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格隆溴铵 /Glycopyrrolate {[allProObj[0].p_purity_real_show]}

货号:A317045 同义名: 甘罗溴铵 / Glycopyrronium bromide;Glycopyrrolate bromide

Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.

Glycopyrrolate 化学结构 CAS号:596-51-0
Glycopyrrolate 化学结构
CAS号:596-51-0
Glycopyrrolate 3D分子结构
CAS号:596-51-0
Glycopyrrolate 化学结构 CAS号:596-51-0
Glycopyrrolate 3D分子结构 CAS号:596-51-0
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Glycopyrrolate 纯度/质量文件 产品仅供科研

货号:A317045 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Glycopyrrolate 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].

Glycopyrrolate 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 <<

Glycopyrrolate 参考文献

[1]Kim HC, Lim SM, et al. Effect of glycopyrrolate versus atropine coadministered with neostigmine for reversal of rocuronium on postoperative catheter-related bladder discomfort in patients undergoing transurethral resection of bladder tumor: a prospective randomized study. J Anesth. 2015 Dec;29(6):831-5.

[2]Blissit KT, Tillery E, et al. Glycopyrrolate for treatment of clozapine-induced sialorrhea in adults. Am J Health Syst Pharm. 2014 Aug 1;71(15):1282-7.

[3]Haddad EB, Patel H, Keeling JE, Yacoub MH, Barnes PJ, Belvisi MG. Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br J Pharmacol. 1999;127(2):413‐420

[4]Man WH, Colen-de Koning JC, Schulte PF, et al. The Effect of Glycopyrrolate on Nocturnal Sialorrhea in Patients Using Clozapine: A Randomized, Crossover, Double-Blind, Placebo-Controlled Trial. J Clin Psychopharmacol. 2017;37(2):155‐161

[5]Howard J, Wigley J, Rosen G, D'mello J. Glycopyrrolate: It's time to review. J Clin Anesth. 2017;36:51‐53

[6]Olsen AK, Sjøgren P. Oral glycopyrrolate alleviates drooling in a patient with tongue cancer. J Pain Symptom Manage. 1999;18(4):300‐302

Glycopyrrolate 实验方案

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

Glycopyrrolate 技术信息

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
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