The galanin receptor is a

G protein-coupled receptor G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related p ...

, or

metabotropic receptor A metabotropic receptor, also referred to by the broader term G-protein-coupled receptor, is a type of membrane receptor that initiates a number of metabolic steps to modulate cell activity. The nervous system utilizes two types of receptors: met ...

which binds

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. Much of galanin's function ...

. 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 Anticonvulsants (also known as antiepileptic drugs or recently as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of b ...

, while antagonists produce

antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...

and

anxiolytic An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxi ...

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 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. Much of galanin's function ...

* Galanin 1-15 fragment *

Galanin-like peptide Galanin-like peptide (GALP) 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 The posterior pituitary (or neurohypophys ...

- 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 In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to ...

)

Antagonists

;Non-selective * M35 peptide ;GAL₁ selective * SCH-202,596 ;GAL₂ selective * M871 peptide ;GAL₃ selective * SNAP-37889 * SNAP-398,299

References

External links

* * {{Neuropeptide receptors G protein-coupled receptors