盐酸比哌立登(Biperiden Hydrochloride) - 药物靶点：mAChRs_在研适应症：药物性运动障碍，帕金森障碍_专利_临床

概要

基本信息

药物类型

小分子化药

别名

1-Bicyclo[2.2.1]hept-5-en-2-yl-1-phenyl-3-piperidin-1-yl-propan-1-ol、Biperiden、Biperiden hydrochloride (JP17/USP)

+ [7]

靶点

mAChRs

作用方式

拮抗剂

作用机制

mAChRs拮抗剂(毒蕈碱型乙酰胆碱受体家族拮抗剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Sumitomo Pharma Co., Ltd.

非在研机构

AbbVie, Inc.

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (1959-09-08),

帕金森病

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C21H30ClNO

InChIKeyRDNLAULGBSQZMP-UHFFFAOYSA-N

CAS号1235-82-1

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关联

15

项与盐酸比哌立登相关的临床试验

RBR-7qtvbh3

/ Completed临床2期IIT

Study of the acute effects of Biperiden on nicotine cravings: double-blind, placebo-controlled study

开始日期2023-10-20

申办/合作机构

Escola Paulista De Medicina

[+1]

RBR-2v4qz72

/ Not yet recruiting临床2/3期

Effects of biperiden in the treatment of alcohol use disorder: a randomized, double-blind, placebo-controlled trial

开始日期2023-09-28

申办/合作机构-

NCT04945213

/ Recruiting临床3期IIT

Biperiden for Prevention of Epilepsy in Patients With Traumatic Brain Injury

One of the most important neurological consequences following Traumatic Brain Injury (TBI) is the development of post traumatic epilepsy (PTE). Nevertheless, there is still no effective therapeutic intervention to reduce the occurrence of PTE. In previous studies with animals models of epilepsy, the biperiden decreased the incidence and intensity of spontaneous epileptic seizures besides delaying their appearance. The aim of this study is the evaluation of biperiden as antiepileptogenic drug to prevent PTE and also the determination of side effects, evaluating its cost-effectiveness in patients with moderate and severe TBI.

开始日期2023-01-10

申办/合作机构

Sociedade Beneficiente de Senhoras Hospital Sírio Libanês

[+6]

100 项与盐酸比哌立登相关的临床结果

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100 项与盐酸比哌立登相关的转化医学

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100 项与盐酸比哌立登相关的专利（医药）

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1,100

项与盐酸比哌立登相关的文献（医药）

2025-05-01·Neuroscience Letters

Evaluation of the effect of biperiden (cholinergic muscarinic receptor antagonist) on ethanol self-administration in rats

Article

作者: Matos Mendes Ferreira Badaro, Sara Emi ; Lira, Clarice Ribeiro ; Leão, Rodrigo Molini ; Palombo, Paola ; Fernandes Galduróz, José Carlos ; Teodoro, Lucas ; Cruz, Fábio Cardoso

Evidence from the literature suggests that alcohol use disorder (AUD) is closely associated with alterations in neuronal plasticity and the memory system, related to modifications in muscarinic receptors. The present study aimed to investigate the effects of systemic injection of biperiden, a muscarinic cholinergic antagonist, in experimental protocols of progressive ratio, 24-hour binge alcohol consumption, and reinstatement of context-induced ethanol self-administration. The results demonstrated that biperiden at doses of 5 and 10 mg/kg (i.p.) effectively reduced the animals' motivation for alcohol consumption, as evidenced by decreased responses on the active lever and a reduction in the last ratio achieved in the progressive ratio protocol. Furthermore, these same doses significantly reduced ethanol consumption in the 24-hour binge protocol. Treatment with biperiden at doses of 1, 5, and 10 mg/kg also attenuated alcohol-seeking behavior after re-exposure to the context associated with ethanol self-administration. These findings suggest that biperiden may have therapeutic potential in the treatment of alcohol use disorder, indicating that modulation of the cholinergic system could be a promising avenue for further investigation.

2025-03-24·Journal of Chemical Information and Modeling

Multidependency Graph Convolutional Networks and Contrastive Learning for Drug Repositioning

Article

作者: Xu, Guangwei ; Li, Shengnan ; Zou, Guobing ; Gan, Yanglan ; Yan, Cairong

The goal of drug repositioning is to expedite the drug development process by finding novel therapeutic applications for approved drugs. Using multifeature learning, different computational drug repositioning techniques have recently been introduced to predict possible drug-disease relationships. Nevertheless, current graph-based methods tend to model drug-disease interaction relationships without considering the semantic influence of node-specific side information on graphs. These approaches also suffer from the noise and sparsity inherent in the data. To address these limitations, we propose MDGCN, a novel drug repositioning method that incorporates multidependency graph convolutional networks and contrastive learning. Based on drug and disease similarity matrices and the drug-disease relationships matrix, this approach constructs multidependency graphs. It subsequently employs graph convolutional networks to spread side information between various graphs in each layer. Meanwhile, the weak supervision of drug-disease connections is effectively addressed by introducing cross-view and cross-layer contrastive learning to align node embedding across various views. Extensive experiments show that MDGCN performs better in drug-disease association prediction than seven advanced methods, offering strong support for investigating novel therapeutic indications for medications of interest.

2025-03-10·Cureus

Uncommon Extrapyramidal Reaction to Ondansetron

Article

作者: Dias, Carolina S ; Gaspar, João ; Moreira, Catarina ; Santos, Maria

We describe the case of a 77-year-old man, who was admitted for the initiation of chemotherapy for stage IV small cell lung cancer without cerebral metastases. On the first day post-admission, the patient developed altered mental status and right-sided weakness after premedication with ondansetron and dexamethasone. Symptoms resolved spontaneously within 90 minutes. An ischemic event was suspected despite unremarkable brain imaging. Prophylactic anticoagulation and statins were initiated. Five days later, a second episode of altered mental status, anisocoria, facial paresis, and severe dysarthria occurred following ondansetron administration. Bloodwork revealed significant hyponatremia (116 mEq/L), suggesting Syndrome of Inappropriate Antidiuretic Hormone Secretion (SIADH), despite this suspicion, there was no further investigation to confirm this diagnosis due to rapid symptom reversal after biperiden administration, implicating an adverse reaction to ondansetron. Ondansetron and metoclopramide were discontinued, hyponatremia was corrected, and no further episodes occurred during the hospital stay. This case highlights the necessity of awareness for adverse reactions of ondansetron that can mimic cerebrovascular events and the need for a thorough revision of medication in complex cases.

1

项与盐酸比哌立登相关的新闻（医药）

2025-02-07

·EndPoints

Belgian regulator recommends blocking Indian drugmaker's API production

Indian drugmaker Maithili Life Sciences has received a non-compliant report from the Brussels-based Federal Agency for Medicines and Health Products for 24 issues related to Maithili’s active pharmaceutical ingredient manufacturing. An inspection of the manufacturer’s factory in Andhra Pradesh, India, ending in November 2024 revealed the problems, according to a report published by the European Medicines Agency and the Belgian regulator. Due to the discrepancies, the FAMHP recommended that Maithili be removed as a manufacturer of active substances and intermediates. The agency also recommended blocking Maithili from supplying products made at the Andhra Pradesh facility, as long as there are alternate suppliers and it wouldn’t cause drug shortages. In particular, the report states the company should be suspended from making its biperiden hydrochloride product, which is a muscarinic receptor antagonist used to treat the muscle spasms and stiffness caused by Parkinson’s disease. The regulator also recommended an assessment of Maithili’s products to decide if the drugmaker should recall batches of its APIs. In addition, all imported products from the Andhra Pradesh factory should be retested, the report states. The 24 deficiencies outlined in the report include issues regarding the cleanliness and maintenance of manufacturing equipment, which could lead to contamination and cross-contamination of APIs. In addition to manufacturing commercial APIs and other raw materials, Maithili Life Sciences also offers research and development capabilities for intermediates and other chemicals, according to its website. It ships its products globally and domestically.

100 项与盐酸比哌立登相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02246	盐酸比哌立登	N04AA02	DB00810

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
药物性运动障碍	日本	Sumitomo Pharma Co., Ltd.	1964-02-28
帕金森障碍	日本	Sumitomo Pharma Co., Ltd.	1964-02-28

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01251393 (CTgov)	临床3期	可卡因相关疾病	111	Biperiden (Biperiden)	憲廠膚窪壓衊廠夢觸憲(範範獵窪艱獵廠糧鏇鑰) = 構淵鏇蓋製觸窪製齋夢顧壓積蓋鹽繭鏇獵淵齋 (齋糧餘鏇顧醖壓艱壓夢, 廠遞鹽鏇鹹廠觸糧鹹網 ~ 網網選艱鹹顧鹽獵衊憲) 更多	-	2020-02-28
				Placebo (Placebo)	憲廠膚窪壓衊廠夢觸憲(範範獵窪艱獵廠糧鏇鑰) = 觸範鏇衊齋淵顧糧鹹齋顧壓積蓋鹽繭鏇獵淵齋 (齋糧餘鏇顧醖壓艱壓夢, 積網糧遞鬱顧窪簾遞齋 ~ 憲蓋衊顧築鏇構構蓋觸) 更多