gal1

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.

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].

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.

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 (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.

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].

Galanin (1-29)(rat, mouse) TFA acts as a non-selective agonist for galanin receptors, exhibiting affinities (Kis) of 0.98 nM for GAL1, 1.48 nM for GAL2, and 1.47 nM for GAL3, respectively, and possesses an anticonvulsant effect [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].

DB21, Galectin-1 Antagonist, is a peptidomimetic conjugated with dibenzofuran, serving as an allosteric inhibitor of galectin-1 (GAL1) interactions with glycans on cell surfaces. This compound enhances the inhibition of angiogenesis and tumor growth in melanoma, lung adenocarcinoma, and ovarian cancer models [1].

Potent and selective galanin receptor 2 (GAL2) agonist (EC50 = 38 nM, Ki values are 6.55, 497 and 587 nM at GAL2, GAL3 and GAL1 respectively). Has an additive effect on the signal transduction of galanin.

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.

Selective galanin GAL1 receptor agonist (Ki values are 0.23 and 5.71 nM for GAL1 and GAL2 receptors respectively). Enhances food consumption in rats following i.c.v. administration and reduces CAP-induced inflammatory pain.

Selective galanin GAL2 receptor antagonist (Ki values are 13.1 and 420 nM for GAL2 and GAL1 receptors respectively). Blocks the pro-nociceptive effect of GAL2 receptor agonists.

Non-selective galanin receptor agonist (Ki values are 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively). Anticonvulsant; prevents the occurrence of full kindled seizures in rats.