Glycopyrrolate (Synonyms: AHR 504, NSC 250836, NSC 251251, NSC 251252) |
رقم الكتالوجGC15029 |
Glycopyrrolate (Glycopyrronium bromide) هو مضاد تنافسي مسكاريني يستخدم كمضاد للتشنج
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 596-51-0
Sample solution is provided at 25 µL, 10mM.
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.
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. |
Prepare stock solution | |||
![]() |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 13 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *