Galanin receptor

Ligands

Agonists

;Non-selective

• Galanin
• Galanin 1-15 fragment
• Galanin-like peptide - agonist at GAL1 and GAL2 but not GAL3
• Galmic
• Galnon
• NAX 5055
• D-Gal(7-Ahp)-B2

;GAL1 selective

• M617

;GAL1/2 selective

• M1154 - has no GalR3 interaction

;GAL2 selective

• Galanin 2-11 amide - also called AR-M 1896, anticonvulsant in mice, CAS# 367518-31-8
• M1145 - selective compared to both GalR1 and GalR3
• M1153 - selective compared to both GalR1 and GalR3
• CYM 2503 (positive allosteric modulator)

Antagonists

;Non-selective

• M35 peptide

;GAL1 selective

• SCH-202,596

;GAL2 selective

• M871 peptide

;GAL3 selective

• SNAP-37889
• SNAP-398,299

References

References

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2. (2000). "Galanin receptor subtypes". Trends Pharmacol. Sci..
3. (June 2005). "Galanin impairs performance on learning and memory tasks: findings from galanin transgenic and GAL-R1 knockout mice". Neuropeptides.
4. (August 2008). "Phenotypic analysis of GalR2 knockout mice in anxiety- and depression-related behavioral tests". Neuropeptides.
5. (August 2006). "Regulation of kindling epileptogenesis by hippocampal galanin type 1 and type 2 receptors: The effects of subtype-selective agonists and the role of G-protein-mediated signaling". The Journal of Pharmacology and Experimental Therapeutics.
6. (June 2008). "Galanin and epilepsy". Cellular and Molecular Life Sciences.
7. (February 2009). "Structural Requirements for a Lipoamino Acid in Modulating the Anticonvulsant Activities of Systemically Active Galanin Analogues". Journal of Medicinal Chemistry.
8. (January 2005). "A role for galanin in antidepressant actions with a focus on the dorsal raphe nucleus". Proceedings of the National Academy of Sciences of the United States of America.
9. (September 2006). "A novel, systemically active, selective galanin receptor type-3 ligand exhibits antidepressant-like activity in preclinical tests". Neuroscience Letters.
10. (June 2007). "The brain galanin receptors: targets for novel antidepressant drugs". CNS & Neurological Disorders Drug Targets.
11. (June 2008). "Galanin, galanin receptor subtypes and depression-like behaviour". Cellular and Molecular Life Sciences.
12. (October 2008). "Differential role of galanin receptors in the regulation of depression-like behavior and monoamine/stress-related genes at the cell body level". Neuropsychopharmacology.
13. (November 2004). "Synthesis of galmic: a nonpeptide galanin receptor agonist". Proceedings of the National Academy of Sciences of the United States of America.
14. (October 2007). "Anxiolytic-like activity of the non-selective galanin receptor agonist, galnon". Neuropeptides.
15. (December 2008). "Design, synthesis, and characterization of high-affinity, systemically-active galanin analogues with potent anticonvulsant activities". Journal of Medicinal Chemistry.
16. (April 2009). "Developing novel antiepileptic drugs: characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models". Neurotherapeutics.
17. Robertson, CR. (May 2012). "Generating orally active galanin analogues with analgesic activities". ChemMedChem.
18. (March 2010). "Binding of Chimeric Peptides M617 and M871 to Galanin Receptor Type 3 Reveals Characteristics of Galanin Receptor–Ligand Interaction". International Journal of Peptide Research and Therapeutics.
19. (2010). "M1154 – A Novel Galanin Ligand to Delineate the Galaninergic System". Proceedings of the 31st European Peptide Symposium.
20. (2009). "A novel GalR2-specific peptide agonist". Neuropeptides.
21. (2011). "Novel galanin receptor subtype specific ligands in feeding regulation". Neurochemistry International.
22. Mittapalli, GK. (2014). "Structure Activity Relationships of Novel Antiepileptic Drugs". Curr Med Chem.
23. (2006). "Galanin receptor antagonists : a potential novel pharmacological treatment for mood disorders". CNS Drugs.
24. (November 2005). "Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299". Proceedings of the National Academy of Sciences of the United States of America.
25. (October 2021). "Theoretical investigation of selective ligand binding mode of galanin receptors". Journal of Biomolecular Structure and Dynamics.