产品说明书
Glycopyrrolate
 |
同义名 : | 甘罗溴铵 ;Glycopyrronium bromide;Glycopyrrolate bromide;NVA 237;Asecryl;NSC 251252;NSC 251251;NSC 250836;AHR 504;Gastrodyn;Robinul |
| CAS号 : | 596-51-0 | |
| 货号 : | A317045 | |
| 分子式 : | C19H28BrNO3 | |
| 纯度 : | 99% | |
| 分子量 : | 398.334 | |
| MDL号 : | MFCD00072137 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(263.6 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 100 mg/mL(251.05 mM)，配合低频超声助溶 |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic. In competition studies, glycopyrrolate and ipratropium bromide bind human peripheral lung and human airway smooth muscle (HASM) muscarinic receptors with affinities in the nanomolar range (K1 values 0.5-3.6 nM). Similar to ipratropium bromide, glycopyrrolate showed no selectivity in its binding to the M1-M3 receptors. Glycopyrrolate bind human and guinea-pig airway muscarinic receptors with high affinity[3]. Glycopyrrolate 1 mg was not superior to placebo, whereas 2 mg showed a significant clinical improvement of nocturnal sialorrhea compared with placebo. Glycopyrrolate seemed to be a tolerable anticholinergic agent in the treatment of clozapine-associated sialorrhea[4]. It has now become common practice to use a dosage ratio of 0.2 mg glycopyrrolate to 1.0 mg neostigmine for NMB (reversal of neuromuscular blockade) reversal[5]. Glycopyrrolate is virtually without side effects to the central nervous system because it penetrates the blood-brain barrier poorly. Glycopyrrolate has a slow and erratic absorption from the gastrointestinal system, but even low plasma levels are associated with a distinct and long-lasting antisialogic effect[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02634983 | Chronic Obstructive Pulmonary ... 展开 >>Disease 收起 << | Phase 3 | Completed | - | United Kingdom ... 展开 >> Novartis Investigative Site Sheffield, South Yorkshire, United Kingdom, S10 2JF Novartis Investigative Site Bradford, West Yorkshire, United Kingdom, BD9 6RJ Novartis Investigative Site Manchester, United Kingdom, M23 9QZ 收起 << |
| NCT01511627 | Hysterectomy | Not Applicable | Withdrawn(Research question wa... 展开 >>s answered by Acta Anaesthesiol Scand 2012; 56 102-109.) 收起 << | - | Canada, Saskatchewan ... 展开 >> Saskatoon City Hospital Saskatoon, Saskatchewan, Canada, S7K0M7 收起 << |
| NCT02325648 | - | Completed | - | Korea, Republic of ... 展开 >> Severance Hospital Seoul, South Korea, Korea, Republic of, 120-752 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.51mL 0.50mL 0.25mL |
12.55mL 2.51mL 1.26mL |
25.10mL 5.02mL 2.51mL |
| 参考文献 |
|---|