| Description | 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). |
| In vitro | Galantide acetate不激活K+传导，但以浓度依赖的方式对galanin诱导的K+传导增加产生拮抗作用（IC50=4 nM）。Galantide acetate的作用类似galanin，抑制电压依赖的Ba2+电流（IBa）。IBa的抑制也是浓度依赖的（IC50=16 nM），galantide产生的最大抑制率约为40%[3]。 |
| In vivo | 经颅脑室内注射 Galantide acetate （5微克/只大鼠）能够抑制有经验的雄性大鼠的性行为，而不会产生其他运动或行为缺陷。通过相同途径注射galanin的拮抗剂Galantide（1或2微克/只大鼠）则能刺激性行为（提高唤醒、动机和表现指标），并拮抗galanin的效果[2]。 Galantide acetate 对改善轻度急性胰腺炎（AP）有益。 Galantide acetate 显著降低AP引起的高酶血症，降低幅度为41-49%[3]。经颅脑室内（i.c.v.）注射 Galantide acetate ，在6-6000 nM剂量范围内，已经被发现可以在“社交认知”测试中改善社会记忆[4]。 |
| Synonyms | Galantide acetate(138579-66-5 Free base) |
| molecular weight | 2259.58 |
| Molecular formula | C106H155N25O28S |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Langel U, et al. Design of chimeric peptide ligands to galanin receptors and substance P receptors. Int J Pept Protein Res. 1992;39(6):516-522. 2. Lindskog S, et al. The novel high-affinity antagonist, galantide, blocks the galanin-mediated inhibition of glucose-induced insulin secretion. Eur J Pharmacol. 1992;210(2):183-188. 3. Mulvaney JM, et al. Galantide distinguishes putative subtypes of galanin receptors in mudpuppy parasympathetic neurons. Eur J Pharmacol. 1995;287(1):97-100. |