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    Pilocarpine HCl
    Pilocarpine HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1206
    CAS #: 54-71-7 Purity ≥98%

    Description: Pilocarpine HCl (Pilocarpal; NSC-5746; Ocusert; Pilocar;Pilocar SMP; Salagen; NSC5746), the hydrochloride salt of pilocarpine, is a naturally occurring and nonselective muscarinic acetylcholine receptor agonist used to treat dry mouth caused by radiotherapy in patients with head and neck cancer and in patients with Sjogren's syndrome. It is also used to produce an experimental model of epilepsy. Pilocarpine is a parasympathomimetic alkaloid extracted from the leaves of tropical American shrubs from the genus Pilocarpus.  Pilocarpine acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis.

    References: Neurosci Lett. 1994 Feb 28;168(1-2):225-8; Eur J Pharmacol. 1999 Jan 1;364(1):7-11.

    Related CAS #: 54-71-7 (HCl)   92-13-7 (free base)   148-72-1 (nitrate) 

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    Molecular Weight (MW)244.72 
    FormulaC11H16N2O2.HCl 
    CAS No.54-71-7 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 49 mg/mL (200.2 mM) 
    Water: 49 mg/mL (200.2 mM) 
    Ethanol: N/A
    Other info

    Chemical Name: (3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one;hydrochloride

    InChi Key: RNAICSBVACLLGM-GNAZCLTHSA-N

    InChi Code: InChI=1S/C11H16N2O2.ClH/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2;/h5,7-8,10H,3-4,6H2,1-2H3;1H/t8-,10-;/m0./s1

    SMILES Code: CCC1C(COC1=O)CC2=CN=CN2C.Cl           

    SynonymsNSC 5746 HCl; Pilocarpine Hydrochloride; Pilocarpal; Pilocar; (+)-Pilocarpine hydrochloride; NSC-5746 HCl; NSC5746 HCl; Pilocar SMP; Salagen; Pilocarpine Mononitrate, (3S-cis)-Isomer; Pilocarpine Nitrate; Pilocarpine, Monohydrochloride, (3S-cis)-Isomer; Ocusert;


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    In Vitro

    In vitro activity: Pilocarpine is a parasympathomimetic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist in the parasympathetic nervous system, which acts therapeutically at themuscarinic acetylcholine receptor M3 due to its topical application, e.g., in glaucoma and xerostomia. Pilocarpine acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis. Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humorleaves the eye to decrease intraocular pressure. In ophthalmology, pilocarpine is also used to reduce the possibility of glare at night from lights when the patient has undergone implantation of phakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, relieving these symptoms. The most common concentration for this use is pilocarpine 1%, the weakest concentration. Pilocarpine is also used to treat dry mouth (xerostomia) which can occur, for example, as a side effect of radiation therapy for head and neck cancers. Pilocarpine stimulates the secretion of large amounts of saliva and sweat.


    Cell Assay: Cell viability is determined by MTT assay. Briefly, HCS cells are inoculated into a 96-well culture plate (Nunc) at a density of 1×104 cells/100 µL/well, and are cultured and treated. At a 4h interval, the Pilocarpine (0.625 to 20 g/L)-containing medium is replaced entirely with 100 µL serum-free DMEM/F12 medium containing 1.0 g/L MTT, and the cells are incubated at 37°C in the dark for 4h. After the MTT-containing medium is discarded with caution, 150 µL DMSO is added to dissolve the produced formazan crystals at 37°C in the dark for 15 min, and the absorbance at 490 nm is measured with a Multiskan GO microplate reader

    In VivoThe Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na+ concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05)
    Animal modelRats: Male, 10-week-old Wistar rats are assigned to one of two groups, exercise (EX, n=6) and control (CN, n=6). The EX rats are kept for 40 days in cages with a running wheel (SN-451), allowing them to undertake voluntary exercise, while the CN rats are kept in cages with the running wheel locked. On the 40th day, Pilocarpine-induced saliva is measured as follows. Briefly, the rats are anesthetized, preweighed cotton was placed in their mouths sublingually, and Pilocarpine (0.5 mg/kg) is intraperitoneally injected to induce saliva secretion. Each cotton ball is then changed every 10 min for 1 h. The collected cotton balls are weighed again, and the mass of saliva secreted is calculated by subtracting the initial from the final weight.
    Formulation & Dosage0.5 mg/kg; i.p.
    References

    Neurosci Lett. 1994 Feb 28;168(1-2):225-8; Eur J Pharmacol. 1999 Jan 1;364(1):7-11.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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