货号:A317045 同义名: 甘罗溴铵 / Glycopyrronium bromide;Glycopyrrolate bromide
Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.
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产品名称 | AChE ↓ ↑ | AChR ↓ ↑ | mAChR ↓ ↑ | nAChR ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Donepezil |
+++
hAChE, IC50: 11.6 nM bAChE, IC50: 8.12 nM |
98% | |||||||||||||||||
Loganin |
++
AChE, IC50: 3.95 μM |
99%+ | |||||||||||||||||
topride HCl |
++
AChE, IC50: 2.04 μM |
98% | |||||||||||||||||
Dehydroevodiamine HCl | ✔ | 99%+ | |||||||||||||||||
Jatrorrhizine |
++
AChE, IC50: 872 nM |
99%+ | |||||||||||||||||
Palmatine |
++
AChE, IC50: 0.51 μM |
98% | |||||||||||||||||
(-)-Huperzine A |
++++
AChE (G4 form), Ki: 7 nM |
98% | |||||||||||||||||
Galanthamine HBr |
++
AChE, IC50: 0.35 μM |
98% | |||||||||||||||||
Trospium chloride | ✔ | 99% | |||||||||||||||||
Tiotropium Bromide Monohydrate | ✔ | 98+% | |||||||||||||||||
Gallamine Triethiodide |
+
AChR, IC50: 68.0 μM |
98% | |||||||||||||||||
Hexamethonium Bromide | ✔ | 99% | |||||||||||||||||
Pancuronium dibromide | ✔ | 98% | |||||||||||||||||
Neostigmine bromide | ✔ | 98% | |||||||||||||||||
Orphenadrine citrate | ✔ | 98% | |||||||||||||||||
Oxybutynin | ✔ | 98% | |||||||||||||||||
Irsogladine | ✔ | PDE | 98% | ||||||||||||||||
Pyridostigmine bromide | ✔ | 99+% | |||||||||||||||||
Rivastigmine |
+
AChR, IC50: 5.5 μM |
98% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | 97% | |||||||||||||||||
Rocuronium Bromide | ✔ | 98% | |||||||||||||||||
Tropicamide |
+++
M4 mAChR, IC50: 8 nM |
98% | |||||||||||||||||
Diphenmanil methylsulfate | ✔ | 98% | |||||||||||||||||
Umeclidinium bromide | ✔ | 95% | |||||||||||||||||
Otilonium bromide | ✔ | 98% | |||||||||||||||||
Flavoxate HCl |
+
mAChR, IC50: 12.2 μM |
98% | |||||||||||||||||
Ipratropium bromide | ✔ | 98% | |||||||||||||||||
Diphenidol HCl | ✔ | 98% | |||||||||||||||||
Darifenacin hydrobromide |
++++
M3 mAChR, pKi: 8.9 |
98% | |||||||||||||||||
Aclidinium Bromide |
++++
M4 mAChR, Ki: 0.21 nM M2 mAChR, Ki: 0.1 nM |
98% | |||||||||||||||||
Oxybutynin chloride | ✔ | 99% | |||||||||||||||||
Pentoxyverine citrate | ✔ | 98% | |||||||||||||||||
Solifenacin | ✔ | 98% | |||||||||||||||||
Catharanthine | ✔ | 98% | |||||||||||||||||
Benzethonium chloride |
+++
α4β2 nAChRs, IC50: 49 nM α7 nAChRs, IC50: 122 nM |
99+% | |||||||||||||||||
Vinblastine sulfate |
+
nAChR, IC50: 8.9 μM |
99% | |||||||||||||||||
PNU-120596 |
++
α7 nAChR, EC50: 216 nM |
99+% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
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 << | |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 596-51-0 |
分子式 | C19H28BrNO3 |
分子量 | 398.334 |
别名 | 甘罗溴铵 ;Glycopyrronium bromide;Glycopyrrolate bromide;NVA 237;Asecryl;NSC 251252;NSC 251251;NSC 250836;AHR 504;Gastrodyn;Robinul |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
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 |