The galanin receptor is a G protein-coupled receptor

G protein-coupled receptor

G protein-coupled receptors , also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors , comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal...

, or metabotropic receptor

Metabotropic receptor

Metabotropic receptor is a subtype of membrane receptors at the surface or in vesicles of eukaryotic cells.In the nervous system, based on their structural and functional characteristics, neurotransmitter receptors can be classified into two broad categories: metabotropic and ionotropic receptors...

 which binds galanin

Galanin

Galanin is a neuropeptide encoded by the GAL gene, that is widely expressed in the brain, spinal cord, and gut of humans as well as other mammals. Galanin signaling occurs through three G protein-coupled receptors....

.

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

Galanin receptor 1

Galanin receptor 1 is a G-protein coupled receptor encoded by the GALR1 gene.-Further reading:...

, GAL-R2

Galanin receptor 2

Galanin receptor 2, is a G-protein coupled receptor encoded by the GALR2 gene.-Further reading:...

, and GAL-R3

Galanin receptor 3

Galanin receptor 3 is a G-protein coupled receptor encoded by the GALR3 gene.-Further reading:...

. 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

Anticonvulsant

The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...

, while antagonists produce antidepressant

Antidepressant

An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...

 and anxiolytic

Anxiolytic

An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...

 effects in animals, so either agonist or antagonist ligands for the galanin receptors may be potentially therapeutic compounds in humans.

Agonists

Non-selective

• Galanin
  Galanin
  Galanin is a neuropeptide encoded by the GAL gene, that is widely expressed in the brain, spinal cord, and gut of humans as well as other mammals. Galanin signaling occurs through three G protein-coupled receptors....
  
  
• Galanin 1-15 fragment
• Galanin-like peptide
  Galanin-like peptide
  Galanin-like peptide is a neuropeptide present in humans and other mammals. It is a 60-amino acid polypeptide produced in the arcuate nucleus of the hypothalamus and the posterior pituitary gland. It is involved in the regulation of appetite and may also have other roles such as in inflammation,...
  
   - agonist at GAL₁ and GAL₂ but not GAL₃
• Galmic
  Galmic
  Galmic is a drug which acts as a selective, non-peptide agonist at the galanin receptors GALR. It has anticonvulsant, antidepressant and analgesic effects in animal studies, but also inhibits memory functions....
  
  
• Galnon
  Galnon
  Galnon is a drug which acts as a selective, non-peptide agonist at the galanin receptors GALR. It has anticonvulsant, anxiolytic, anorectic and amnestic effects in animal studies....
  
  
• NAX 5055

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 - seletive compared to both GalR1 and GalR3
• M1153 - seletive compared to both GalR1 and GalR3

Antagonists

Non-selective

• M35 peptide

GAL₁ selective

• SCH-202,596

GAL₂ selective

• M871 peptide

GAL₃ selective

• SNAP-37889
• SNAP-398,299