biperiden lactate

Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders[1][2].

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

Biperiden lactate (29.6 μg/ml, 72 hours) can significantly induce apoptosis and inhibit proliferation at high doses in human pancreatic ductal adenocarcinoma cells[1]. Cell Proliferation Assay[1] Cell Line: Panc-1, Panc-2 and BxPC3 human pancreatic ductal adenocarcinoma cells Concentration: 29.6 μg/mL Incubation Time: 72 hours Result: Inhibited cell proliferation at 72 hours significantly by reducing nuclear c-Rel translocation.

Biperiden lactate (intraperitoneal injection, 10 mg/kg, everyday, 3 weeks) reduces tumor size by 83% in subcutaneous xenograft mouse using Panc-1 human pancreatic ductal adenocarcinoma cells[1]. Biperiden lactate (intraperitoneal injection, 8 mg/kg, every 8 hours, 10 days) can reduce frequency of spontaneous seizures and extracellular hippocampal glutamate levels while cause a long-term decrease in hippocampal excitability[2]. Animal Model: Subcutaneous xenograft mouse using Panc-1 human pancreatic ductal adenocarcinoma cells[1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; everyday; 3 weeks Result: Tumor size reduced by 83%. Animal Model: Male Wistar rats (200-250 g)[2] Dosage: 8 mg/kg Administration: Intraperitoneal injection; every 8 hours; 10 days Result: Reduced late seizures by about three times with no affecting emotional memory damage

[1]. Leonie Konczalla，et al. Biperiden and mepazine effectively inhibit MALT1 activity and tumor growth in pancreatic cancer. Int J Cancer. 2020 Mar 15;146(6):1618-1630.

[2]. Simone Bittencourt, et al. Modification of the natural progression of epileptogenesis by means of biperiden in the pilocarpine model of epilepsy. Epilepsy Res. 2017 Dec;138:88-97. doi: 10.1016/j.eplepsyres.2017.10.019. Epub 2017 Oct 29.

MOLECULAR WEIGHT :

401.60

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

161 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

335 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

61 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 1,74,1967