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Opiranserin

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Opiranserin
Clinical data
Other namesVVZ-149; VVZ-000149
Routes of
administration
Intravenous
Identifiers
  • 4-Butoxy-N-([4-(dimethylamino)oxan-4-yl]methyl)-3,5-dimethoxybenzamide
CAS Number
PubChemCID
UNII
Chemical and physical data
FormulaC21H34N2O5
Molar mass394.512 g·mol−1
3D model (JSmol)
  • O=C(NCC1(N(C)C)CCOCC1)C2=CC(OC)=C(OCCCC)C(OC)=C2
  • InChI=1S/C21H34N2O5/c1-6-7-10-28-19-17(25-4)13-16(14-18(19)26-5)20(24)22-15-21(23(2)3)8-11-27-12-9-21/h13-14H,6-12,15H2,1-5H3,(H,22,24)
  • Key:JQUVQWMHZSYCRQ-UHFFFAOYSA-N

Opiranserin (INNTooltip International Nonproprietary Name; developmental code nameVVZ-149) is aselective and combinedglycineGlyT2transporterblocker (IC50Tooltip Half-maximal inhibitory concentration = 0.86 μM),purineP2X3 receptorantagonist (IC50 = 0.87 μM), andserotonin5-HT2A receptor antagonist (IC50Tooltip Half-maximal inhibitory concentration = 1.3 μM) which is under development by Vivozon for theintravenous treatment ofpostoperative pain.[1][2][3][4] As of April 2017, it is inphase IIclinical trials for this indication.[3] TheINNTooltip International Nonproprietary Name of the drug was issued in 2017.[2] Approved for post-operative pain management in South Korea in December of 2024.

References

[edit]
  1. ^Pang MH, Kim Y, Jung KW, Cho S, Lee DH (2012). "A series of case studies: practical methodology for identifying antinociceptive multi-target drugs".Drug Discov. Today.17 (9–10):425–34.doi:10.1016/j.drudis.2012.01.003.PMID 22269134.
  2. ^ab[1][dead link]
  3. ^ab"Opiranserin - Vivozon - AdisInsight".adisinsight.springer.com.
  4. ^Nedeljkovic SS, Correll DJ, Bao X, Zamor N, Zeballos JL, Zhang Y, Young MJ, Ledley J, Sorace J, Eng K, Hamsher CP, Maniam R, Chin JW, Tsui B, Cho S, Lee DH (2017)."Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery".BMJ Open.7 (2) e011035.doi:10.1136/bmjopen-2016-011035.PMC 5318554.PMID 28213593.


Receptor
(ligands)
GlyRTooltip Glycine receptor
NMDARTooltip N-Methyl-D-aspartate receptor
Transporter
(blockers)
GlyT1Tooltip Glycine transporter 1
GlyT2Tooltip Glycine transporter 2
Receptor
(ligands)
P0 (adenine)
P1
(adenosine)
P2
(nucleotide)
P2X
(ATPTooltip Adenosine triphosphate)
P2Y
Transporter
(blockers)
CNTsTooltip Concentrative nucleoside transporters
ENTsTooltip Equilibrative nucleoside transporters
PMATTooltip Plasma membrane monoamine transporter
Enzyme
(inhibitors)
XOTooltip Xanthine oxidase
Others
Others
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Retrieved from "https://en.wikipedia.org/w/index.php?title=Opiranserin&oldid=1315053436"
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