Summary of the probe development effort to identify antagonists of the Galanin Receptor 3 (GALR3)
Name: Summary of the probe development effort to identify antagonists of the Galanin Receptor 3 (GALR3). ..more
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Patricia McDonald, The Scripps Research Institute
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: 1 R21 NS067631-01
Grant Proposal PI: Patricia McDonald, The Scripps Research Institute
External Assay ID: GALR3_ANT_SUMMARY
Name: Summary of the probe development effort to identify antagonists of the Galanin Receptor 3 (GALR3).
Galanin, a 29 amino acid neuropeptide (30 residues in humans), is cleaved from preprogalanin and is involved in many physiological processes including nervous system development, feeding, metabolism and reproduction, and regulation of neurotransmitter and hormone release (1, 2). The physiologic response to galanin is mediated in part by three G protein-coupled metabotropic 7-transmembrane receptor subtypes, GALR1, GALR2 and GALR3. These receptors are expressed throughout the peripheral and central nervous systems as well as the endocrine system. Both GALR1 and GALR2 are widely expressed in the CNS whereas GALR3 is the least abundantly expressed of the galanin receptor subtypes. The GALR3 in particular has been strongly implicated in addiction and mood related disorders such as anxiety and depression. It has been the target of many drug discovery programs within the pharmaceutical industry but despite the significant resources and effort devoted to discovery of galanin receptor subtype selective small molecule modulators, there have been very few reports for the discovery of such molecules and in addition, all access to primary screening data remains proprietary information. As a result the identification of novel GALR3 antagonists would serve as useful tools for understanding galanin biology and for possible investigations into the role of GALR3 in addiction and mood disorders (3-5).
Summary of Probe Development Effort:
This probe development effort is focused on the identification of antagonists of the Galanin Receptor 3 (GALR3). All AIDs that contain results associated with this project can be found in the "Related Bioassays" section of this Summary AID.
1. Walton, K. M., Chin, J. E., Duplantier, A. J., and Mather, R. J. Galanin function in the central nervous system. Current opinion in drug discovery & development, 2006. 9(5): p. 560-570.
2. Wrenn, C. C., and Holmes, A. The role of galanin in modulating stress-related neural pathways. Drug news & perspectives, 2006. 19(8).
3. Swanson, C.J., et al., Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A, 2005. 102(48): p. 17489-94.
4. Packiarajan, M, - 2,4,6-Triaminopyrimidines for the treatment of depression and/or anxiety. US Patent 6936607, 2005.
5. Packiarajan, M, Use of GAL3 antagonist for treatment of depression and/or anxiety and compounds useful in such methods. US Patent 7465750, 2008.
Summary, Summary AID, PRUN, CNG, ActOne, Galanin receptor, anxiety, addiction, mood, pain, CNS, receptor, galanin, cAMP, fluor, fluorescence, forskolin, membrane potential, dye, FLIPR, Gi, G-protein, biosensor, GALR3, antagonist, inhibitor, HTS, primary, dose response screen, G protein coupled receptor, GPCR, 1536, inhibit, decrease, high throughput screen, 1536, Scripps Florida, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.