Delving into the Latest Updates on Brilliant Blue G with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Acid Blue 90, BRILLIANT BLUE G, Brilliant blue G (JAN)

+ [3]

Target

P2X7 receptor

Mechanism

P2X7 receptor antagonists(P2X purinoceptor 7 antagonists)

Therapeutic Areas

Other DiseasesCongenital DisordersEye Diseases+ [1]

Active Indication

Ophthalmologic surgical proceduresFibrosisNephritis+ [1]

Inactive Indication-

Originator Organization

D.O.R.C. Dutch Ophthalmic Research Center (International) BV

Active Organization

D.O.R.C. Dutch Ophthalmic Research Center (International) BV

Kyushu University

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (20 Dec 2019),

Ophthalmologic surgical procedures

RegulationOrphan Drug (US)

Login to view timeline

Structure/Sequence

Molecular FormulaC47H49N3NaO7S2

InChIKeyRWFXCYWTHJDCMJ-UHFFFAOYSA-N

CAS Registry6104-58-1

View All Structures (2)

Psychological stress can lead to emotional disorders, such as anxiety and depression; however, the underlying mechanisms are complicated and remain unclear. In this study, we established a mouse psychological stress model using an improved communication box, in which the psychologically stressed mice received visual, auditory, and olfactory emotional stimuli from the mice receiving electric foot shock, thus avoiding physical stress interference. After the 14-day psychological stress paradigm, our mice exhibited a significant increase in depressive and anxious behaviors. We then performed proteomic liquid chromatography-tandem mass spectrometry for proteomic data analysis of the amygdala, and the results demonstrated that differentially expressed proteins were more enriched in myelin-related biological processes, cellular components, and molecular functions, indicating a correlation between psychological stress-induced emotional disorders and amygdala myelin damage. Molecular and morphological evidence further confirmed that psychological stress damages myelin ultrastructure, downregulated myelin basic protein and proteolipid protein expression, and reduced oligodendrocyte proliferation in the amygdala. Moreover, clemastine, an antimuscarinic and antihistaminic compound that has been shown to enhance oligodendrocyte differentiation and myelination, rescued depressive behaviors accompanied by increased oligodendrogenesis. In the amygdala, psychological stress was also noted to activate microglia and increase the levels of NOD-like receptor protein 3 (NLRP3) and the proinflammatory cytokines interleukin 1β and tumor necrosis factor α, as indicated by ELISA and Western blot analyses. Moreover, in stressed mice, the administration of Brilliant Blue G, a purinergic ligand-gated ion channel 7 receptor (P2X7R) antagonist, completely reversed the increases in NLRP3 and cleaved caspase-1 levels and partially prevented amygdala myelin damage. In conclusion, amygdala demyelination may mediate psychological stress-induced emotional disorders, and P2X7R/NLRP3 cascade activation partially contributes to amygdala myelin damage after psychological stress.

01 Dec 2024·Molecular Immunology

The role and mechanism of P2X7R in cirrhotic cardiomyopathy

Article

Author: Ding, Xu ; Zhou, Yiting ; Shao, Zhenhao ; Dai, Yufei ; Wang, Ruxing ; Wu, Dan ; Luo, Yu ; Yu, Zhiming ; Qian, Lingling ; Zhou, Jiabin

In the context of liver cirrhosis, the incidence of myocardial inflammation and apoptosis escalates, contributing to the development and progression of cirrhotic cardiomyopathy. The P2X7 receptor, a purinergic receptor linked to inflammatory processes, has been identified in the etiology of a range of autoinflammatory, autoimmune, chronic inflammatory, and metabolic disorders. Despite this, the specific role of the P2X7 receptor in the etiology of cirrhotic cardiomyopathy remains to be elucidated. In our research, a cirrhotic cardiomyopathy animal model was established using mice subjected to bile duct ligation. The expression of the P2X7 receptor was suppressed via intraperitoneal administration of Brilliant Blue G. Cardiac function was evaluated using echocardiographic techniques, while histopathological examination and enzyme-linked immunosorbent assays were employed to assess the presence of inflammation and apoptosis in liver and cardiac tissues. The expression of key proteins, including P2X7, NLRP3, and IL-1β, in the myocardial tissue was quantified by Western blot analysis. Our research has unveiled significant findings in a murine model of liver fibrosis induced by two weeks of bile duct ligation. Notably, we detected escalated levels of liver fibrosis coupled with disruptions in liver blood flow dynamics. Concurrently, there was a marked increase in myocardial inflammation and apoptosis, which adversely affected heart function. Intriguingly, the expression of P2X7 receptors (P2X7R) in cardiac and hepatic tissues was found to be significantly elevated. Targeting and inhibiting the expression of P2X7R not only alleviated myocardial inflammation and apoptosis but also enhanced cardiac performance. Furthermore, this intervention resulted in a noticeable reduction in liver fibrosis. The interplay between the P2X7 and NLRP3 pathways emerges as a pivotal mechanism in the etiology and progression of cirrhotic cardiomyopathy. Our findings suggest that modulating the P2X7-NLRP3 axis could offer promising therapeutic avenues for managing cirrhotic cardiomyopathy.

01 Dec 2024·Biomedicine & Pharmacotherapy

The analgesic and gastroprotective activities of the three fungal extracts and their possible correlation with the inhibition of the P2X7 receptor

Article

Author: da Silva Frutuoso, Válber ; Miranda, Julliana Alves Azeredo ; Zani, Carlos Leomar ; da Silva Ferreira, Natiele Carla ; Soares-Bezerra, Rômulo José ; Rosa, Luiz Henrique ; Alves, Luiz Anastacio ; de Almeida Alves, Tânia Maria ; Lima-Quaresma, Kátia Regina Ferreira ; Calheiros, Andrea Surrage ; de Souza, Cristiane Zanon

P2X7 is a purinergic receptor physiologically activated by extracellular ATP. Its activation induces proinflammatory responses, including cytokine release, reactive oxygen species formation, and cell death. Previous in vivo experimental models demonstrated that P2X7 blockade has anti-inflammatory effects; however, there are no drugs used in clinical therapy that act on the P2X7 receptor. In the context of inflammatory diseases, nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used as the first-line treatment; however, their major side effects include stomach ulcer formation, which increases patient morbidity and mortality. Here, we analyzed for the first time the analgesic and gastroprotective activities of three fungal extracts that showed antagonistic effects on P2X7 in vitro. The Antarctic fungal extracts obtained from Vishniacozyma victoriae, Metschnikowia australis, and Ascomycota sp. were tested in animal models of acute pain and ethanol-induced ulceration. These three extracts reduced paw licking by approximately 50 %, which is related to pain behavior, and reduced the number of stomach ulcers 3-7 times compared with the control (70 % ethanol), making them more efficient than the lansoprazole, an NSAID drug, and Brilliant Blue G (BBG), a known P2X7 antagonist, which only halves the number of ulcers. Furthermore, the extracts also protected the gastric mucosa and significantly reduced the levels of liver and renal enzymes compared with those in the ethanol group. Taken together, the fungal extracts presented both analgesic and possibly anti-inflammatory activities and had a protective effect on the gastric epithelium.

100 Deals associated with Brilliant Blue G

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D10799	-	S01	DB15594

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Ophthalmologic surgical procedures	CA	D.O.R.C. Dutch Ophthalmic Research Center (International) BV	-

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Fibrosis	Preclinical	-	-	01 Apr 2013
Nephritis	Preclinical	-	-	01 Apr 2013
Retinal Degeneration	Preclinical	JP	Kyushu University	01 Apr 2011

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2019	Not Applicable	Retinal Perforations	-	brilliant Blue G (No-dye group)	(gdwftrlixq) = The rates of changes in deficiency of EZ at 1 and 6 months compared with baseline in BBG group were significantly greater than those in no dye group bjybtgjrom (qdslpxlexs ) View more	-	01 Jul 2019
				brilliant Blue G (BBG group)
ASN2012	Not Applicable	Ureteral Obstruction P2X7 receptor	-	Brilliant Blue G (Sham operated and saline infusion)	brnsyasylg(sxsebwpzqj) = xdetdhdkmn jyslqefljw (mdtbgrgvon ) View more	Positive	30 Oct 2012
				Sham and BBG 25mg/kg intravenously (IV)	brnsyasylg(sxsebwpzqj) = typnbmutvx jyslqefljw (mdtbgrgvon ) View more
ARVO2011	Not Applicable	Toxicity	-	Brilliant Blue G 1 mg/ml	asvgawwtpw(uhwsgswoca) = olgaxjevbm nxsoftmslk (qoecbormfj )	Positive	01 Apr 2011
ARVO2011	Not Applicable	Optic Nerve Injuries	-	Brilliant Blue G	wqomvdbizb(rrusqurzcx) = dhckxueiju dnsdzufcga (nqyqqyynre ) View more	-	01 Apr 2011
				Vehicle (0.9% NaCl)	(hjmtkziddz) = bujrooiyfs rwafywzgtx (rrlzywplfd )
PO531 (AAO2010)	Not Applicable	Retinal Perforations Adjuvant	-	Brilliant Blue	(teklljimqe) = fjizggopfl kjcipdxrml (aoijyufvaa ) View more	-	18 Oct 2010
				Brilliant Blue	(teklljimqe) = bvlvyvgzrz kjcipdxrml (aoijyufvaa ) View more
ARVO2010	Not Applicable	Toxicity	8	Brilliant Blue G 1mg/ml	iwmhhvailp(uqzkpqsnkb) = hfnsnsfift zsyjxfviix (xuuhapcwkw ) View more	Positive	01 Apr 2010
				Brilliant Blue G Staining (SF6 gas tamponade)	iwmhhvailp(uqzkpqsnkb) = pafaztlhvf zsyjxfviix (xuuhapcwkw ) View more