biperiden

Modify Date: 2024-01-02 15:47:57

biperiden Structure
biperiden structure
Common Name biperiden
CAS Number 514-65-8 Molecular Weight 311.461
Density 1.1±0.1 g/cm3 Boiling Point 462.1±40.0 °C at 760 mmHg
Molecular Formula C21H29NO Melting Point 114ºC
MSDS N/A Flash Point 224.5±26.0 °C

 Use of biperiden


Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.Target: M1 receptorsBiperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic)[1]. Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervate. It also has a prominent central blocking effect on M1 receptors [2].Biperiden (0.11 mg/kg), benactyzine (0.3 mg/kg),caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg) is to make a comparative assessment of potential cognitive effects. The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not [3].Clinical indications: parkinsonismFDA Approved Date: Toxicity: Drowsiness; vertigo; headache; dizziness

 Names

Name biperiden
Synonym More Synonyms

 biperiden Biological Activity

Description Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.Target: M1 receptorsBiperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic)[1]. Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervate. It also has a prominent central blocking effect on M1 receptors [2].Biperiden (0.11 mg/kg), benactyzine (0.3 mg/kg),caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg) is to make a comparative assessment of potential cognitive effects. The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not [3].Clinical indications: parkinsonismFDA Approved Date: Toxicity: Drowsiness; vertigo; headache; dizziness
Related Catalog
References

[1]. Pehl C, et al. Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Aliment Pharmacol Ther. 1998 Oct;12(10)

[2]. Kornhuber J, et al. Identification of novel functional inhibitors of acid sphingomyelinase. PLoS One. 2011;6(8)

[3]. Myhrer T, et al. Antiparkinson drugs used as prophylactics for nerve agents: studies of cognitive side effects in rats. Pharmacol Biochem Behav. 2008 Jun;89(4):633-8.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 462.1±40.0 °C at 760 mmHg
Melting Point 114ºC
Molecular Formula C21H29NO
Molecular Weight 311.461
Flash Point 224.5±26.0 °C
Exact Mass 311.224915
PSA 23.47000
LogP 4.01
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.583
Water Solubility 25.1 mg/L

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TN3675000
CHEMICAL NAME :
1-Piperidinepropanol, alpha-5-norbornen-2-yl-alpha-phenyl-
CAS REGISTRY NUMBER :
514-65-8
BEILSTEIN REFERENCE NO. :
0290038
LAST UPDATED :
199612
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C21-H29-N-O
MOLECULAR WEIGHT :
311.51
WISWESSER LINE NOTATION :
L55 A CUTJ FXQR&2- AT6NTJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
530 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982
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 :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
195 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 128,204,1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
56 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 128,204,1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
340 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,636,1982

 Safety Information

RIDADR NONH for all modes of transport
HS Code 2933399090

 Customs

HS Code 2933399090
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Biperidene [INN-French]
1-Piperidinepropanol, α-bicyclo[2.2.1]hept-5-en-2-yl-α-phenyl-
1-(5-bicyclo[2.2.1]hept-2-enyl)-1-phenyl-3-(1-piperidyl)propan-1-ol
EINECS 208-184-6
1-piperidinepropanol, a-bicyclo[2.2.1]hept-5-en-2-yl-a-phenyl-
Biperideno
1-norborn-5-en-2-yl-1-phenyl-3-piperidino-propan-1-ol
Biperidene
Biperidine
Beperiden
a-5-Norbornen-2-yl-a-phenyl-1-piperidinepropanol
biperiden
UNII:0FRP6G56LD
1-(Bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin-1-yl)propan-1-ol
1-norborn-5-en-2-yl-1-phenyl-3-piperidin-1-yl-propan-1-ol
3-Piperidino-1-phenyl-(D5-bicyclo[2.2.1]hepten-2-yl)-1-propanol
Akineton
1-Piperidinepropanol, α-[(1R,4R)-bicyclo[2.2.1]hept-5-en-2-yl]-α-phenyl-
1-(5-bicyclo[2.2.1]hept-2-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol
1-Bicycloheptenyl-1-phenyl-3-piperidinopropanol
1-Piperidinepropanol, α-bicyclo(2.2.1)hept-5-en-2-yl-α-phenyl-
Biperidenum
a-Bicyclo[2.2.1]hept-5-en-2-yl-a-phenyl-1-piperidinepropanol
Biperideno [INN-Spanish]
Biperidenum [INN-Latin]
1-[(1R,4R)-Bicyclo[2.2.1]hept-5-en-2-yl]-1-phenyl-3-(1-piperidinyl)-1-propanol
1-(Bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(1-piperidinyl)-1-propanol
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