTLNSAGYLLGPKKK(palmitoyl)K-amide 3.5 (h) 51.5 (h) - [147] J18 RGNWTLNSAGYLLGPkkK(stearoyl)k-amide 138 20 112 [148] Displacement was performed on the rat galanin receptor unless marked (h)-human. Amino acids in lower case are D-isomers.…”

Section: Sch 202596mentioning

confidence: 99%

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Galanin receptors as a potential target for neurological disease

Freimann

Kurrikoff

Langel

2015

Expert Opinion on Therapeutic Targets

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Section: Sch 202596mentioning

confidence: 99%

“…M871 was found to be an GalR2-selective antagonist in vivo [143][144][145]. Many recent studies have designed various other GalR2-selective chimeric ligands [146].…”

Section: Sch 202596mentioning

confidence: 99%

Galanin receptors as a potential target for neurological disease

Freimann

Kurrikoff

Langel

2015

Expert Opinion on Therapeutic Targets

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“…M617 has thereafter been shown to produce anti-nociceptive effects (Jimenez-Andrade et al, 2006) and to delay the development of seizure in an animal model (Mazarati et al, 2006). The M871 peptide is N-terminally truncated and has two additional amino acid residues compared to the M40 peptide and function as a partial agonist, selective for GalR2 (Sollenberg Eriksson et al, 2006, 2010). M871 has been used in several in vivo studies (Jimenez-Andrade et al, 2006; Alier et al, 2007; Kuteeva et al, 2008).…”

Section: Peptide Ligands For the Galanin Receptorsmentioning

confidence: 99%

Galanin Receptors and Ligands

Webling¹,

Runesson²,

Bartfai³

et al. 2012

Front. Endocrin.

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114

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The neuropeptide galanin was first discovered 30 years ago. Today, the galanin family consists of galanin, galanin-like peptide (GALP), galanin-message associated peptide (GMAP), and alarin and this family has been shown to be involved in a wide variety of biological and pathological functions. The effect is mediated through three GPCR subtypes, GalR1-3. The limited number of specific ligands to the galanin receptor subtypes has hindered the understanding of the individual effects of each receptor subtype. This review aims to summarize the current data of the importance of the galanin receptor subtypes and receptor subtype specific agonists and antagonists and their involvement in different biological and pathological functions.

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“…Xu et al, ), indicating that the galanin‐induced antinociception is mediated by GalRs. However, because of the lack of selective GalR agonists and antagonists, the specific receptor type mediating the effect of galanin in pain transmission remained unclear until chimeric peptide M617, galanin(1–13)‐Gln(14)‐bradykinin(2–9)‐amide, was demonstrated to be a new selective agonist of GalR1 (Lundström et al, ; Sollenberg et al, ). The present study analyzes whether M617 can induce antinociceptive effects in the nucleus accumbens (NAc) of rats with experimental sciatic neuropathy.…”

mentioning

confidence: 99%

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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Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction

Cited by 18 publications

References 26 publications

Galanin receptors as a potential target for neurological disease

Galanin receptors as a potential target for neurological disease

Galanin Receptors and Ligands

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

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