Movatterモバイル変換

[0]ホーム
URL:

Jump to content
WikipediaThe Free Encyclopedia
Search

Zevaquenabant

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Zevaquenabant
Clinical data
Other namesS-MRI-1867; INV-101; MRI-1867
Legal status
Legal status
  • Investigational
Identifiers
  • (4S)-N-(1-Aminoethylidene)-5-(4-chlorophenyl)-4-phenyl-N′-[4-(trifluoromethyl)phenyl]sulfonyl-3,4-dihydropyrazole-2-carboximidamide
CAS Number
PubChemCID
UNII
Chemical and physical data
FormulaC25H21ClF3N5O2S
Molar mass547.98 g·mol−1

Zevaquenabant (S-MRI-1867,INV-101, orMRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at theNational Institutes of Health. Zevaquenabant was described as a third generationcannabinoid receptor 1 (CB1R) antagonist due to itsperipheral selectivity andpolypharmacology.[1] It acts as a peripherally selectiveinverse agonist of thecannabinoid receptor 1 and aninducible nitric oxide synthase (iNOS) inhibitor.[2][3] It has been studied in the experimental models of fibrotic disorders such asliver fibrosis[1],chronic kidney disease,[4]idiopathic pulmonary fibrosis,[5]Hermansky-Pudlak syndrome pulmonary fibrosis,[6][7] skin fibrosis,[8] and metabolic disorders such asobesity[2] anddyslipidemia.[9]

See also

[edit]

References

[edit]
  1. ^Cinar, R; Iyer, MR; Kunos, G (April 2020)."The therapeutic potential of second and third generation CB(1)R antagonists".Pharmacology & Therapeutics.208: 107477.doi:10.1016/j.pharmthera.2020.107477.PMC 8605822.PMID 31926199.
  2. ^Cinar, Resat; Iyer, Malliga R.; Liu, Ziyi; Cao, Zongxian; Jourdan, Tony; Erdelyi, Katalin; Godlewski, Grzegorz; Szanda, Gergő; Liu, Jie; Park, Joshua K.; Mukhopadhyay, Bani; Rosenberg, Avi Z.; Lieow, Jeih-San; Lorenz, Robin G.; Pacher, Pal; Innis, Robert B.; Kunos, George (21 July 2016)."Hybrid inhibitor of peripheral cannabinoid-1 receptors and inducible nitric oxide synthase mitigates liver fibrosis".JCI Insight.1 (11).doi:10.1172/jci.insight.87336.PMC 4979564.PMID 27525312.
  3. ^Iyer, Malliga R.; Cinar, Resat; Coffey, Nathan J.; Kunos, George (August 2018). "Synthesis of 13 C 6 -labeled, dual-target inhibitor of cannabinoid-1 receptor (CB 1 R) and inducible nitric oxide synthase (iNOS)".Journal of Labelled Compounds and Radiopharmaceuticals.61 (10):773–779.doi:10.1002/jlcr.3639.PMID 29790591.S2CID 46895177.
  4. ^Udi, Shiran; Hinden, Liad; Ahmad, Majdoleen; Drori, Adi; Iyer, Malliga R.; Cinar, Resat; Herman-Edelstein, Michal; Tam, Joseph (January 2020)."Dual inhibition of cannabinoid CB 1 receptor and inducible NOS attenuates obesity-induced chronic kidney disease".British Journal of Pharmacology.177 (1):110–127.doi:10.1111/bph.14849.PMC 6976880.PMID 31454063.
  5. ^Cinar, Resat; Gochuico, Bernadette R.; Iyer, Malliga R.; Jourdan, Tony; Yokoyama, Tadafumi; Park, Joshua K.; Coffey, Nathan J.; Pri-Chen, Hadass; Szanda, Gergő; Liu, Ziyi; Mackie, Ken; Gahl, William A.; Kunos, George (20 April 2017)."Cannabinoid CB1 receptor overactivity contributes to the pathogenesis of idiopathic pulmonary fibrosis".JCI Insight.2 (8).doi:10.1172/jci.insight.92281.PMC 5396529.PMID 28422760.
  6. ^Padilha, Elias C.; Yang, Mengbi; Shah, Pranav; Wang, Amy Q.; Duan, Jianmin; Park, Joshua K.; Zawatsky, Charles N.; Malicdan, May Christine V.; Kunos, George; Iyer, Malliga R.; Gaucher, Geneviève; Ravenelle, François; Cinar, Resat; Xu, Xin (December 2023)."In vitro and in vivo pharmacokinetic characterization, chiral conversion and PBPK scaling towards human PK simulation of S-MRI-1867, a drug candidate for Hermansky-Pudlak syndrome pulmonary fibrosis".Biomedicine & Pharmacotherapy.168: 115178.doi:10.1016/j.biopha.2023.115178.PMC 10715448.PMID 37890204.S2CID 264505730.
  7. ^Cinar, R; Park, JK; Zawatsky, CN; Coffey, NJ; Bodine, SP; Abdalla, J; Yokoyama, T; Jourdan, T; Jay, L; Zuo, MXG; O'Brien, KJ; Huang, J; Mackie, K; Alimardanov, A; Iyer, MR; Gahl, WA; Kunos, G; Gochuico, BR; Malicdan, MCV (July 2021)."CB(1) R and iNOS are distinct players promoting pulmonary fibrosis in Hermansky-Pudlak syndrome".Clinical and Translational Medicine.11 (7): e471.doi:10.1002/ctm2.471.PMC 8255071.PMID 34323400.
  8. ^Zawatsky, CN; Park, JK; Abdalla, J; Kunos, G; Iyer, MR; Cinar, R (2021)."Peripheral Hybrid CB(1)R and iNOS Antagonist MRI-1867 Displays Anti-Fibrotic Efficacy in Bleomycin-Induced Skin Fibrosis".Frontiers in Endocrinology.12: 744857.doi:10.3389/fendo.2021.744857.PMC 8505776.PMID 34650521.
  9. ^Roger, Célia; Buch, Chloé; Muller, Tania; Leemput, Julia; Demizieux, Laurent; Passilly-Degrace, Patricia; Cinar, Resat; Iyer, Malliga R.; Kunos, George; Vergès, Bruno; Degrace, Pascal; Jourdan, Tony (1 October 2020)."Simultaneous Inhibition of Peripheral CB1R and iNOS Mitigates Obesity-Related Dyslipidemia Through Distinct Mechanisms".Diabetes.69 (10):2120–2132.doi:10.2337/db20-0078.PMC 7506827.PMID 32680936.
Receptor
(ligands)
CB1Tooltip Cannabinoid receptor type 1
Agonists
(abridged,
full list)
Inverse agonists
Antagonists
CB2Tooltip Cannabinoid receptor type 2
Agonists
Antagonists
NAGly
(GPR18)
Agonists
Antagonists
GPR55
Agonists
Antagonists
GPR119
Agonists
Transporter
(modulators)
eCBTsTooltip Endocannabinoid transporter
Enzyme
(modulators)
FAAHTooltip Fatty acid amide hydrolase
MAGL
ABHD6
ABHD12
Others
  • Others:2-PG(directly potentiates activity of 2-AG at CB1 receptor)
  • ARN-272(FAAH-like anandamide transporter inhibitor)
See also
Receptor/signaling modulators
Cannabinoids (cannabinoids by structure)
Retrieved from "https://en.wikipedia.org/w/index.php?title=Zevaquenabant&oldid=1248565289"
Categories:
Hidden categories:
[8]ページ先頭
©2009-2025 Movatter.jp