预约演示
更新于：2026-02-27
Lormetazepam
氯甲西泮
更新于：2026-02-27
概要
基本信息
药物类型 小分子化药 |
别名 (RS)-Lormetazepam、(±)-Lormetazepam、7-Chloro-1,3-dihydro-5-(o-chlorophenyl)-3-hydroxy-1-methyl-2H-1,4-benzodiazepin-2-one + [12] |
作用方式 激动剂 |
作用机制 GABAA receptor激动剂(γ-氨基丁酸 A 受体激动剂) |
在研适应症 |
非在研适应症 |
原研机构- |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (1990-06-29), |
最高研发阶段(中国)无进展 |
特殊审评- |
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结构/序列
分子式C16H12Cl2N2O2 |
InChIKeyFJIKWRGCXUCUIG-UHFFFAOYSA-N |
CAS号848-75-9 |
关联
6
项与 氯甲西泮 相关的临床试验CTR20232320
评价氯甲西泮注射液用于区域性麻醉手术患者术前镇静抗焦虑治疗的有效性和安全性的多中心、随机、双盲、安慰剂平行对照III期临床试验
CTR20223082
一项在中国健康志愿者中评估氯甲西泮注射液单次给药的药代动力学和药效
学、安全性的 I 期临床研究
EUCTR2015-000691-94-FR
Self-help program for hypnotics withdrawal in insomniac patients: A randomized controlled clinical trial.
100 项与 氯甲西泮 相关的临床结果
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100 项与 氯甲西泮 相关的转化医学
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100 项与 氯甲西泮 相关的专利（医药）
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739
项与 氯甲西泮 相关的文献（医药）2026-01-13ANALYTICAL CHEMISTRY
Toward AI-Assisted Greener Chiral HPLC: Predicting Efficient Enantioseparation–Mobile Phase (EES–MP) Profiles for MP Selection─A Lux Cellulose-1 Case Study
Article
作者: Sagrado, Salvador ; Martín-Biosca, Yolanda ; Medina-Hernández, María José ; Escuder-Gilabert, Laura ; Pardo-Cortina, Carlos
Chiral HPLC method development still relies heavily on trial-and-error screening. We introduce the Efficient Enantioseparation (EES) parameter─a single metric integrating resolution (Rs) and retention (k)─to move from point predictions to full mobile-phase (MP) profile modeling. Using EES as the response, we trained multiple artificial neural networks (ANNs) on 62 variables (molecular descriptors) and 76 objects (structurally diverse neutral and basic compounds chromatographed on a Lux Cellulose-1 column under aqueous-acetonitrile conditions at nine MP compositions). ANNs were optimized with a chaotic competitive-learning optimizer (CCLNNA), then ranked/selected and combined into a consensus model to enhance robustness and limit overfitting. The ANN-consensus model accurately reproduces full EES-MP profiles (R2 > 0.9) with lower error dispersion, enabling prospective feasibility checks and single-shot selection of high-EES mobile-phase compositions. External tests on fluoxetine and lormetazepam confirmed prospective utility by anticipating separability at one or more MPs (nominating the MP with maximal EES) or nonseparability across the explored MP range. To our knowledge, this work provides the first proof-of-concept for in silico prediction of full EES-MP profiles in chiral HPLC, enabling intelligent MP selection. Rather than a definitive model, this work evaluates the potential of the strategy: consensus stabilizes learning with limited data and offers greener, actionable guidance that can reduce experiments, reagent consumption, and development time. The framework is extensible to broader chemotypes and stationary and mobile phases; larger data sets could further generalize EES-profile prediction and support intelligent MP selection in sustainable chiral HPLC.
2025-12-01Purinergic Signalling
The CALHM1 blocker CGP37157 increases seizure severity during status epilepticus in adult mice
Article
作者: Engel, Tobias ; Brett, Francesca M ; Henshall, David ; O'Brien, Donncha F ; Mitra, Meghma ; Farrell, Michael A ; Beausang, Alan ; Cryan, Jane ; Cano-Abad, Maria F ; Delanty, Norman ; Rodriguez, Amaya Sanz
Abstract:
Epilepsy is one of the most common chronic brain diseases affecting up to 70 million people worldwide. Major challenges of epilepsy treatment include the high pharmacoresistance in patients and the lack of disease-modification. Extracellular adenosine 3’triphosphate (ATP), a key neurotransmitter in the activation of the purinergic signalling system, is increasingly recognized to contribute to pathological brain hyperexcitability in epilepsy. Consequently, targeting ATP-release mechanisms may constitute a new therapeutic strategy for seizure control and epilepsy. The calcium channel, Calcium Homeostasis Modulator 1 (CALHM1), a voltage-gated, non-selective ion channel that permits the passage of various cations and small molecules, is expressed in neurons and plays an essential role during neuronal excitability and neurotransmission. In addition to ions, CALHM1 also allows the passage of ATP into the extracellular space, activating thereby purinergic receptors. Here, we tested if the pharmacological blocking of CALHM1 via CGP37157 (7-chloro-5-(2-chlorophenyl)-3,5-dihydro-4,1-benzothiazepin-2-(1H)-one) alters the severity of intra-amygdala kainic acid-induced status epilepticus. Our results show that CGP37157 increased the severity of seizures during status epilepticus. In addition, CALHM1 protein levels are down-regulated in the hippocampus in epileptic mice and Temporal Lobe Epilepsy (TLE) patients. In summary, our results identify CALHM1 as a new contributor to seizures and suggest targeting of CALHM1 as new treatment strategy for epilepsy.
2025-10-01Drug Testing and Analysis
Monitoring Community Use of Benzodiazepines Through Wastewater‐Based Epidemiology
Article
作者: Rudminienė, Olesia ; Van Wichelen, Natan ; Georgescu, Milica ; Boogaerts, Tim ; Delputte, Peter ; Iliescu, Ruxanda ; van Nuijs, Alexander L. N. ; Vanaga‐Arāja, Diāna ; Quireyns, Maarten ; De Roeck, Naomi ; Schaerlaekens, Sofie ; Covaci, Adrian
ABSTRACT:
Benzodiazepines and related z‐drugs (BZDs) are widely used pharmaceuticals but require careful monitoring due to limited efficacy, tolerance development and the risk of dependence. Wastewater‐based epidemiology (WBE) is a valuable approach to gather population‐wide information on consumption patterns through analysis of influent wastewater. This study examines how overlapping metabolic pathways within the BZD drug class can lead to misinterpretation if not carefully considered. An analytical method is developed and validated for 26 biomarkers of prescription BZDs in influent wastewater using solid‐phase extraction and liquid chromatography–tandem mass spectrometry and applied to influent wastewater samples for the first time in Belgium (13 locations), Latvia (1), Lithuania (3) and Romania (1). The countries were chosen for their differing prescription BZD market registration, allowing testing of different hypotheses. To aid in complex data interpretation, this study presents a structured categorisation of BZDs into
direct
biomarkers, which directly reflect consumption, and
downstream
biomarkers, which are influenced by multiple BZDs, and further discusses the implication this has on the interpretation. Spatial differences were noted among
direct
biomarkers such as higher consumption of zolpidem in Belgium and zopiclone in Riga (LVA). Downstream biomarkers had higher population‐normalised mass loads but cannot be interpreted in isolation, for example, lorazepam (ranging 4–25 mg/day/1000 inhabitants over all locations), lormetazepam (8–30), oxazepam (10–50) and temazepam (1–12). These findings highlight challenges in interpreting BZD consumption trends and emphasise the need of distinguishing different biomarker classes to ensure accurate and comparable results across studies needed to guide informed decision‐making.
1
项与 氯甲西泮 相关的新闻（医药）2024-07-22
·信狐药迅
细胞疗法免疫疗法申请上市临床申请ASH会议
100 项与 氯甲西泮 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 入睡和睡眠障碍 | 日本 | 1990-06-29 | |
| 入睡和睡眠障碍 | 日本 | 1990-06-29 | |
| 入睡和睡眠障碍 | 日本 | 1990-06-29 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 麻醉 | 临床1期 | 中国 | 2022-11-17 |
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