Английская Википедия:Galanin receptor

Содержание

Текст

Текст

Текст

Текст

Текст

Текст

Текст

Текст

Текст

Шаблон:Cs1 config Шаблон:Short description Шаблон:Infobox protein Шаблон:Infobox protein Шаблон:Infobox protein The galanin receptor is a G protein-coupled receptor, or metabotropic receptor which binds galanin.

Galanin receptors can be found throughout the peripheral and central nervous systems and the endocrine system. So far three subtypes are known to exist: GAL-R1, GAL-R2, and GAL-R3. The specific function of each subtype remains to be fully elucidated, although as of 2009 great progress is currently being made in this respect with the generation of receptor subtype-specific knockout mice, and the first selective ligands for galanin receptor subtypes. Selective galanin agonists are anticonvulsant, while antagonists produce antidepressant and anxiolytic effects in animals, so either agonist or antagonist ligands for the galanin receptors may be potentially therapeutic compounds in humans.

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

GAL_1/2 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

External links

• Шаблон:Cite web
• Шаблон:MeshName