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Pilocarpine (nitrate)


CAS No. : 148-72-1

148-72-1
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Cat. No. : HY-B1006
M.Wt: 271.27
Formula: C11H17N3O5
Purity: >98 %
Solubility: DMSO : 250 mg/mL (ultrasonic);H2O : 100 mg/mL (ultrasonic)
Introduction of 148-72-1 :

Pilocarpine nitrate is an orally active, selective M3 muscarinic acetylcholine receptor agonist. Pilocarpine nitrate can induce seizures and is used in research on conditions such as epilepsy, dry mouth (xerostomia), and elevated intraocular pressure[1][2][3][4]. IC50 & Target:M3 muscarinic receptor[1] In Vitro:To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls[2]. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM)[3]. In Vivo:

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Pilocarpine nitrate is a cholinergic muscarinic (M) receptor agonist. When used to induce epilepsy, it primarily acts via the central cholinergic system to increase neuronal excitability; this subsequently recruits systems such as the glutamatergic/NMDA pathways, ultimately resulting in status epilepticus (SE)[4].

Induction of epilepsy[4]
Background
Pilocarpine nitrate induces widespread neuronal excitation and abnormal discharges within limbic system networks by activating central muscarinic cholinergic receptors, progressively leading to recurrent convulsions and status epilepticus (SE). Neuronal damage caused by acute SE and the subsequent remodeling of neural networks are considered key substrates for the later development of epilepsy. Following SE, animals enter a latent period before exhibiting spontaneous recurrent seizures (SRS), thereby establishing a chronic temporal lobe epilepsy phenotype[4].
Specific Modeling Methods
Mice: Male NMRI mice, 28-32 g (5-6 weeks old)
Administration method: Pilocarpine (250-400 mg/kg) nitrate •Intraperitoneal injection, single dose; methscopolamine bromide (HY-B0344) is administered prior to Pilocarpine nitrate.
Note
(1) Continuous observation of behavioral changes in the animals following drug administration.
(2) The control group must receive the same solvent used for the drug solution to eliminate any effects of the solvent itself.
Modeling Indicators
Histological analysis: Significant remodeling of hippocampal tissue structure, accompanied by neuronal loss and astrogliosis.
EEG assessment: Persistent abnormal electrical activity and seizure-related EEG discharges during status epilepticus (SE).

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