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更新于：2025-03-30
Ergoloid Mesylates
甲磺酸二氢麦角碱
更新于：2025-03-30
概要
基本信息
药物类型 小分子化药 |
别名 co-dergocrine mesilate、Co-dergocrine Mesylate、co-dergocrine methanesulfonate + [29] |
作用方式 拮抗剂 |
作用机制 α-adrenergic receptor拮抗剂(α-肾上腺素能受体家族拮抗剂) |
非在研适应症- |
最高研发阶段批准上市 |
首次获批日期 美国 (1953-11-05), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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关联
2
项与 甲磺酸二氢麦角碱 相关的临床试验NCT05030129
An Exploratory Single Blind Study of Ergoloid Mesylates, 5-Hydroxytryptophan, and the Combination in Adult Males With Fragile X Syndrome
ChiCTR-IPR-17011155
Dihydroergotoxine mesylate for the treatment of sialorrhea in Parkinson's disease
100 项与 甲磺酸二氢麦角碱 相关的临床结果
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100 项与 甲磺酸二氢麦角碱 相关的转化医学
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100 项与 甲磺酸二氢麦角碱 相关的专利（医药）
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746
项与 甲磺酸二氢麦角碱 相关的文献（医药）2024-05-01Neuropharmacology
DHEC mesylate attenuates pathologies and aberrant bisecting N-glycosylation in Alzheimer's disease models
Article
作者: Xue, Yue ; Wang, Yue ; Cao, Yiming ; Gao, Xiangdong ; Chen, Song ; Huang, Hongfei
Tremendous progress has been made to develop the therapy of Alzheimer's disease (AD). Existing several anti-AD remedies, with certain limitations, are far from adequate. Evidence suggests that dihydroergocristine (DHEC) mesylate, one of the main components of Ergoloid mesylates, can reduce the production of amyloid-β in vitro. However, the therapeutic effect of DHEC mesylate in AD and its underlying mechanism are still largely unknown. Herein, we characterized the pharmacological effect of DHEC mesylate in AD and found that the spatial memory disorders and Alzheimer-type pathologies were alleviated by DHEC mesylate administration. Moreover, we demonstrated that DHEC mesylate improved aberrant bisecting N-glycosylation, which was identified as a potential biomarker of AD. We further explored the underlying mechanism and confirmed that DHEC mesylate protected against AD via AMPK and ERK signaling, in which, AMPK was the dominant down-stream molecule of DHEC mesylate. In summary, our findings provide foundations for development of DHEC mesylate as a therapeutic approach for AD.
2024-04-01Molecular diversity
Evaluation of the interaction between potent small molecules against the Nipah virus Glycoprotein in Malaysia and Bangladesh strains, accompanied by the human Ephrin-B2 and Ephrin-B3 receptors; a simulation approach
Article
作者: Alijanianzadeh, Mahdi ; Ebrahimi, Maryam
Malaysia reported the first human case of Nipah virus (NiV) in late September 1998 with encephalitis and respiratory symptoms. As a result of viral genomic mutations, two main strains (NiV-Malaysia and NiV-Bangladesh) have spread around the world. There are no licensed molecular therapeutics available for this biosafety level 4 pathogen. NiV attachment glycoprotein plays a critical role in viral transmission through its human receptors (Ephrin-B2 and Ephrin-B3), so identifying small molecules that can be repurposed to inhibit them is crucial to developing anti-NiV drugs. Consequently, in this study annealing simulations, pharmacophore modeling, molecular docking, and molecular dynamics were used to evaluate seven potential drugs (Pemirolast, Nitrofurantoin, Isoniazid Pyruvate, Eriodictyol, Cepharanthine, Ergoloid, and Hypericin) against NiV-G, Ephrin-B2, and Ephrin-B3 receptors. Based on the annealing analysis, Pemirolast for efnb2 protein and Isoniazid Pyruvate for efnb3 receptor were repurposed as the most promising small molecule candidates. Furthermore, Hypericin and Cepharanthine, with notable interaction values, are the top Glycoprotein inhibitors in Malaysia and Bangladesh strains, respectively. In addition, docking calculations revealed that their binding affinity scores are related to efnb2-pem (- 7.1 kcal/mol), efnb3-iso (- 5.8 kcal/mol), gm-hyp (- 9.6 kcal/mol), gb-ceph (- 9.2 kcal/mol). Finally, our computational research minimizes the time-consuming aspects and provides options for dealing with any new variants of Nipah virus that might emerge in the future.
2022-08-13Journal of biomolecular structure & dynamics
Exploring potential inhibitor of SARS-CoV2 replicase from FDA approved drugs using insilico drug discovery methods
Article
作者: Ahmed, Mohammad Z. ; Qamar, Imteyaz ; Singh, Nagendra ; Alqahtani, Ali S. ; Chandra, Anshuman ; Gurjar, Vaishali
Severe Acute Respiratory Syndrome Corona Virus-2 (SARS-CoV2) is responsible for fetal pneumonia called COVID19. SARS-CoV2 emerged in Wuhan, Hubei Province of China in December 2019. The COVID19 pandemic has now gripped the entire world with more than 70 million cases and over 1.5 million deaths so far. There no treatment option for COVID19 is in term of a drug or vaccine is currently available. Therefore drug repurposing may only provide a quick method for utilizing existing drugs for a therapeutic option. The virus genome contains several non-structural proteins (NSP) which serve as target for designing of antiviral agents. NSP9 of SARS-CoV2 encodes for a replicase enzyme which is essential for the virus replication in the host cell. In search of potent inhibitors, we have screened FDA approved drugs against NSP9 using in silico methods. Five drugs fluspirilene, troglitazone, alvesco, dihydroergotoxine and avodart were found to have highest affinities with the replicase. The molecular dynamics simulation (MDS) studies demonstrated strong drugs binding and stable NSP9-drugs complexes formation. The findings are also strongly supported by root-mean-square deviation, root-mean-square fluctuation, radius of gyration, and hydrogen bond analysis of the complexes. Principal component analysis showed the stable conformation of NSP9 upon drug binding. It could be inferred that these five drugs individually or in combinations may be used as potential inhibitors of NSP9 of SARS-CoV-2 after exploring their in vivo antiviral potential.Communicated by Ramaswamy H. Sarma.
3
项与 甲磺酸二氢麦角碱 相关的新闻（医药）2022-08-30
2022-08-18
2022-07-27
100 项与 甲磺酸二氢麦角碱 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 头痛 | 中国 | 1999-08-13 | |
| 痴呆 | 美国 | 1953-11-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 15 | Matching placebo for 5-Hydroxytryptophan+Ergoloid Mesylates (Ergoloid Mesylates (EM)) | 鑰鑰願積蓋遞範蓋積壓 = 顧夢觸廠憲網淵壓顧遞 壓鏇製鏇積積願醖膚鑰 (鏇選鬱築築構壓願積願, 餘鑰築鹽淵壓構願壓衊 ~ 構鹹蓋鬱築憲襯齋膚淵) 更多 | - | 2024-09-19 | ||
(Ergoloid Mesylates (EM) and 5-hydroxytryptophan (5-HTP)) | 鑰鑰願積蓋遞範蓋積壓 = 鏇遞積獵簾構鹽衊壓餘 壓鏇製鏇積積願醖膚鑰 (鏇選鬱築築構壓願積願, 憲糧糧醖衊積鏇網觸壓 ~ 選範鬱選鏇構築鹹選遞) 更多 |
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