Sex and dose-dependent antinociceptive effects of the JNK (c-Jun N-terminal kinase) inhibitor SU 3327 are mediated by CB2 receptors in female, and CB1/CB2 receptors in male mice in an inflammatory pain model

The antinociceptive effect of methadone in the morphine-resistant inflammatory pain state was described in the paw-withdrawal test using the complete Freund’s adjuvant (CFA)-induced mouse inflammatory pain model. After intraplantar (i.pl.) injection of CFA, thermal hyperalgesia was observed in the ipsilateral paw. The antinociceptive effects of subcutaneous (s.c.) injection of morphine, fentanyl, and oxycodone against thermal hyperalgesia in the inflammatory pain state were reduced in the ipsilateral paw 7 days after CFA pretreatment. On the contrary, the antinociceptive effect of s.c. injection of methadone was maintained in the ipsilateral paw 7 days after CFA pretreatment. The suppressed morphine antinociception in the CFA model mice was bilaterally restored following s.c. treatment with methadone 20 min prior to or 3 days after CFA pretreatment. The suppressed morphine antinociception was also bilaterally restored by intraperitoneal treatment with MK-801 30 min prior to CFA pretreatment; however, the s.c. injection of morphine 30 min prior to CFA pretreatment failed to restore the suppressed morphine antinociception in the CFA model mice. The expression level of mRNA for µ-opioid receptors 7 days after i.pl. pretreatment was not significantly changed by i.pl. pretreatment with CFA or s.c. pretreatment with methadone. In conclusion, methadone is extremely effective against thermal hyperalgesia in the morphine-resistant inflammatory pain state, and restores suppressed morphine antinociception in the inflammatory pain state without altering the expression level of mRNA for µ-opioid receptors.

Download Full-text

RETRACTED: Antinociceptive effects of endomorphin-2: Suppression of substance P release in the inflammatory pain model rat

Neurochemistry International ◽

10.1016/j.neuint.2015.01.004 ◽

2015 ◽

Vol 82 ◽

pp. 1-9 ◽

Cited By ~ 8

Author(s):

Xiao-Na Wu ◽

Tao Zhang ◽

Nian-Song Qian ◽

Xiao-Dong Guo ◽

Hong-Jun Yang ◽

...

Keyword(s):

Substance P ◽

Inflammatory Pain ◽

Pain Model ◽

P Release ◽

Antinociceptive Effects ◽

Substance P Release

Download Full-text

Intrathecal administration of neuronostatin induces an antinociceptive effect in a mouse visceral pain model

Brain Science Advances ◽

10.26599/bsa.2020.9050023 ◽

2020 ◽

Vol 6 (4) ◽

pp. 344-354

Author(s):

Tingji Shao ◽

Shaobin Yang ◽

Peng Yu

Keyword(s):

Visceral Pain ◽

Antinociceptive Effect ◽

Intrathecal Administration ◽

Writhing Test ◽

New Approach ◽

Pain Model ◽

Antinociceptive Effects ◽

Μ Opioid Receptor ◽

G Protein Coupled ◽

Dose Dependent

Neuronostatin (NST) is a peptide encoded by the somatostatin gene that serves important physiological functions in diverse tissues. Previous studies have shown that intracerebroventricular administration of NST induces antinociceptive effects and hyperalgesic effects as determined by the tail immersion assay and formalin test, respectively. In the present study, we aimed to evaluate the effects of intrathecal (i.t.) injection of NST on nociception in a model of visceral pain, and determine possible mechanisms of action in mice. NST (1, 3, 6, or 12 nmol) was administered to mice, leading to a dose‐dependent antinociceptive effect as determined by the acetic acid‐induced writhing test in mice. NST (1 nmol) also enhanced the antinociceptive effect of morphine (2.5 and 5 μg/kg) in the spine. Naloxone and β‐funaltrexamine hydrochloride significantly antagonized the antinociceptive effect of NST. The expression of G‐protein‐coupled receptor 107 (GPR107) protein and the phosphorylation of PKA at Thr197 were increased after i.t. administration of NST, suggesting that the μ‐opioid receptor and GPR107/PKA signaling pathway are involved in the analgesic response. In conclusion, i.t. injection of NST may potentially be used as a new approach in the mediation of visceral pain.

Download Full-text

Chemical Composition and Antinociceptive Potential of Plinia edulis Fruits Peels

Natural Product Communications ◽

10.1177/1934578x1801300503 ◽

2018 ◽

Vol 13 (5) ◽

pp. 1934578X1801300

Author(s):

Luciane Angela Nottar Nesello ◽

Adriana Campos ◽

Karla Capistrano ◽

Fátima de Campos Buzzi ◽

Valdir Cechinel Filho

Keyword(s):

Chemical Composition ◽

Antinociceptive Effect ◽

Reference Drug ◽

Writhing Test ◽

Maslinic Acid ◽

Pain Model ◽

Antinociceptive Effects ◽

Dose Dependent ◽

Dose Dependent Effect ◽

Different Doses

The present study deals with the chemical composition and antinociceptive effects of Plinia edulis fruit peels, analyzed by writhing, formalin, glutamate and capsaicin tests and comparison with two reference analgesic drugs, acetylsalicylic acid and acetaminophen. Phytochemical analyses of the nonpolar fraction (dichloromethane) obtained from the peels of P. edulis fruits revealed the presence of two triterpenes, maslinic acid and ursolic acid. The methanol extract of P. edulis peels showed a pronounced antinociceptive activity in the writhing test, with inhibition of 91.3% at 10 mg/kg, and its dichloromethane and ethyl acetate fractions presented inhibition of 68.3% and 51.5%, respectively. Maslinic acid showed a dose-dependent effect with inhibition of 60.8% at a dose of 10 mg/kg and ID50 value of 3.31 (2.75 to 4.0) mg/kg. The dichloromethane fraction, evaluated in the formalin-induced pain model at a dose of 10 mg/kg, showed a significant effect on both phases of pain. Maslinic acid was evaluated at different doses (1, 3 and 6 mg/kg) and presented a dose-dependent profile in both phases of pain, being more effective than the reference drug (acetaminophen), which was evaluated at 10 mg/kg. The dichloromethane fraction also inhibited the pain induced by glutamate and capsaicin by around 54% and 44%, respectively, whereas maslinic acid was more effective against glutamate, with 62.5% inhibition at 6 mg/kg, and 32% inhibition against capsaicin-induced pain. The results demonstrated that the pronounced antinociceptive effect presented by P. edulis fruits peels is related, at least in part, to the presence of the triterpenes evidenced in this study.

Download Full-text

Retraction notice to “Antinociceptive effects of endomorphin-2: Suppression of substance P release in the inflammatory pain model rat”

Neurochemistry International ◽

10.1016/j.neuint.2016.05.013 ◽

2016 ◽

Vol 97 ◽

pp. 200

Author(s):

Xiao-Na Wu ◽

Tao Zhang ◽

Nian-Song Qian ◽

Xiao-Dong Guo ◽

Hong-Jun Yang ◽

...

Keyword(s):

Substance P ◽

Inflammatory Pain ◽

Pain Model ◽

P Release ◽

Antinociceptive Effects ◽

Retraction Notice ◽

Substance P Release

Download Full-text

The effect of deer antler from East Kalimantan to increase trabecular bone density and calcium levels in serum on osteoporotic mice

Journal of Basic and Clinical Physiology and Pharmacology ◽

10.1515/jbcpp-2020-0140 ◽

2021 ◽

Vol 0 (0) ◽

Author(s):

Retno Widyowati ◽

Suciati Suciati ◽

Dewi Melani Haryadi ◽

Hsin-I Chang ◽

IPG Ngurah Suryawan ◽

...

Keyword(s):

Bone Density ◽

Trabecular Bone ◽

Aqueous Extract ◽

Dependent Manner ◽

Aqueous Extracts ◽

Trabecular Bone Density ◽

Male Mice ◽

Deer Antler ◽

East Kalimantan ◽

Dose Dependent

Abstract Objectives Glucocorticoid-induced osteoporosis (dexamethasone) is a primary cause of secondary osteoporosis by the decreasing formation and increasing resorption activities. Previously, the in vitro study showed that 70% ethanol and aqueous extract of deer antler have increased alkaline phosphatase in osteoblast cell that known as marker of bone formation. The mind of this study is to analyze the effect of deer antlers in increasing the bone trabecular density of osteoporosis-induced male mice. Methods This study used a post-test control group design. A total of 54 healthy male mice were randomly divided to nine groups, i.e., healthy control, osteoporotic, positive control, 70% ethanol (4, 8, and 12 mg/kg BW), and aqueous extracts (4, 8, and 12 mg/kg BW) of deer antler groups. All of the interventions were given 1 mL of test sample for 4 weeks orally. The bone densities were determined using histomorphometry by Image J and Adobe Photoshop. The statistical data were performed using SPSS 23 and statistical significance was set at p<0.05. Results The results showed that alendronate group, 70% ethanol, and aqueous extract groups increased bone density and calcium levels in serum (p<0.05) compared to osteoporotic group in dose dependent manner. It indicated that 70% ethanol and aqueous extract of deer antler stimulating bone turnover and aqueous extract showed the highest. Conclusions Dexamethasone induction for 4 weeks caused osteoporotic mice and the administration of 70% ethanol and aqueous extracts of deer antler from East Kalimantan increased trabecular bone density and calcium levels in dose dependent manner.

Download Full-text

Purinergic ATP triggers moxibustion-induced local anti-nociceptive effect on inflammatory pain model

Purinergic Signalling ◽

10.1007/s11302-021-09815-5 ◽

2021 ◽

Author(s):

Hai-Yan Yin ◽

Ya-Peng Fan ◽

Juan Liu ◽

Dao-Tong Li ◽

Jing Guo ◽

...

Keyword(s):

High Performance Liquid Chromatography ◽

Liquid Chromatography ◽

Inflammatory Pain ◽

Analgesic Effect ◽

Intramuscular Injection ◽

High Performance ◽

Atp Hydrolysis ◽

Purinergic Signalling ◽

Pain Model ◽

Speed Up

AbstractPurinergic signalling adenosine and its A1 receptors have been demonstrated to get involved in the mechanism of acupuncture (needling therapy) analgesia. However, whether purinergic signalling would be responsible for the local analgesic effect of moxibustion therapy, the predominant member in acupuncture family procedures also could trigger analgesic effect on pain diseases, it still remains unclear. In this study, we applied moxibustion to generate analgesic effect on complete Freund’s adjuvant (CFA)-induced inflammatory pain rats and detected the purine released from moxibustioned-acupoint by high-performance liquid chromatography (HPLC) approach. Intramuscular injection of ARL67156 into the acupoint Zusanli (ST36) to inhibit the breakdown of ATP showed the analgesic effect of moxibustion was increased while intramuscular injection of ATPase to speed up ATP hydrolysis caused a reduced moxibustion-induced analgesia. These data implied that purinergic ATP at the location of ST36 acupoint is a potentially beneficial factor for moxibustion-induced analgesia.

Download Full-text