Opiranserin

Opiranserin
Clinical data
Other names	VVZ-149; VVZ-000149
Routes of; administration	Intravenous
Identifiers
	IUPAC name 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
Formula	C21H34N2O5
Molar mass	394.512 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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-HT_2A 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

^ 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.
^ ^a ^b [1]^{[dead link]}
^ ^a ^b "Opiranserin - Vivozon - AdisInsight". adisinsight.springer.com.
^ 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.