Antinociceptive activity of a novel CB1 receptor agonist in pain and its anti-exudative effect in inflammation in experiment

Gurkin NV, Bykov VV, Bykova AV, Larchenko VV, Il’ina IV, Volcho KP, Salakhutdinov NF, Khazanov VA, Vengerovskii AI. Antinociceptive activity of a novel CB1 receptor agonist in pain and its anti-exudative effect in inflammation in experiment. Russian Journal of Pain. 2025;23(4):13‑18. (In Russ., In Engl.).
https://doi.org/10.17116/pain20252304113

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OBJECTIVE

To study in experiment antinociceptive activity of cannabinoid CB₁ receptor agonist (derivative of 2H-chromene, code CHR) in models of visceral postoperative and neuropathic pain, and to assess the contribution of its potential anti-exudative effect to mechanism of antinociceptive action.

MATERIAL AND METHODS

The study was conducted on CD-1 mice and Sprague Dawley rats. Animals were administered the 2H-chromene derivative CHR orally at an effective dose of 5 mg/kg. Antinociceptive activity of CHR compound was evaluated in models of postoperative and neuropathic pain in comparison with effects of tramadol 20 mg/kg and gabapentin 100 mg/kg. Anti-exudative and antinociceptive effects of CHR compound were investigated after a single administration to rats in a model of hind paw edema induced by carrageenan. We compared these effects with those following injection of sodium diclofenac 10 mg/kg.

RESULTS

CHR compound increased pain threshold by 40 times in postoperative pain model, in experimental neuropathic pain — by 3.5, 70 and 100 times within 1-7 days, respectively. Antinociceptive effect of CHR was not inferior tramadol and gabapentin. In hind paw edema model, CHR compound reduced exudation by 42%, while sodium diclofenac decreased exudation by 67%. Both compounds increased pain threshold by 15 times (p<0.05).

CONCLUSION

The 2H chromene derivative CHR at effective dose of 5 mg/kg demonstrates antinociceptive effect in experimental postoperative and neuropathic pain. CHR inhibits exudation less effectively than sodium diclofenac but demonstrates comparable antinociceptive activity.

Keywords:

2H-chromene derivative

cannabinoid CB1 receptor

agonist

antinociceptive

anti-inflammatory activity

mice

rats

Authors:

N.V. Gurkin

Siberian State Medical University;
Innovative Pharmacology Research LLC (IFAR LLC)

ORCID: 0000-0002-1481-0421

V.V. Bykov

Siberian State Medical University;
Innovative Pharmacology Research LLC (IFAR LLC)

ORCID: 0000-0002-5145-2184

A.V. Bykova

Innovative Pharmacology Research LLC (IFAR LLC)

ORCID: 0000-0002-8495-8560

V.V. Larchenko

Innovative Pharmacology Research LLC (IFAR LLC)

ORCID: 0000-0003-1884-3164

I.V. Il’ina

Novosibirsk Institute of Organic Chemistry

ORCID: 0009-0006-7878-5305

K.P. Volcho

Novosibirsk Institute of Organic Chemistry

ORCID: 0000-0002-4083-9324

N.F. Salakhutdinov

Novosibirsk Institute of Organic Chemistry

ORCID: 0000-0001-8512-4309

V.A. Khazanov

Innovative Pharmacology Research LLC (IFAR LLC)

ORCID: 0000-0002-8833-785X

A.I. Vengerovskii

Siberian State Medical University

ORCID: 0000-0001-5094-3742

Received:

14.04.2025

Accepted:

29.08.2025

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