Proparacaine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

不可逆的局部麻醉剂；抑制疼痛感，据信可作为电压门控钠通道的拮抗剂。

An irreversible local anesthetic; inhibits pain sensations that is believed to act as an antagonist on voltage-gated sodium channels.Pain Approved(In Vitro):Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro.Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells .Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells.Proparacaine Hydrochloride induces caspase-2, -3 and -9 activation, and mitochondrial transmembrane potential disruption.Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor.(In Vivo):Proparacaine Hydrochloride (75 μg/30 μL; intranasal administration; for 7 days) significantly decreases nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa.

Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro.Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells .Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells.Proparacaine Hydrochloride induces caspase-2, -3 and -9 activation, and mitochondrial transmembrane potential disruption.Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor. Cell Viability Assay Cell Line:HCS cells Concentration:294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation Time:4 hours, 8 hours, and 12 hours, 16 hours, 20 hours, 24 hours, 28 hours Result:Decreased the viability of HCS cells with concentration and time at concentrations above 588.93 μM.Apoptosis Analysis Cell Line:HCS cells Concentration:294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation Time:4 hours, 8 hours, and 12 hours Result:Induced apoptosis of HCS cells.Cell Cycle Analysis Cell Line:HCS cells Concentration:4.71 mM Incubation Time:4 hours, 8 hours, and 12 hours Result:Arrested HCS cells at the G1 phase of the cell cycle.Western Blot Analysis Cell Line:HCS cells Concentration:4.71 mM Incubation Time:4 hours, 8 hours, and 12 hours Result:Down-regulated the expression level of anti-apoptotic protein Bcl-xL and up-regulated the pro-apoptotic protein Bax, whereas significantly up-regulated the cytoplasmic amounts of mitochondria-released cytochrome C and apoptosis-inducing factor (AIF).

Proparacaine Hydrochloride (75 μg/30 μL; intranasal administration; for 7 days) significantly decreases nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa. Animal Model:7-week-old female BALB/c mice, allergic rhinitis model Dosage:75 μg/30 μL Administration:Intranasal administration, for 7 days Result:Significantly reduced nasal rubbing and sneezing.

Proxymetacaine hydrochloride

Membrane Transporter/Ion Channel

Sodium Channel

Voltage-gatedsodiumchannel

Neurological Disease

Pain

5875-06-9

330.8502

C16H27ClN2O3

>98% (HPLC)

10 mM in DMSO

CCCOC1=C(C=C(C=C1)C(=O)OCCN(CC)CC)N.Cl

Benzoic acid, 3-amino-4-propoxy-, 2-(diethylamino)ethyl ester, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years