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Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests

Academic Article
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Overview

authors

  • Bartfai, Tamas
  • Lu, Xiaoying
  • Badie-Mahdavi, H.
  • Barr, A. M.
  • Mazarati, A.
  • Hua, X. Y.
  • Yaksh, T.
  • Haberhauer, G.
  • Ceide, S. C.
  • Trembleau, L.
  • Somogyi, L.
  • Krock, L.
  • Rebek Jr., Julius

publication date

  • July 2004

journal

  • Proceedings of the National Academy of Sciences of the United States of America  Journal

abstract

  • The pharmacological exploitation of the galanin receptors as drug targets for treatment of epilepsy, depression, and pain has been hampered by the lack of workable compounds for medicinal chemists from random screening of large chemical libraries. The present work uses the tripeptidomimetic galnon and displays its presumed pharmacophores on a rigid molecular scaffold. The scaffold is related to marine natural products and presents three functional groups near one another in space, in a manner reminiscent of a protein surface. An active compound, Galmic, was identified from a small synthetic library and tested in vitro and in vivo for its affinity and efficacy at galanin receptors. Galmic has micromolar affinity for GalR1 receptors (Ki = 34.2 microM) and virtually no affinity for GalR2 receptors. In vitro, Galmic, like galanin, suppresses long-term potentiation in the dentate gyrus; it blocks status epilepticus when injected intrahippocampally or administered i.p. Galmic applied i.p. shows antidepressant-like effects in the forced-swim test, and it is a potent inhibitor of flinching behavior in the inflammatory pain model induced by formalin injection. These data further implicate brain and spinal cord galanin receptors as drug targets and provide an example of a systemically active compound based on a scaffold that mimics protein surfaces.

subject areas

  • Animals
  • CHO Cells
  • Cell Line, Tumor
  • Cricetinae
  • Dentate Gyrus
  • Exploratory Behavior
  • Long-Term Potentiation
  • Male
  • Melanoma
  • Mice
  • Mice, Inbred C57BL
  • Neuronal Plasticity
  • Neuropeptides
  • Pain
  • Pain Measurement
  • Peptides, Cyclic
  • Rats
  • Receptors, Galanin
  • Status Epilepticus
  • Swimming
  • Synaptic Transmission
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Identity

PubMed Central ID

  • PMC478593

International Standard Serial Number (ISSN)

  • 0027-8424

Digital Object Identifier (DOI)

  • 10.1073/pnas.0403802101

PubMed ID

  • 15240875
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Additional Document Info

start page

  • 10470

end page

  • 10475

volume

  • 101

issue

  • 28

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