| Description | Galnon is a novel non-peptide galanin receptor agonist (GAL1 and GAL2 with Ki of 11.7 and 34.1 μM respectively). |
| In vivo | Galnon 在分离的Wistar大鼠胰岛中强力刺激胰岛素释放；100μM浓度的该化合物在3.3 mM和16.7 mM葡萄糖浓度下分别使释放量增加8.5倍（p<0.001）和3.7倍（p<0.001）。在胰岛灌流实验中，galnon也显著增强了对葡萄糖反应中胰岛素响应的急性及晚期几个阶段。此外，galnon在GK大鼠胰岛中也刺激了胰岛素释放。这些效果并未被galanin或其受体拮抗剂M35的存在所抑制。Galnon的刺激效果在16.7 mM但非3.3 mM葡萄糖浓度下被PKA和PKC抑制剂H-89和calphostin C部分抑制。在Wistar和GK大鼠胰岛中，30 mM KCl的去极化作用刺激了胰岛素释放，而100μMgalnon进一步增强了胰岛素释放1.5-2倍（p<0.05）。通过fura-2确定的细胞内钙水平与胰岛素释放同步增加，L型Ca2+通道阻断剂nimodipine抑制了对葡萄糖和galnon的胰岛素反应。作为GAL受体激动剂的galnon可能在OVX大鼠中增强破骨细胞的骨吸收。尽管galnon减少了骨量，生物力学测试显示galnon处理的动物的骨骼按单位面积计算具有更优的机械性能。综合来看，galnon在刺激OVX大鼠模型中的破骨活性的同时，同时改善了皮质骨的内在质量。 |
| Animal experiments | OVX rats were treated with either vehicle or galnon for 6 weeks via mini-osmotic pumps. Plasma osteocalcin concentrations, osseous cell gene expression, morphological and biomechanical properties of the skeleton were compared between the two groups[2] |
| molecular weight | 792.84 |
| Molecular formula | C42H47F3N4O8 |
| CAS | 1217448-19-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (269.28 mM) |
| References | 1. Quynh N T T , Islam S M , Anders Florén, et al. Effects of galnon, a non-peptide galanin-receptor agonist, on insulin release from rat pancreatic islets[J]. Biochem Biophys Res Commun, 2005, 328(1):213-220. 2. Mcgowan H W , Schuijers J A , Grills B L , et al. Galnon, a galanin receptor agonist, improves intrinsic cortical bone tissue properties but exacerbates bone loss in an ovariectomised rat model[J]. Journal of musculoskeletal & neuronal interactions, 2014, 14(2):162-172. |