- Drug Targets, Indications, Patents

Request Demo

Last update 16 May 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Synonyms

Sulpyrine, スルピリン

Target-

Mechanism-

Therapeutic Areas

Active Indication

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest Phase

First Approval Date

JP (14 May 1985),

Regulation-

Structure

Molecular FormulaC13H17N3O4S

InChIKeyLVWZTYCIRDMTEY-UHFFFAOYSA-N

CAS Registry50567-35-6

View All Structures (2)

100 Clinical Results associated with

100 Translational Medicine associated with

100 Patents (Medical) associated with

Literatures (Medical) associated with

01 Oct 2020·Pharmacological ReportsQ4 · MEDICINE

Metamizole relieves pain by influencing cytokine levels in dorsal root ganglia in a rat model of neuropathic pain

Q4 · MEDICINE

Article

Author: Rojewska, Ewelina ; Mika, Joanna ; Wordliczek, Jerzy ; Zajaczkowska, Renata ; Makuch, Wioletta ; Pawlik, Katarzyna ; Kwiatkowski, Klaudia ; Piotrowska, Anna

AbstractBackgroundTreatment of neuropathic pain is still challenging. Recent studies have suggested that dorsal root ganglia (DRG), which carry sensory neural signals from the peripheral nervous system to the central nervous system, are important for pathological nociception. A proper understanding of the significance and function of DRG and their role in pharmacotherapy can help to improve the treatment of neuropathic pain. Metamizole, also known as sulpyrine or dipyrone, is a non-opioid analgesic commonly used in clinical practice, but it is not used for neuropathic pain treatment.MethodsChronic constriction injury (CCI) of the sciatic nerve was induced in Wistar rats. Metamizole was administered intraperitoneally (ip) preemptively at 16 and 1 h before CCI and then twice a day for 7 days. To evaluate tactile and thermal hypersensitivity, von Frey and cold plate tests were conducted, respectively.ResultsOur behavioral results provide evidence that repeated intraperitoneal administration of metamizole diminishes the development of neuropathic pain symptoms in rats. Simultaneously, our findings provide evidence that metamizole diminishes the expression of pronociceptive interleukins (IL-1beta, IL-6, and IL-18) and chemokines (CCL2, CCL4, and CCL7) in DRG measured 7 days after sciatic nerve injury. These assays indicate, for the first time, that metamizole exerts antinociceptive effects on nerve injury-induced neuropathic pain at the DRG level.ConclusionsFinally, we indicate that metamizole-induced analgesia in neuropathy is associated with silencing of a broad spectrum of cytokines in DRG. Our results also suggest that metamizole is likely to be an effective medication for neuropathic pain.Graphic abstract

01 Dec 2018·Pharmacology Biochemistry and BehaviorQ4 · PSYCHOLOGY

Involvement of microglial cells in the antinociceptive effects of metamizol in a mouse model of neuropathic pain

Q4 · PSYCHOLOGY

Article

Author: Makuch, W ; Rojewska, E ; Popiolek-Barczyk, K ; Zajaczkowska, R ; Wordliczek, J ; Mika, J ; Pilat, D

Metamizol (also known as dipyrone or sulpyrine) is one of the non-opioid analgesics commonly used in clinical practice in the treatment of somatic and visceral pain. Here, our results give evidence that repeated twice daily intraperitoneal metamizol administration during 7 days diminished development of neuropathic pain symptoms in a mouse model of neuropathic pain. We observed that metamizol inhibited the activation of spinal microglia in neuropathic mice. Moreover, our findings provide evidence that pronociceptive (IL-1β, XCL1, and CCL2), but not antinociceptive (IL-1α, IL-1RA, and IL-18BP), factors play an important role in metamizol-induced antinociception. We observed that metamizol influences the spinal levels of the nociceptin receptor (NOP) but does not alter the expression of other members of the opioid receptor family (mu (MOP), delta (DOP) and kappa (KOP)), or other important nociception receptors (transient receptor potential vanilloid 1 (TRPV1) and transient receptor potential ankyrin 1 (TRPA1)). Metamizol administration did not affect the levels of the opioid prohormones (proopiomelanocortin (POMC), proenkephalin (PENK), prodynorphin (PDYN), and pronociceptin (PNOC)). However, we observed an enhanced antinociceptive effect of oxycodone, but not buprenorphine, after metamizol treatment. In conclusion, we found that metamizol-induced analgesia in neuropathy is associated with silencing microglia activation and, consequently, with a reduction in pronociceptive cytokines. These results provide evidence that metamizol may join the modest arsenal of effective remedies for neuropathic pain and may constitute part of a multimodal pain therapy.

01 Aug 2011·Clinical & Experimental AllergyQ2 · MEDICINE

Over-expression of LTC4 in mice reproduces human aspirin-induced asthma

Q2 · MEDICINE

Article

Author: M. Arima ; T. Fukuda ; T. Tokuhisa ; H. Hirata ; K. Sugiyama ; Y. Fukushima ; K. Honda

BACKGROUNDThe pathogenesis of aspirin-induced asthma (AIA) is presumed to involve the aspirin/non-steroidal anti-inflammatory drug (NSAID)-induced abnormal metabolism of arachidonic acid, resulting in an increase in 5-lipoxygenase (5-LO) metabolites, particularly leukotriene C(4) (LTC(4) ). However, the role of LTC(4) in the development of AIA has yet to be conclusively demonstrated.OBJECTIVEThe aim of this study was to evaluate the contribution of the lipid product LTC(4) secreted by the 5-LO pathway to the pathogenesis of AIA.METHODSTo evaluate antigen-induced airway inflammation, the concentrations of T-helper type 2 cytokine in bronchoalveolar lavage fluid (BALF) obtained from LTC(4) synthase-transgenic (Tg) and wild-type (WT) mice after challenge with ovalbumin were measured. Subsequently, the ex vivo and in vivo effects of the NSAID sulpyrine were investigated in these Tg and WT mice by measuring the secretion of LTC(4) from sulpyrine-treated BAL cells and the levels of LTC(4) in BALF following challenge with sulpyrine. Finally, the sulpyrine-induced airway response by the administration of pranlukast, an antagonist of the cysteinyl (cs)-LT1 receptor, was analysed.RESULTSThe concentrations of IL-4, -5, and -13 in BALF from Tg mice were significantly higher than those in WT mice. In addition, sulpyrine augmented the secretion of LTC(4) in BALF and by BAL cells in Tg mice, but not in WT mice. Additionally, the increased airway resistance induced by sulpyrine could be reduced by treatment with pranlukast. Furthermore, the secretion of LTC(4) from mast cells, eosinophils, and macrophages was increased in the allergen-stimulated LTC(4) synthase gene Tg mice, even in the absence of sulpyrine, as well as in BAL cells after sulpyrine.CONCLUSION AND CLINICAL RELEVANCEThe over-expression of the LTC(4) synthase in a mouse asthma model also replicates the key features of AIA. And our study supports that cys-LTs play a major role in the pathogenesis of AIA in patients with chronic asthma.

100 Deals associated with

R&D Status

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
-	JP	-	14 May 1985

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

Overview

Basic Info

Structure

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation