1441000-45-8
Chemical Structure
Opiranserin
Synonym(s): VVZ-149
- CAS No.: 1441000-45-8
- Formula:C21H34N2O5
- Molecular Weight:394.51
IUPAC Name: 4-butoxy-N-((4-(dimethylamino)tetrahydro-2H-pyran-4-yl)methyl)-3,5-dimethoxybenzamide
InChIKey: JQUVQWMHZSYCRQ-UHFFFAOYSA-N
SMILES: O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C
Biological Activity: Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain[1][2][3].
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Opiranserin | Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain. | |||||||||||||||||||||
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- [1]. Oh J, et al. Safety, Tolerability, and Pharmacokinetic Characteristics of a Novel Nonopioid Analgesic, VVZ-149 Injections in Healthy Volunteers: A First-in-Class, First-in-Human Study. J Clin Pharmacol. 2018 Jan;58(1):64-73. [Content Brief]
- [2]. Nedeljkovic SS, et al. 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. 2017 Feb 17;7(2):e011035. [Content Brief]
- [3]. Pang MH, et al. A series of case studies: practical methodology for identifying antinociceptive multi-target drugs. Drug Discov Today. 2012 May;17(9-10):425-34. [Content Brief]
Keywords
