galanin receptor

Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of the galanin receptor (Kd = 0.1 nM).

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

Galanin (1-16), mouse, porcine, rat, is a hippocampal galanin receptor agonist (Kd = 3 nM) exhibiting high biological activity on locus coeruleus neurons.

M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

M871 acetate is a selective galanin GAL2 receptor antagonist (Ki values are 13.1 and 420 nM at GAL2 and GAL1 receptors, respectively).It blocks pronociceptive effects of GAL2 agonists including AR-M1896.

Galnon is a galanin receptor agonist, improves intrinsic cortical bone tissue properties

Galnon is a novel non-peptide galanin receptor agonist (GAL1 and GAL2 with Ki of 11.7 and 34.1 μM respectively).

Spexin acetate is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by ad

The chimeric peptide M35 [galanin (1-13)-bradykinin(2-9) amide] is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. The radiolabelled M35 and perf

M1145 acetate, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 acetate shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 acetate has an additive effect on the signal transduction of galanin[1].

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

7-Amino-4-(trifluoromethyl)coumarin (Coumarin 151) is a 5-Hydroxytryptamine Receptor Subtype 1E (HTR1E) antagonist, a Galanin Receptor 2 (GALR2) antagonist, and a hydroxysteroid (17-beta) dehydrogenase 4 (HSD17B4) inhibitor with an activity value of 21 µM.

M617 acetate is a selective agonist of galanin receptor 1 (GAL1). M617 acetate acts through central GAL1, promotes GLUT4 expression, and enhances GLUT4 content in the cardiac muscle of type 2 diabetic rats. The Ki values are 0.23 and 5.71 nM for GAL1 and GAL2, respectively.

Galantide is a reversible and non-specific antagonist of galanin receptor.

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobility in the forced swim test in rats.3It also reduces the hind paw mechanical pain threshold and increases the hind paw cold sensitivity threshold in rats.1

Galanin (Human) (Acetate) is a 30-amino acid neuropeptide and galanin (GAL) receptor agonist.It inhibits forskolin-induced cAMP production in HEK293E cells expressing recombinant human GAL1 receptors (EC50= 0.031 nM) and stimulates inositol phosphate accumulation in CHO cells expressing recombinant human GAL2receptors (EC50= 12.3 nM).Human galanin induces contractions in isolated rat longitudinal fundus strips with an EC50value of 13.8 nM.Intrathecal administration of human galanin (3, 10, and 30 nmol/animal) reduces paw licking and flinching in the second, but not first, phase of the formalin test in rats.

HT-2157 (SNAP-37889) is a selective, high-affinity competitive antagonist of the galanin-3 receptor (Gal3), demonstrating effective inhibition of this target.

Galantide TFA, a reversible and non-specific antagonist of the galanin (GAL) receptor, demonstrates dose-dependent inhibition of galanin-induced K+ conductance, exhibiting an IC50 value of 4 nM. It is utilized in neurological disease and hormone metabolism research [1] [2].

M617 TFA, a selective galanin receptor 1 (GAL1) agonist, exhibits dissociation constants (Kis) of 0.23 nM for GAL1 and 5.71 nM for GAL2. Through activation of GAL1, M617 TFA enhances GLUT4 expression and content in the cardiac muscle of type 2 diabetic rats [1] [2].

M1145 TFA, a chimeric peptide, acts as a selective agonist for the galanin receptor type 2 (GAL2), demonstrating a binding affinity (K i) of 6.55 nM. It exhibits significantly greater selectivity for GAL2, with over 90-fold and 76-fold higher affinity compared to GAL1 (K i = 587 nM) and GalR3 (K i = 497 nM), respectively. Additionally, M1145 TFA enhances galanin signal transduction mechanisms [1].

Spexin TFA, a potent agonist for galanin receptor 2/3 (GAL2/GAL3) with EC50 values of 45.7 and 112.2 nM respectively, shows no significant activity towards galanin receptor 1. As an endogenous peptide promoting satiety, it reduces long chain fatty acid uptake by adipocytes and lowers food consumption in diet-induced obese mice and rats. Additionally, it moderates LH secretion in goldfish and demonstrates anxiolytic effects in vivo.

Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide originally isolated from the porcine hypothalamus, exhibiting high affinity for the GALR2 receptor with an IC50 of 0.24 nM, and comparatively lower affinity for the GALR1 receptor with an IC50 of 4.3 nM [1].

Human GALP (3-32) (Galanin-like peptide (3-32)) serves as a high-affinity agonist for galanin receptors GalR1 (IC50 = 33 nM) and GalR2 (IC50 = 15 nM), as evidenced by competitive binding studies. It demonstrates significant potency in modifying the extracellular acidification rate in SH-SY5Y cells expressing GalR2 (EC50 = 360 nM) [1].