Opiranserin hydrochloride salt form · hydrochloride · Parent Opiranserin hydrochloride · Synonyms: VVZ-149 hydrochloride

Opiranserin hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2.

For research use only. Not for human or veterinary use.

Target GlyT 5-HT Receptor P2X Receptor

Research area Neurological Disease

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Data Sheet SDS COA

Opiranserin hydrochloride structure

CAS No.: 1440796-75-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 685.00	BP-02246A-25mg	In stock	Get quote
50 mg	USD 985.00	BP-02246A-50mg	In stock	Get quote
100 mg	USD 1,385.00	BP-02246A-100mg	In stock	Get quote
200 mg	USD 2,185.00	BP-02246A-200mg	In stock	Get quote
500 mg	USD 3,985.00	BP-02246A-500mg	In stock	Get quote

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Description

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).

Biological activity

Opiranserin hydrochloride (25 mg/kg, s.c.) effectively reduced mechanical allodynia and pain-related behaviors with efficacy comparable to 3 mg/kg Morphine Opiranserin hydrochloride (80 mg/kg, p.o.) reduced mechanical allodynia in a rat spinal nerve ligation model

Identifiers

SMILES: O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C.[H]Cl
InChIKey: GSCGQHXDHYVKOL-UHFFFAOYSA-N

Specifications

MW (average): 430.9660
Formula: C₂₁H₃₅ClN₂O₅
CAS No.: 1440796-75-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: 4°C, sealed storage, away from moisture

Solubility

Soluble in DMSO

In vitro: DMSO : 50 mg/mL

Documents

References

[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.

[4]. Christopher L Cioffi. Inhibition of Glycine Re-Uptake: A Potential Approach for Treating Pain by Augmenting Glycine-Mediated Spinal Neurotransmission and Blunting Central Nociceptive Signaling. Biomolecules. 2021 Jun 10;11(6):864.

Same target

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Same research area

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