Galanin receptor ligands
نویسنده
چکیده
The three galanin receptor subtypes (GalR1-3) belong to the G protein-coupled receptor superfamily. The widespread distribution of galanin and its receptors in the CNS and PNS and the numerous physiological and pharmacological effects of galanin (for review, cf. Vrontakis, 2002) render the three galanin receptors attractive drug targets. The industrial efforts, however, have not yet resulted in a wealth of receptor subtype specific agonists or antagonists with high affinity and selectivity. The present paper summarizes the properties of the galanin ligands used at the end of 2004 in the ca. 2000 publications and complements their pharmacological characterization with new data.
منابع مشابه
Galanin Receptors and Ligands
The neuropeptide galanin was first discovered 30 years ago. Today, the galanin family consists of galanin, galanin-like peptide (GALP), galanin-message associated peptide (GMAP), and alarin and this family has been shown to be involved in a wide variety of biological and pathological functions. The effect is mediated through three GPCR subtypes, GalR1-3. The limited number of specific ligands t...
متن کاملSubtype selective activation and molecular characterization of galanin receptors
A galanin receptor subtype 1 specific agonist. M871 – a novel peptide antagonist selectively recognizing the galanin receptor type 2. Molecular characterization of the ligand binding site of the human galanin receptor type 2, identifying subtype selective interactions. Regulation of kindling epileptogenesis by hippocampal galanin type 1 and type 2 receptors: the effects of subtype selective ago...
متن کاملGalanin Receptor Ligands Contents
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متن کاملSynthesis of galmic: a nonpeptide galanin receptor agonist.
Galanin is a neuropeptide with a wide variety of biological functions. Few nonpeptide ligands, capable of activating galanin receptors, are available today. Based on known pharmacophores of galanin and the tripeptidomimetic galnon, a combinatorial library was formulated, synthesized, and screened against the galanin receptor. An active compound, galmic, was identified and tested in vitro and in...
متن کاملAla5-galanin (2–11) is a GAL2R specific galanin analogue
It is over 30years since the regulatory peptide galanin was discovered by Professor Mutt and co-workers. Galanin exerts its effects by binding to three galanin G-protein coupled receptors, namely GAL1R, GAL2R and GAL3R. Each galanin receptor has a different distribution in the central nervous system and the peripheral nervous system as well as distinctive signaling pathways, which implicates th...
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