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Glycopyrrolate (Synonyms: AHR 504, NSC 250836, NSC 251251, NSC 251252)

رقم الكتالوجGC15029

Glycopyrrolate (Glycopyrronium bromide) هو مضاد تنافسي مسكاريني يستخدم كمضاد للتشنج

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Glycopyrrolate التركيب الكيميائي

Cas No.: 596-51-0

الحجم السعر المخزون الكميّة
5mg
17٫00
متوفر
10mM (in 1mL DMSO)
19٫00
متوفر
10mg
25٫00
متوفر
25mg
39٫00
متوفر
50mg
53٫00
متوفر
100mg
77٫00
متوفر
500mg
199٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Glycopyrrolate

Glycopyrrolate (Glycopyrronium bromide) is a muscarinic competitive antagonist used as an antispasmodic.IC50 Value:Target: mAChR (Muscarinic acetylcholine receptor M1)in vitro: Glycopyrrolate showed no selectivity in its binding to the M1-M3 receptors. Kinetics studies, however, showed that glycopyrrolate dissociates slowly from HASM muscarinic receptors (60% protection against [3H]-NMS binding at 30 nM) compared to ipratropium bromide [1].in vivo: Glycopyrrolate (1 mg) tablets were then administered, starting with one tablet daily the third week and increasing the daily dose by one tablet per week until a maximum of four tablets during week six and 4 days of week seven when the daily dose was reduced to two tablets for 3 days. glycopyrrolate can be given in controlled doses provided that an adequate medical assessment has been undertaken [2]. 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 [3]. Oral glycopyrrolate is emerging as a potential second-line treatment option, but experience with safety, efficacy, and dosing is especially limited in children [4]. phase III study, 52.3% of glycopyrrolate oral solution recipients (aged 3-18 years; n = 137) had an mTDS response (primary endpoint); the response rate was consistently above 50% at all 4-weekly timepoints, aside from the first assessment at week 4 (40.3%). In general, glycopyrrolate oral solution was well tolerated in clinical trials. The majority of adverse events were within expectations as characteristic anticholinergic outcomes [5].Toxicity: Side effects include dry mouth, difficult urinating, heachaches, diarrhea and constipation. The medication also induces drowsiness or blurred vision. LD50=709 mg/kg (rat, oral).

References:
[1]. Haddad, E.B., et al., Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br J Pharmacol, 1999. 127(2): p. 413-20.
[2]. Neverlien, P.O., et al., Glycopyrrolate treatment of drooling in an adult male patient with cerebral palsy. Clin Exp Pharmacol Physiol, 2000. 27(4): p. 320-2.
[3]. Olsen, A.K. and P. Sjogren, Oral glycopyrrolate alleviates drooling in a patient with tongue cancer. J Pain Symptom Manage, 1999. 18(4): p. 300-2.
[4]. Kumar, M.G., et al., Oral Glycopyrrolate for Refractory Pediatric and Adolescent Hyperhidrosis. Pediatr Dermatol, 2013.
[5]. Garnock-Jones, K.P., Glycopyrrolate oral solution: for chronic, severe drooling in pediatric patients with neurologic conditions. Paediatr Drugs, 2012. 14(4): p. 263-9.

Chemical Properties of Glycopyrrolate

Cas No. 596-51-0 SDF
المرادفات AHR 504, NSC 250836, NSC 251251, NSC 251252
Chemical Name (1,1-dimethylpyrrolidin-1-ium-3-yl) 2-cyclopentyl-2-hydroxy-2-phenylacetate;bromide
Canonical SMILES C[N+]1(CCC(C1)OC(=O)C(C2CCCC2)(C3=CC=CC=C3)O)C.[Br-]
Formula C19H28BrNO3 M.Wt 398.33
الذوبان ≥ 19.9mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Glycopyrrolate

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1 mg 5 mg 10 mg
1 mM 2.5105 mL 12.5524 mL 25.1048 mL
5 mM 0.5021 mL 2.5105 mL 5.021 mL
10 mM 0.251 mL 1.2552 mL 2.5105 mL
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