Opiranserin hydrochloride (Synonyms: VVZ-149 hydrochloride) |
| カタログ番号GC64690 |
オピランセリン (VVZ-149) 塩酸塩は、非オピオイドおよび非 NSAID 鎮痛剤の候補であり、グリシン輸送体 2 型 (GlyT2) およびセロトニン受容体 2A (5HT2A) のデュアル アンタゴニストであり、IC50 はそれぞれ 0.86 および 1.3 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1440796-75-7
Sample solution is provided at 25 µL, 10mM.
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Opiranserin (VVZ-149) hydrochloride, 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 hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain[1][2][3].
[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.
[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.
[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.
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