Biperiden-d5
目录号 : GC49069An internal standard for the quantification of biperiden
Cas No.:2938691-75-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Biperiden-d5 is intended for use as an internal standard for the quantification of biperiden by GC- or LC-MS. Biperiden is an antagonist of muscarinic acetylcholine receptors (mAChRs; IC50s = 0.48, 6.3, 3.9, 2.4, and 6.3 nM for M1-5 receptors, respectively).1 It increases spontaneous and electrically evoked dopamine release and electrically evoked acetylcholine (ACh) release from rabbit caudate nucleus slices preincubated with dopamine.2 Biperiden (10 µM) also inhibits NMDA-induced ACh release in rabbit caudate nucleus slices.3 Biperiden (0.01-1.0 mg/kg) reduces physostigmine-induced tremor in rats.4 Formulations containing biperiden have been used as an adjuvant treatment for Parkinson’s disease.
1.Bolden, C., Cusack, B., and Richelson, E.Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cellsJ. Pharmacol. Exp. Ther.260(2)576-580(1992) 2.Jackisch, R., Huang, H.Y., Reimann, W., et al.Effects of the antiparkinsonian drug budipine on neurotransmitter release in central nervous system tissue in vitroJ. Pharmacol. Exp. Ther.264(2)889-898(1993) 3.Jackisch, R., Kruchen, A., Sauermann, W., et al.The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonistsEur. J. Pharmacol.264(2)207-211(1994) 4.GothÓni, P., Lehtinen, M., and Fincke, M.Drugs for Parkinson’s disease reduce tremor induced by physostigmineNaunyn Schmiedebergs Arch. Pharmacol.323(3)205-210(1983)
Cas No. | 2938691-75-7 | SDF | |
Canonical SMILES | OC(CCN1CCCCC1)(C2CC3C=CC2C3)C4=C([2H])C([2H])=C([2H])C([2H])=C4[2H] | ||
分子式 | C21H24D5NO | 分子量 | 316.5 |
溶解度 | Acetonitrile: soluble,DMSO: soluble,Methanol: soluble | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.1596 mL | 15.7978 mL | 31.5956 mL |
5 mM | 0.6319 mL | 3.1596 mL | 6.3191 mL |
10 mM | 0.316 mL | 1.5798 mL | 3.1596 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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A novel method for the therapeutic drug monitoring of biperiden in plasma by GC-MS using salt-assisted liquid-liquid microextraction
Clin Chim Acta 2023 Mar 15;543:117322.PMID:37001688DOI:10.1016/j.cca.2023.117322
Biperiden is an anticholinergic agent with central effects. It is used in Parkinson's syndromes and in the treatment of extrapyramidal symptoms that occur with the use of various agents (neuroleptics, antipsychotics). It causes anticholinergic syndrome in high doses. For this reason, therapeutic drug monitoring of biperiden is important. This study, it was aimed to develop a validated GC-MS method for the therapeutic monitoring of biperiden in human plasma. Biperiden and internal standard Biperiden-d5 were extracted from plasma using the salt-assisted liquid-liquid extraction method. The method was validated according to the European Medicines Agency (EMA), Bioanalytical method validation guidelines. The lower limit of quantification of the developed method was chosen as 0.5 ng/mL. The calibration curve of biperiden for the method was validated between 0.5 and 15 ng/mL, showing correlation coefficients >0.99. In addition, the developed method was used for the therapeutic drug monitoring of biperiden in real patient plasma.