Pilocarpine Hydrochloride - CAS 54-71-7
Catalog number: 54-71-7
Category: Inhibitor
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Pilocarpine HCl is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.
NSC 5746 HCl; NSC5746 HCl; NSC-5746 HCl
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1.Spatiotemporal profile of Map2 and microglial changes in the hippocampal CA1 region following pilocarpine-induced status epilepticus.
Schartz ND1, Herr SA1, Madsen L1, Butts SJ1, Torres C2, Mendez LB2, Brewster AL1,3. Sci Rep. 2016 May 4;6:24988. doi: 10.1038/srep24988.
Status epilepticus (SE) triggers pathological changes to hippocampal dendrites that may promote epileptogenesis. The microtubule associated protein 2 (Map2) helps stabilize microtubules of the dendritic cytoskeleton. Recently, we reported a substantial decline in Map2 that coincided with robust microglia accumulation in the CA1 hippocampal region after an episode of SE. A spatial correlation between Map2 loss and reactive microglia was also reported in human cortex from refractory epilepsy. New evidence supports that microglia modulate dendritic structures. Thus, to identify a potential association between SE-induced Map2 and microglial changes, a spatiotemporal profile of these events is necessary. We used immunohistochemistry to determine the distribution of Map2 and the microglia marker IBA1 in the hippocampus after pilocarpine-induced SE from 4 hrs to 35 days. We found a decline in Map2 immunoreactivity in the CA1 area that reached minimal levels at 14 days post-SE and partially increased thereafter.
2.Gallic acid grafting effect on delivery performance and antiglaucoma efficacy of antioxidant-functionalized intracameral pilocarpine carriers.
Chou SF1, Luo LJ2, Lai JY3. Acta Biomater. 2016 Apr 26. pii: S1742-7061(16)30197-0. doi: 10.1016/j.actbio.2016.04.035. [Epub ahead of print]
Functionalization of therapeutic carrier biomaterials can potentially provide additional benefits in drug delivery for disease treatment. Given that this modification determines final therapeutic efficacy of drug carriers, here, we investigate systematically the role of grafting amount of antioxidant gallic acid (GA) onto GN in situ gelling copolymers made of biodegradable gelatin and thermo-responsive poly(N-isopropylacrylamide) for intracameral delivery of pilocarpine in antiglaucoma treatment. As expected,increasingredox reaction time increased totalantioxidantactivitiesand free radical scavenging abilities ofsynthesizedcarrierbiomaterials. The hydrophilic nature of antioxidant molecules strongly affected physicochemical properties of carrier materials with varying GA grafting amounts, thereby dictating in vitro release behaviors and mechanisms of pilocarpine. In vitro oxidative stress challenges revealed that biocompatible carriers with high GA content alleviated lens epithelial cell damage and reduced reactive oxygen species.
3.Synthesis of N-1', N-3'-disubstituted spirohydantoins and their anticonvulsant activities in pilocarpine model of temporal lobe epilepsy.
Yang C1, Schanne FA1, Yoganathan S2, Stephani RA3. Bioorg Med Chem Lett. 2016 Apr 18. pii: S0960-894X(16)30413-9. doi: 10.1016/j.bmcl.2016.04.040. [Epub ahead of print]
Herein we report the synthesis and anticonvulsant activity of a library of eighteen new compounds that are structural mimics of phenytoin. These class of compounds contain a N-1', N-3'-disubstituted spirohydantoin scaffold, where the N-1' and N-3' positions are modified with an alkyl group or aryl group. Of the eighteen compounds synthesized and tested, compound 5c showed the best anticonvulsant activity. It completely prevented the precursor events of motor seizure in the pilocarpine model of temporal lobe epilepsy. Additionally, ten of the analogs were more effective than phenytoin when compared using the Racine's score in the pilocarpine model. Based on the structure activity relationship (SAR), we concluded that alkyl groups (ethyl, propyl or cyclopropyl) at N-3' position and 4-nitro phenyl group at N-1' position are desirable.
4.Dual mechanisms of rapid expression of anxiety-related behavior in pilocarpine-treated epileptic mice.
Otsuka S1, Ohkido T2, Itakura M3, Watanabe S4, Yamamori S5, Iida Y6, Saito M7, Miyaoka H8, Takahashi M9. Epilepsy Res. 2016 Apr 25;123:55-67. doi: 10.1016/j.eplepsyres.2016.04.007. [Epub ahead of print]
A mouse model of epilepsy was generated by inducing status epilepticus (SE) for either 1.5 or 4.5h with pilocarpine to study anxiety-related behaviors, changes in the electroencephalogram of the cerebral cortex and hippocampus, and expression of hippocampal proteins. The viability and rate of success of SE induction were high in C57BL/6N mice but not in C57BL/6J mice. C57BL/6N mice were immotile during the first 2days after SE; however, by the third day, most mice were recovered and exhibited strong anxiety-related behaviors in response to the light/dark preference test and open field test. There was a striking difference in the temporal appearance of anxiety-related behavior between the two SE durations: 1.5h SE mice exhibited strong anxiety-related behavior 3days after SE that gradually attenuated over the next few weeks, whereas 4.5h SE mice exhibited strong anxiety-related behavior 3days after SE that persisted even at nearly 1year after SE.
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CAS 54-71-7 Pilocarpine Hydrochloride

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