Literature DB >> 33578710

A Comparison of the Antinociceptive Properties of SJP-005 and Morphine in Rats.

Joris C Verster1,2, Andrew Scholey2, Thomas A Dahl3, Jacqueline M Iversen3.   

Abstract

SJP-005 (a combination of ketotifen and ibuprofen) is being developed as a potential treatment for pain and for opioid use disorder. It is therefore important to investigate the potential antinociceptive properties of SJP-005. Two studies were conducted to evaluate the potential effects of SJP-005 in rats. Study 1 applied the von Frey test to examine the antinociceptive effect of morphine with and without SJP-005 in adjuvant-induced hypersensitivity to tactile stimulation. In a double-blind, between-groups design, groups of rats (n = 10 each) received morphine at 3, 10, or 30 mg/kg bodyweight (bw) (subcutaneous injection) with or without SJP-005 (oral). Mechanic allodynia and paw volume were assessed before and after treatment. Study 2 utilized the hot plate test. Using a crossover design, groups of rats (n = 10 each) received either morphine at 3, 10, or 30 mg/kg bw (subcutaneous injection) preceded by oral administration of placebo (Week 1) or SJP-005 (Week 2). In Study 1, in the von Frey up-and-down test, Δ paw withdrawal responses in Group 1 (3 mg/kg bw morphine) were significantly lower compared to those in Group 4 (3 mg/kg bw morphine plus SJP-005), whereas the differences in Δ paw withdrawal between Group 2 and Group 5 (10 mg/kg bw morphine with and without SJP-005) and between Group 3 and Group 6 (10 mg/kg bw morphine with and without SJP-005) did not reach statistical difference. Trendline analysis of the dose-response relationship for the morphine + placebo groups and morphine + SJP-005 groups revealed no significant differences in the intercepts and slopes. In Study 2, no significant differences were observed on hot plate performance between morphine and morphine in combination with SJP-005. In conclusion, the findings in the von Frey up-and-down test (Study 1) suggest that animals can withstand higher levels of painful stimuli when SJP-005 is co-administered. This may also suggest a possible opioid sparing effect. However, in the hot plate test (Study 2), animals did not respond more adaptively to stronger painful stimuli after co-administering SJP-005. These observations warrant further investigation of the antinociceptive properties of SJP-005.

Entities:  

Keywords:  PPAR-γ; SJP-005; TRL4 inhibitor; analgesic properties; opioid dependence; opioid use disorder; opioid withdrawal; pain; treatment

Year:  2021        PMID: 33578710      PMCID: PMC7916340          DOI: 10.3390/pharmaceutics13020243

Source DB:  PubMed          Journal:  Pharmaceutics        ISSN: 1999-4923            Impact factor:   6.321


  23 in total

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Review 5.  Lofexidine, an {alpha}2-receptor agonist for opioid detoxification.

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6.  Pioglitazone attenuates tactile allodynia and thermal hyperalgesia in mice subjected to peripheral nerve injury.

Authors:  Takehiko Maeda; Norikazu Kiguchi; Yuka Kobayashi; Masanobu Ozaki; Shiroh Kishioka
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7.  Antinociceptive and antiedematogenic activities of fenofibrate, an agonist of PPAR alpha, and pioglitazone, an agonist of PPAR gamma.

Authors:  Antônio Carlos P Oliveira; Caryne M Bertollo; Leonardo Tadeu S Rocha; Elias B Nascimento; Karina A Costa; Márcio M Coelho
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8.  Functional observation after morphine withdrawal: effects of SJP-005.

Authors:  Joris C Verster; Andrew Scholey; Thomas A Dahl; Jacqueline M Iversen
Journal:  Psychopharmacology (Berl)       Date:  2021-02-08       Impact factor: 4.530

9.  Challenges in using opioids to treat pain in persons with substance use disorders.

Authors:  Seddon R Savage; Kenneth L Kirsh; Steven D Passik
Journal:  Addict Sci Clin Pract       Date:  2008-06

10.  A double-blind, randomized, placebo-controlled pilot trial to determine the efficacy and safety of ibudilast, a potential glial attenuator, in chronic migraine.

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