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A galanin receptor ...
A galanin receptor subtype 1 specific agonist
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- Lundström, Linda (author)
- Stockholms universitet,Institutionen för neurokemi och neurotoxikologi
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- Sollenberg, Ulla (author)
- Stockholms universitet,Institutionen för neurokemi och neurotoxikologi
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Brewer, Ariel (author)
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Kouya, Poli Francois (author)
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Zheng, Kang (author)
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- Xu, Xiao-Jun (author)
- Karolinska Institutet
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Xia, Sheng (author)
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Robinson, John K. (author)
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- Wiesenfeld-Hallin, Zsuzsanna (author)
- Karolinska Institutet
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- Xu, Zhi-Qing (author)
- Karolinska Institutet
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- Hökfelt, Tomas (author)
- Karolinska Institutet
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Bartfai, Tamas (author)
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- Langel, Ülo (author)
- Stockholms universitet,Institutionen för neurokemi och neurotoxikologi
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(creator_code:org_t)
- Springer Science and Business Media LLC, 2005
- 2005
- English.
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In: International Journal of Peptide Research and Therapeutics. - : Springer Science and Business Media LLC. - 1573-3904 .- 1573-3149. ; 11:1, s. 17-27
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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http://kipublication...
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Abstract
Subject headings
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- The chimeric peptide M617, galanin(1–13)-Gln14-bradykinin(2–9)amide, is a novel galanin receptor ligand with increased subtype specificity for GalR1 and agonistic activity in cultured cells as well as in vivo. Displacement studies on cell membranes expressing hGalR1 or hGalR2 show the presence of a high affinity binding site for M617 on GalR1 (K i=0.23±.12 nM) while lower affinity was seen towards GalR2 (K i=5.71±1.28 nM) resulting in 25-fold specificity for GalR1. Activation of GalR1 upon stimulation with M617 is further confirmed by internalization of a GalR1-EGFP conjugate. Intracellular signaling studies show the ability of M617 to inhibit forskolin stimulated cAMP formation with 57% and to produce a 5-fold increase in inositol phosphate (IP) accumulation. Agonistic effects on signal transduction are shown on both receptors studied after treatment with M617 in the presence of galanin. In noradrenergic locus coeruleus neurons, M617 induces an outward current even in the presence of TTX plus Ca2+, high Mg2+, suggesting a postsynaptic effect. Intracerebroventricular (i.c.v.) administration of M617 dose-dependently stimulates food uptake in rats while, in contrast, M35 completely fails to affect the feeding behavior. Spinal cord flexor reflex is facilitated by intrathecal (i.t.) administration of M617 as well as galanin with no significant change upon pre-treatment with M617. M617 dose dependently antagonizes the spinal cord hyperexcitablility induced by C-fiber conditioning stimulus and does neither enhance nor antagonize the effect of galanin. These data demonstrate a novel galanin receptor ligand with subtype specificity for GalR1 and agonistic activity, both in vitro and in vivo.
Subject headings
- NATURVETENSKAP -- Biologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences (hsv//eng)
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Keyword
- cAMP production
- chimeric peptide
- feeding behavior
- galanin
- galanin receptor
- inositol phosphate production
- locus coeruleus
- nociception
- receptor internalization
- receptor specificity
Publication and Content Type
- ref (subject category)
- art (subject category)
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To the university's database
- By the author/editor
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Lundström, Linda
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Sollenberg, Ulla
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Brewer, Ariel
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Kouya, Poli Fran ...
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Zheng, Kang
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Xu, Xiao-Jun
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show more...
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Xia, Sheng
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Robinson, John K ...
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Wiesenfeld-Halli ...
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Xu, Zhi-Qing
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Hökfelt, Tomas
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Bartfai, Tamas
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Langel, Ülo
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Biological Scien ...
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
- Articles in the publication
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International Jo ...
- By the university
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Stockholm University
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Karolinska Institutet