Delving into the Latest Updates on Ergoloid Mesylates with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Co-dergocrine Mesylate, Dihydroergotoxine Mesilate, Dihydroergotoxine Mesylate

+ [29]

Target

α-adrenergic receptor

Action

antagonists

Mechanism

α-adrenergic receptor antagonists(Alpha adrenergic receptor antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

DementiaHeadache

Inactive Indication-

Originator Organization

Novartis Pharmaceuticals Corp.

Active Organization

Lek Pharmaceuticals dd

Inactive Organization

Novartis Pharmaceuticals Corp.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (05 Nov 1953),

Dementia

Regulation-

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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.

01 Apr 2024·Molecular 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

Author: 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.

13 Aug 2022·Journal of Biomolecular Structure and Dynamics

Exploring potential inhibitor of SARS-CoV2 replicase from FDA approved drugs using insilico drug discovery methods

Article

Author: Gurjar, Vaishali ; Chandra, Anshuman ; Qamar, Imteyaz ; Alqahtani, Ali S. ; Ahmed, Mohammad Z. ; Singh, Nagendra

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.

100 Deals associated with Ergoloid Mesylates

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External Link

KEGG	Wiki	ATC	Drug Bank
D02268	Ergoloid Mesylates	C04AE01	DB01049

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Dementia	China	Lek Pharmaceuticals dd	13 Aug 1999
Headache	China	Lek Pharmaceuticals dd	13 Aug 1999

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05030129 (CTgov)	Phase 2	Fragile X Syndrome	15	Matching placebo for 5-Hydroxytryptophan+Ergoloid Mesylates (Ergoloid Mesylates (EM))	frjjjcacjw(xmueayxoqj) = anfrrtamac jzqhxoxnck (mkzlnmuhbb, coiidcmjil - yubtqpqwqu) View more	-	19 Sep 2024
				Ergoloid Mesylates+5-hydroxytryptophan (Ergoloid Mesylates (EM) and 5-hydroxytryptophan (5-HTP))	frjjjcacjw(xmueayxoqj) = lvttangimy jzqhxoxnck (mkzlnmuhbb, psbecapstm - bopiujowuw) View more