Opiranserin

Chemical 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
  • 1441000-45-8
PubChem CID
  • 71566778
UNII
  • AP031EC2NI
Chemical and physical data
FormulaC21H34N2O5
Molar mass394.512 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C(NCC1(N(C)C)CCOCC1)C2=CC(OC)=C(OCCCC)C(OC)=C2
InChI
  • 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 name VVZ-149) is a selective and combined glycine GlyT2 transporter blocker (IC50Tooltip Half-maximal inhibitory concentration = 0.86 μM), purine P2X3 receptor antagonist (IC50 = 0.87 μM), and serotonin 5-HT2A receptor antagonist (IC50Tooltip Half-maximal inhibitory concentration = 1.3 μM) which is under development by Vivozon for the intravenous treatment of postoperative pain.[1][2][3][4] As of April 2017, it is in phase II clinical trials for this indication.[3] The INNTooltip International Nonproprietary Name of the drug was issued in 2017.[2]

References

  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. ^ a b [1][dead link]
  3. ^ a b "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.


  • v
  • t
  • e
Receptor
(ligands)
GlyRTooltip Glycine receptor
NMDARTooltip N-Methyl-D-aspartate receptor
  • See here instead.
Transporter
(blockers)
GlyT1Tooltip Glycine transporter 1
GlyT2Tooltip Glycine transporter 2
See also
Receptor/signaling modulators
GABA receptor modulators
GABAA receptor positive modulators
Ionotropic glutamate receptor modulators
  • v
  • t
  • e
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
See also: Receptor/signaling modulators
  • v
  • t
  • e
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins