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Glycopyrrolate

CAS No. : 596-51-0

Biological Activity：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).

Research Area：Neurological Disease

Targets：mAChR

Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;FDA-Approved Drug Library Mini;Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Neuronal Signaling Compound Library;FDA-Approved Drug Library;Anti-Cancer Compound Library;CNS-Penetrant Compound Library;Drug Repurposing Compound Library;NMPA-Approved Drug Library;Orally Active Compound Library;Neurotransmitter Receptor Compound Library;FDA Approved & Pharmacopeial Drug Library;Drug-Induced Liver Injury (DILI) Compound Library;Anti-Parkinson’s Disease Compound Library;Neurodegenerative Disease-related Compound Library;Rare Diseases Drug Library;Children’s Drug Library;FDA-Approved Anticancer Drug Library;Human Metabolite Library;

Related Small Molecules:VU0357017 hydrochloride;TBPB;Imidafenacin;Sabcomeline;MK-6884;Brompheniramine-d6 maleate;Navafenterol saccharinate;DREADD agonist 21;Cyclobuxine D;Brompheniramine maleate;Dexetimide;Anisodamine hydrobromide;Anisotropine bromide;PD 102807;Nebracetam hydrochloride;Muscarine-d9 iodide;Mazaticol;VU0455691;Arborine;Oxitropium Bromide;Propiverine hydrochloride;VU0152099;MHP 133;YM-58790;Elucaine;Rispenzepine;Phenglutarimid;Rapacuronium bromide;Ambutonium bromide;Temiverine hydrochloride;Procyclidine;M4 mAChR agonist-1;Camylofine

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