GB-83

Names

[ Name ]:
GB-83

[Synonym ]:
5-isoxazoyl-Cha-Ile-spiroindane-1,4'-piperidine
Pentanoic acid,5-isothiocyanato
5-Isothiocyanatovaleriansaeure
5-Isothiocyanato-pentanoic acid
GB-83

Biological Activity

[Description]:

GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Protease-Activated Receptor (PAR)

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

[Target]

PAR2

[In Vitro]

GB83 (10 µM) blocks the effect of MET-1 (microbial ecosystem therapeutic-1) supernatant on nodose ganglion (NG) neurons[2].

[In Vivo]

GB83 (5 µg; i.p.) reverses neutrophil elastase‐induced synovitis and pain in PAR2 KO mice[1]. Animal Model: 8-14 weeks, 20-30 g male C57Bl/6 mice (PAR2 KO mice)[1] Dosage: 5 µg Administration: I.p.; 3 times at 10 min before and 110 and 230 min after neutrophil elastase administered Result: Significantly blocked the neutrophil elastase induced increase in vascular perfusion, as well as the number of rolling adherent leukocytes, and also significantly attenuated hindpaw allodynia.

[References]

[1]. Muley MM, et al. Neutrophil elastase induces inflammation and pain in mouse knee joints via activation of proteinase-activated receptor-2. Br J Pharmacol. 2016 Feb;173(4):766-77.

[2]. Pradhananga S, et al. Protease-dependent excitation of nodose ganglion neurons by commensal gut bacteria. J Physiol. 2020 Jun;598(11):2137-2151.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₄₄N₄O₄

[ Molecular Weight ]:
548.71600

[ Exact Mass ]:
548.33600

[ PSA ]:
108.03000

[ LogP ]:
5.95000

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.