M-15: high-affinity chimeric peptide that blocks the neuronal actions of galanin in the hippocampus, locus coeruleus, and spinal cord
Tamas Bartfai,Katarina Bedecs,Tiit Land,Ülo Langel,Rosalia Bertorelli,P. Girotti,Silvana Consolo,Xiao-Jun Xu,Zsuzsanna Wiesenfeld-Hallin,S. Nilsson +9 more
TLDR
The chimeric peptide M-15 [GAL-(1-13)-substance P-(5-11)amide] represents the first antagonist to the neuronal actions of GAL.Abstract:
The 20-amino acid peptide M-15 binds with high affinity (IC50 approximately 0.1 nM) to 125I-labeled galanin (125I-GAL) binding sites in membranes from the ventral hippocampus, midbrain, and rat spinal cord. Receptor autoradiographic studies show that M-15 can displace 125I-GAL from all labeled sites. M-15 acts as a reversible high-affinity antagonist in blocking the inhibitory effects of GAL on the evoked release of acetylcholine in vivo in the hippocampus and on the GAL-induced hyperpolarization of locus coeruleus neurons in slices. M-15 also blocks the facilitatory effects of GAL on the spinal flexor reflex. Thus, the chimeric peptide M-15 [GAL-(1-13)-substance P-(5-11)amide] represents the first antagonist to the neuronal actions of GAL.read more
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Physiology, Signaling, and Pharmacology of Galanin Peptides and Receptors: Three Decades of Emerging Diversity
Roland Lang,Andrew L. Gundlach,Fiona E. Holmes,Sally A. Hobson,David Wynick,Tomas Hökfelt,Barbara Kofler +6 more
TL;DR: In this review, the importance of novel galanin receptor–specific agonists and antagonists are emphasized, and new approaches, including new transgenic mouse lines (such as a recently characterized GAL3 knockout mouse) represent, in combination with viral-based techniques, critical tools required to better evaluate Galanin system physiology.
Journal ArticleDOI
Expression Cloning of a Rat Hypothalamic Galanin Receptor Coupled to Phosphoinositide Turnover
Kelli E. Smith,Carlos Forray,Mary W. Walker,Kenneth A. Jones,Joseph A. Tamm,Jonathan A. Bard,Theresa Branchek,David L. Linemeyer,Christophe P. G. Gerald +8 more
TL;DR: Activation of GALR2 receptors with porcine Galanin and other galanin analogues increased inositol phospholipid turnover and intracellular calcium levels in stably transfected Chinese hamster ovary cells and generated calcium-activated chloride currents in Xenopus oocytes, suggesting that the rat GALr2 receptor is primarily coupled to the activation of phospholIPase C.
References
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Galanin — a novel biologically active peptide from porcine intestine
TL;DR: It was found that galanin consists of 29 amino acids and the complete amino acid sequence is: contract smooth muscle preparations from the rat and to cause a mild and sustained hyperglycemia in dog.
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A new method for receptor autoradiography: [3H]opioid receptors in rat brain.
W. Scott Young,Michael J. Kuhar +1 more
TL;DR: The distribution of [3H]diprenorphine binding sites determined by this in vitro method is identical to the distribution found in earlier studies utilizing in vivo labeling of opioid receptors.
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Coexistence of galanin-like immunoreactivity with catecholamines, 5- hydroxytryptamine, GABA and neuropeptides in the rat CNS
T. Melander,Tomas Hökfelt,Åke Rökaeus,A.C. Cuello,Wolfgang H. Oertel,A. Verhofstad,Menek Goldstein +6 more
TL;DR: The present results demonstrate that a GAL-like peptide is present in many systems containing other neuroactive compounds, including dopamine, norepinephrine, 5-HT, GABA, and vasopressin.
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Evidence for norepinephrine-mediated collateral inhibition of locus coeruleus neurons
Journal ArticleDOI
Galanin inhibits acetylcholine release in the ventral hippocampus of the rat: histochemical, autoradiographic, in vivo, and in vitro studies.
Gilberto Fisone,Chun F. Wu,Silvana Consolo,Öie Nordström,Niclas Brynne,Tamas Bartfai,T. Melander,Tomas Hökfelt +7 more
TL;DR: It was shown that galanin, in a concentration-dependent manner, inhibited the evoked release of acetylcholine in the ventral, but not in the dorsal, hippocampus of the rat, suggesting that a large proportion of them is localized on cholinergic nerve terminals of septal afferents.