Biperiden Lactate

HCID 197083

기본 정보

CAS
7085-45-2
표준 SMILES
CC(O)C(=O)O.OC(CCN1CCCCC1)(c1ccccc1)C1CC2C=CC1C2
InChIKey
GLPUBCPQWZZFNJ-UHFFFAOYSA-N
분자식
C24H35NO4
평균 분자량
401.5 g/mol
단동위원소 질량
401.2566086

개요

A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine. [PubChem]

이름 및 식별자

우선 이름
Biperiden Lactate
IUPAC
1-(2-bicyclo[2.2.1]hept-5-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol;2-hydroxypropanoic acid
영어명
BIPERIDEN LACTATE
분자식
C24H35NO4
분자량
401.55

이름 및 동의어

Biperiden lactate7085-45-209TD6C5147DTXSID40991120biperidene lactateRefChem:57528DTXCID601418206Akinetonalpha-5-Norbornen-2-yl-alpha-phenyl-1-piperidinepropanol lactate (salt)Tasmolin (TN)Akineton Lactate1-(2-bicyclo[2.2.1]hept-5-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol;2-hydroxypropanoic acid
이름 더 보기
akinetonlactateBIPERIDEN LACTATE USP/EP/BPalpha-5-norbornen-2-yl-alpha-phenyl-1-piperidinepropanolcompd.withlacticalacticacid,compd.withalpha-5-norbornen-2-yl-alpha-phenyl-1-piperidinepropanlactic acid, compound with alpha-bicyclo[2.2.1]hept-5-en-2-yl-alpha-phenylpiperidin-1-propanol (1:1)Propanoic acid, 2-hydroxy-, compd. with α-bicyclo[2.2.1]hept-5-en-2-yl-α-phenyl-1-piperidinepropanol (1:1)
EINECS 230-388-9BiperidenlactatUNII-09TD6C5147Biperiden lactate [USP:BAN:JAN]SCHEMBL41834Biperiden lactate (JAN/USP)orb1698140BIPERIDEN LACTATE [JAN]

데이터베이스 식별자

CAS
7085-45-2
PubChem CID
197083
DTXSID
DTXSID40991120
ChEMBL
CHEMBL1201067
UNII
09TD6C5147
EC Number
230-388-9

물성

구조 계산 물성

극성 표면적
81 Ų
수소 결합 공여자 수
3
수소 결합 수용자 수
5
회전 가능 결합 수
6
무거운 원자 수
29

실험 및 물리화학적 성질

Human Drugs · 3건

Breast Feeding; Lactation; Milk, Human; Antiparkinson Agents; Parasympatholytics; Muscarinic Antagonists

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

물리화학적 성질

녹는점
97 · 97-101°C
저장 조건
-20 °C · -20°C Freezer
용해도
클로로포름(약간 용해됨), DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태
고체
색상
하얀색

안전 및 규제

독성 정보

Treatment · 1건

Treatment of acute overdose revolves around symptomatic and supportive therapy. If Biperiden was administered orally, gastric lavage or other measures to limit absorption should be instituted. A small dose of diazepam or a short acting barbiturate may be administered if CNS excitation is observed. Phenothiazines are contraindicated because the toxicity may be intensified due to their antimuscarinic action, causing coma. Respiratory support, artificial respiration or vasopressor agents may be necessary. Hyperpyrexia must be reversed, fluid volume replaced and acid-base balance maintained. Urinary catheterization may be necessary. Routine use of physostigmine for overdose is controversial. Delirium, hallucinations, coma, and supraventricular tachycardia (not ventricular tachycardias or conduction defects) seem to respond. If indicated, 1 mg (half this amount for the children or elderly) may be given intramuscularly or by slow intravenous infusion. If there is no response within 20 minutes, and additional 1 mg dose may be given; this may be repeated until a total of 4 mg has been administered, a reversal of the toxic effects occur or excessive cholinergic signs are seen. Frequent monitoring of clinical signs should be done. Since physostigmine is rapidly destroyed, additional injections may be required every one or two hours to maintain control. The relapse intervals tend to lengthen as the toxic anticholinergic agent is metabolized, so the patient should be carefully observed for 8 to 12 hours following the last relapse. (L1712)

Exposure RoutesOral
Toxicity Summary · 1건

Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.

Signs and Symptoms · 1건

Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Effects During Pregnancy and Lactation◉ Summary of Use during Lactation

화학 및 산업

약리 정보

Metabolism/MetabolitesThe metabolism of biperiden is not completely understood, but does involve hydroxylation.
MeSH Pharmacological Classification · 3건

Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.

Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

용도 및 제조

UsesFor use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.

응용 분야

용도Anticholinergic; antiparkinsonian.

공급사11 곳

Dayang Chem (Hangzhou) Co.,Ltd.+86-0571-88938639 17705817739 · [email protected]
Chongqing jooe co., ltd+86-15223382610 · [email protected]
西安美川生物科技有限公司029-89275612 +8618991951683 · [email protected]
艾吉析科技(上海)有限公司17721401538;17717235263 17721401538 · [email protected]
sgtlifesciences pvt ltd+91-8790379245 · [email protected]

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