mAChR3/muscarinic acetylcholine receptor

The morphology and viability of human corneal stromal (HCS) cells were assessed using light microscopy and the MTT assay, respectively, in order to assess the cytotoxicity of pilocarpine. HCS cells exposed to pilocarpine at concentrations ranging from 0.625 to 20 g/L exhibited morphological abnormalities, including cell shrinkage, cytoplasmic vacuolization, detachment from the culture matrix, and eventual death, as well as dose- and time-dependent proliferation retardation. At concentrations lower than 0.625 g/L, however, no discernible difference was found between the pilocarpine exposure group and the control group. The MTT assay results demonstrated that HCS cell viability decreased with increasing time and concentration following treatment with pilocarpine at a concentration greater than 0.625 g/L (P<0.01 or 0.05), whereas cell viability of HCS cells treated with pilocarpine at a concentration lower than 0.625 decreased with increasing time and concentration (P<0.01 or 0.05). g/L did not change appreciably from the control [2]. In isolated segments of rat tail arteries constricted with norepinephrine (10 to 200 nM), the partial muscarinic agonist pilocarpine elicits concentration-dependent relaxation with an EC50 of 2.4 mM [3].

The effects of pilocarpine on salivation were investigated in exercised (EX) and control (CN) rats. Saliva volume caused by pilocarpine was considerably higher in EX rats compared to CN rats (P<0.01). Conversely, EX rats' saliva had a considerably lower Na+ content than CN rats' (P<0.05)[1].

After HCS cells were treated with pilocarpine at a concentration from 0.15625 g/L to 20.0 g/L, their morphology and viability were detected by light microscopy and MTT assay. The membrane permeability, DNA fragmentation and ultrastructure were examined by acridine orange (AO)/ethidium bromide (EB) double-staining. DNA electrophoresis and transmission electron microscopy (TEM), cell cycle, phosphatidylserine (PS) orientation and mitochondrial transmembrane potential (MTP) were assayed by flow cytometry (FCM). And the activation of caspases was checked by ELISA[3].

0.5 mg/kg; i.p. Rats: 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.

[1]. Matsuzaki K, et al. Daily voluntary exercise enhances pilocarpine-induced saliva secretion and aquaporin 1 expression in rat submandibular glands. FEBS Open Bio. 2017 Dec 7;8(1):85-93.
[2]. Tonta MA, et al. Pilocarpine-induced relaxation of rat tail artery by a non-cholinergic mechanism and in the absence of an intact endothelium. Br J Pharmacol. 1994 Jun;112(2):525-32.
[3]. Yuan XL, et al. Cytotoxicity of pilocarpine to human corneal stromal cells and its underlying cytotoxic mechanisms. Int J Ophthalmol. 2016 Apr 18;9(4):505-11.
[4]. Wang RF, et al. Post-treatment with the GLP-1 analogue liraglutide alleviate chronic inflammation and mitochondrial stress induced by Status epilepticus. Epilepsy Res. 2018 Mar 9;142:45-52.

(+)-pilocarpine is the (+)-enantiomer of pilocarpine. It has a role as an antiglaucoma drug. It is an enantiomer of a (-)-pilocarpine.
A naturally occurring alkaloid derived from the Pilocarpus plants, pilocarpine is a muscarinic acetylcholine agonist. Pilocarpine is associated with parasympathomimetic effects by selectively working on muscarinic receptors. Pilocarpine is used to treat dry mouth and various ophthalmic conditions, including elevated intraocular pressure and glaucoma. The usage of glaucoma by pilocarpine dates back to 1875.
Pilocarpine is a Cholinergic Receptor Agonist. The mechanism of action of pilocarpine is as a Cholinergic Agonist, and Cholinergic Muscarinic Agonist.
Pilocarpine is an orally available cholinergic agonist that is used to treat symptoms of dry mouth in patients with keratoconjunctivitis sicca (Sjögren syndrome) or with xerostomia (dry mouth) due to local irradiation. Pilocarpine has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent liver injury.

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Pilocarpine is a natural product found in Pilocarpus microphyllus, Pilocarpus racemosus, and other organisms with data available.
Pilocarpine is a natural alkaloid extracted from plants of the genus Pilocarpus with cholinergic agonist activity. As a cholinergic parasympathomimetic agent, pilocarpine predominantly binds to muscarinic receptors, thereby inducing exocrine gland secretion and stimulating smooth muscle in the bronchi, urinary tract, biliary tract, and intestinal tract. When applied topically to eyes, this agent stimulates the sphincter pupillae to contract, resulting in miosis; stimulates the ciliary muscle to contract, resulting in spasm of accommodation; and may cause a transitory rise in intraocular pressure followed by a more persistent fall due to opening of the trabecular meshwork and an increase in the outflow of aqueous humor.
Pilocarpine is only found in individuals that have used or taken this drug. It is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma. [PubChem]Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.

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Pilocarpine is a muscarinic agent that mediates diaphoretic, miotic, and central nervous system effects. Pilocarpine stimulates the secretion of various exocrine glands, such as sweat, lacrimal, salivary, and gastrointestinal glands. Following oral administration, pilocarpine increased the mean salivary flow rate by 2- to lO-folds than placebo. Its peak levels were maintained for at least one to two hours. Pilocarpine increases smooth muscle tone, contracts the pupillary and iris sphincter muscles, and induces miosis. Because pilocarpine may affect all five muscarinic receptor subtypes, it is associated with parasympathetic side effects.
The elimination half-life was 0.76 and 1.35 hours following administration of a 5mg or lOmg dose 3 times daily, respectively. Following ophthalmic administration in healthy subjects, the half-life was 3.96 hours.

C11H16N23O2

208.2569

208.12118

C, 63.44; H, 7.74; N, 13.45; O, 15.36

92-13-7

Pilocarpine Hydrochloride;54-71-7;Pilocarpine nitrate;148-72-1

5910

Typically exists as colorless to light yellow solid (<34°C), or liquid (>34°C)

1.2±0.1 g/cm3

431.8±18.0 °C at 760 mmHg

34℃

215.0±21.2 °C

0.0±1.0 mmHg at 25°C

1.585

-0.09

44.12

O=C1OC[C@H](CC2=CN=CN2C)[C@@H]1CC

QCHFTSOMWOSFHM-WPRPVWTQSA-N

InChI=1S/C11H16N2O2/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/t8-,10-/m0/s1

2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, (3S,4R)-

AI3-50523 AI3 50523 AI350523

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~480.17 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (12.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (12.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (12.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)