Galanin—10 years with a neuroendocrine peptide

Galanin—10 years with a neuroendocrine peptide Galanin is a 29 30 amino acids long neuropeptide which does not belong to any known peptide family. The N-terminal first 16 amino acids of the molecule are both necessary and sufficient for receptor recognition and receptor activation. The main pharmacophores of galanin in its central and pancreatic actions are Gly 1 , Trp 2 , Asn 5 and Tyr 9 , respectively. The neuropeptide galanin has multiple effects in both the central and peripheral nervous systems. Centrally, galanin potently stimulates fat intake and impairs cognitive performance. Anoxic glutamate release in the hippocampus is inhibited by galanin and the noradrenergic tonus in the brain is influenced by a hyperpolarizing action of galanin in the locus coeruleus. In the spinal cord galanin inhibits spinal excitability and potentiates the analgesic effect of morphine. In the neuroendocrine system galanin acts in a stimulatory manner on the release of growth hormone and prolactin, and peripherally galanin inhibits glucose induced insulin release. Galanin also causes contraction of the jejunum. The galanin receptor is a G i -protein-coupled, membrane-bound glycoprotein with an estimated molecular mass of 53 kDa. Several putative tissue specific galanin receptor subtypes have been proposed on a pharmacological basis. The distribution of galanin receptors and of galanin like immunoreactivity are overlapping in the CNS, both being high in areas such as the locus coeruleus, raphe nucleus and hypothalamus. Galanin receptor activation leads to a reduced intracellular Ca 2+ -concentration, either by direct action on voltage sensitive Ca 2+ -channels or indirectly via opening of K + -channels or via inhibition of adenylyl cyclase activity. The lowered intracellular Ca 2+ level subsequently leads to a reduced PLC activity. Galanin also inhibits cGMP synthesis induced by depolarization. A number of synthetic high affinity galanin receptor antagonists of the peptide type were developed recently, which have enabled the elucidation of functional roles of endogenous galanin in several systems. Furthermore, putative subtypes of galanin receptors can be distinguished by the use of these new galanin receptor ligands. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png The International Journal of Biochemistry & Cell Biology Elsevier

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Publisher
Elsevier
Copyright
Copyright © 1995 Elsevier Ltd
ISSN
1357-2725
eISSN
1878-5875
DOI
10.1016/1357-2725(95)00008-D
Publisher site
See Article on Publisher Site

Abstract

Galanin is a 29 30 amino acids long neuropeptide which does not belong to any known peptide family. The N-terminal first 16 amino acids of the molecule are both necessary and sufficient for receptor recognition and receptor activation. The main pharmacophores of galanin in its central and pancreatic actions are Gly 1 , Trp 2 , Asn 5 and Tyr 9 , respectively. The neuropeptide galanin has multiple effects in both the central and peripheral nervous systems. Centrally, galanin potently stimulates fat intake and impairs cognitive performance. Anoxic glutamate release in the hippocampus is inhibited by galanin and the noradrenergic tonus in the brain is influenced by a hyperpolarizing action of galanin in the locus coeruleus. In the spinal cord galanin inhibits spinal excitability and potentiates the analgesic effect of morphine. In the neuroendocrine system galanin acts in a stimulatory manner on the release of growth hormone and prolactin, and peripherally galanin inhibits glucose induced insulin release. Galanin also causes contraction of the jejunum. The galanin receptor is a G i -protein-coupled, membrane-bound glycoprotein with an estimated molecular mass of 53 kDa. Several putative tissue specific galanin receptor subtypes have been proposed on a pharmacological basis. The distribution of galanin receptors and of galanin like immunoreactivity are overlapping in the CNS, both being high in areas such as the locus coeruleus, raphe nucleus and hypothalamus. Galanin receptor activation leads to a reduced intracellular Ca 2+ -concentration, either by direct action on voltage sensitive Ca 2+ -channels or indirectly via opening of K + -channels or via inhibition of adenylyl cyclase activity. The lowered intracellular Ca 2+ level subsequently leads to a reduced PLC activity. Galanin also inhibits cGMP synthesis induced by depolarization. A number of synthetic high affinity galanin receptor antagonists of the peptide type were developed recently, which have enabled the elucidation of functional roles of endogenous galanin in several systems. Furthermore, putative subtypes of galanin receptors can be distinguished by the use of these new galanin receptor ligands.

Journal

The International Journal of Biochemistry & Cell BiologyElsevier

Published: Apr 1, 1995

References

  • Galanin: neuromodulatory and direct contractile effects on smooth muscle preparations
    Ekblad, E.; Häkanson, R.; Sundler, F.; Wahlestedt, C.
  • Distribution of galanin-binding sites in the monkey and human telencephalon: preliminary observations
    Köhler, C.; Persson, A.; Melander, T.; Theodorsson, E.; Sedvall, G.; Hökfelt, T.
  • Distribution of galanin-like immunoreactivity in the gastro-intestinal tract of several mammalian species
    Melander, T.; Hökfelt, T.; Rökaeus, Å.; Fahrenkrug, J.; Tatemoto, K.; Mutt, V.
  • Galanin reduces carbachol stimulation of phosphoinositide turnover in rat ventral hippocampus by lowering Ca 2+ influx through voltage-sensitive Ca 2+ channels
    Palazzi, E.; Felinska, S.; Zambelli, M.; Fisone, G.; Bartfai, T.; Consolo, S.
  • On the Solution Structure of Galanin
    Rigler, R.; Wennerberg, A.; Cooke, R.M.; Elofson, A.; Nilsson, L.; Vogel, H.; Holley, L.M.; Carlquist, M.; Langel, Ü.; Bartfai, T.; Campbell, I.D.
  • Mechanism of action of galanin on myenteric neurons
    Tamura, K.; Palmer, J.M.; Winkelmann, C.K.; Wood, J.D.

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