Opiranserin

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Opiranserin
Opiranserin.svg
Clinical data
Synonyms VVZ-149; VVZ-000149
Routes of
administration
Intravenous
Identifiers
CAS Number
Chemical and physical data
Formula C21H34N2O5
Molar mass 394.505 g/mol
3D model (JSmol)

Opiranserin (INN; developmental code name VVZ-149) is a selective and combined glycine GlyT2 transporter blocker (IC50 = 0.86 µM), purine P2X3 receptor antagonist (IC50 = 0.87 µM), and serotonin 5-HT2A receptor antagonist (IC50 = 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 INN of the drug was issued in 2017.[2]

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. ^ a b http://apps.who.int/medicinedocs/documents/s23256en/s23256en.pdf
  3. ^ a b http://adisinsight.springer.com/drugs/800038462
  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 5318554Freely accessible. PMID 28213593.