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Chemical Compound Review

Galnon     9H-fluoren-9-ylmethyl N-[(1S)-1-[[(1S)-5...

Synonyms: AC1NSKC5, CHEBI:704583, DNC000673, NCGC00165798-01
 
 
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Disease relevance of Galnon

  • Intrahippocampal injection of galnon also shortened the duration of self-sustaining status epilepticus in rats, confirming its agonist properties in vivo [1].
  • While intraperitoneally applied galnon produced no significant effect on mechanical or cold hypersensitivity, it dose-dependently prolonged heat withdrawal latency in nerve-injured rats [2].
  • Systemic galnon, a low-molecular weight galanin receptor agonist, reduces heat hyperalgesia in rats with nerve injury [2].
 

High impact information on Galnon

  • Direct activation of galanin receptors by a galanin receptor agonist, galnon, was found to produce an antidepressant-like effect in the same task [3].
  • Based on known pharmacophores of galanin and the tripeptidomimetic galnon, a combinatorial library was formulated, synthesized, and screened against the galanin receptor [4].
  • The current study addresses whether galanin affects morphine withdrawal signs by using a galanin agonist, galnon, that crosses the blood-brain barrier, and mice genetically engineered to under- or overexpress galanin peptide [5].
  • Pretreatment of rats with antisense peptide nucleic acid targeted to galanin receptor type 1 mRNA abolished the effect of galnon, suggesting mediation of its anticonvulsant properties through this receptor subtype [1].
  • Autoradiographic binding assay on rat spinal cord sections confirmed the ability of galnon to displace (125)I-galanin from its binding sites [1].
 

Biological context of Galnon

 

Anatomical context of Galnon

 

Gene context of Galnon

References

  1. Anticonvulsant activity of a nonpeptide galanin receptor agonist. Saar, K., Mazarati, A.M., Mahlapuu, R., Hallnemo, G., Soomets, U., Kilk, K., Hellberg, S., Pooga, M., Tolf, B.R., Shi, T.S., Hökfelt, T., Wasterlain, C., Bartfai, T., Langel, U. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  2. Systemic galnon, a low-molecular weight galanin receptor agonist, reduces heat hyperalgesia in rats with nerve injury. Wu, W.P., Hao, J.X., Lundström, L., Wiesenfeld-Hallin, Z., Langel, U., Bartfai, T., Xu, X.J. Eur. J. Pharmacol. (2003) [Pubmed]
  3. A role for galanin in antidepressant actions with a focus on the dorsal raphe nucleus. Lu, X., Barr, A.M., Kinney, J.W., Sanna, P., Conti, B., Behrens, M.M., Bartfai, T. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  4. Synthesis of galmic: a nonpeptide galanin receptor agonist. Ceide, S.C., Trembleau, L., Haberhauer, G., Somogyi, L., Lu, X., Bartfai, T., Rebek, J. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  5. The neuropeptide galanin modulates behavioral and neurochemical signs of opiate withdrawal. Zachariou, V., Brunzell, D.H., Hawes, J., Stedman, D.R., Bartfai, T., Steiner, R.A., Wynick, D., Langel, U., Picciotto, M.R. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  6. Regulation of feeding by galnon. Abramov, U., Florén, A., Echevarria, D.J., Brewer, A., Manuzon, H., Robinson, J.K., Bartfai, T., Vasar, E., Langel, U. Neuropeptides (2004) [Pubmed]
  7. Effect of galnon on induction of long-term potentiation in dentate gyrus of C57BL/6 mice. Badie-Mahdavi, H., Behrens, M.M., Rebek, J., Bartfai, T. Neuropeptides (2005) [Pubmed]
  8. Effects of galnon, a non-peptide galanin-receptor agonist, on insulin release from rat pancreatic islets. Quynh, N.T., Islam, S.M., Florén, A., Bartfai, T., Langel, U., Ostenson, C.G. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  9. Multiple interaction sites of galnon trigger its biological effects. Florén, A., Sollenberg, U., Lundström, L., Zorko, M., Stojan, J., Budihna, M., Wheatley, M., Martin, N.P., Kilk, K., Mazarati, A., Bartfai, T., Lindgren, M., Langel, U. Neuropeptides (2005) [Pubmed]
 
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