Treatment with Antisense Oligodeoxynucleotide to a Conserved Sequence of Opioid Receptors Inhibits Antinociceptive Effects of Delta Subtype Selective Ligands

1995 ◽  
Vol 15 (1-4) ◽  
pp. 643-650 ◽  
Author(s):  
J. Lai ◽  
E. J. Bilsky ◽  
F. Porreca
2017 ◽  
Vol 8 (6) ◽  
pp. 1305-1312 ◽  
Author(s):  
Lakeisha A. Lewter ◽  
Janet L. Fisher ◽  
Justin N. Siemian ◽  
Kashi Reddy Methuku ◽  
Michael M. Poe ◽  
...  

2008 ◽  
Vol 580 (3) ◽  
pp. 306-313 ◽  
Author(s):  
Leonardo M. Loscalzo ◽  
Cristina Wasowski ◽  
Alejandro C. Paladini ◽  
Mariel Marder

The intrathecal infusion of opioid receptor agonists reduces behavioural responses to cutaneous noxious thermal stimuli. Compounds selective for μ- and δ-opioid receptors are clearly effective (Schmauss & Yaksh 1984) but a role for κ receptors is less well established (Han & Xie 1984). The dynorphins, which are present in the dorsal horn, are selective ligands for the K receptor (Corbett et al. 1982). The effects of a dynorphin and those of μ- and δ-selective enkephalin analogues DAGO and DADL, are compared here on the cutaneous sensory responses of single identified dorsal horn neurons whose axons ascend towards supraspinal regions (spinocervical tract, SCT neurons).


2020 ◽  
Vol 11 ◽  
Author(s):  
Chizuko Watanabe ◽  
Asami Komiyama ◽  
Masaru Yoshizumi ◽  
Shinobu Sakurada ◽  
Hirokazu Mizoguchi

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.


Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2237 ◽  
Author(s):  
Chung Ping ◽  
Tengku Tengku Mohamad ◽  
Muhammad Akhtar ◽  
Enoch Perimal ◽  
Ahmad Akira ◽  
...  

Pain is one of the most common cause for hospital visits. It plays an important role in inflammation and serves as a warning sign to avoid further injury. Analgesics are used to manage pain and provide comfort to patients. However, prolonged usage of pain treatments like opioids and NSAIDs are accompanied with undesirable side effects. Therefore, research to identify novel compounds that produce analgesia with lesser side effects are necessary. The present study investigated the antinociceptive potentials of a natural compound, cardamonin, isolated from Boesenbergia rotunda (L) Mansf. using chemical and thermal models of nociception. Our findings showed that intraperitoneal and oral administration of cardamonin (0.3, 1, 3, and 10 mg/kg) produced significant and dose-dependent inhibition of pain in abdominal writhing responses induced by acetic acid. The present study also demonstrated that cardamonin produced significant analgesia in formalin-, capsaicin-, and glutamate-induced paw licking tests. In the thermal-induced nociception model, cardamonin exhibited significant increase in response latency time of animals subjected to hot-plate thermal stimuli. The rota-rod assessment confirmed that the antinociceptive activities elicited by cardamonin was not related to muscle relaxant or sedative effects of the compound. In conclusion, the present findings showed that cardamonin exerted significant peripheral and central antinociception through chemical- and thermal-induced nociception in mice through the involvement of TRPV1, glutamate, and opioid receptors.


2018 ◽  
Vol 33 (2) ◽  
pp. 244-249 ◽  
Author(s):  
Amaia M Erdozain ◽  
Iria Brocos-Mosquera ◽  
Ane M Gabilondo ◽  
J Javier Meana ◽  
Luis F Callado

Background: Three different α2-adrenoceptor (α2-AR) subtypes have been described. The α2A-AR and α2C-AR subtypes are highly expressed in the human prefrontal cortex, where they modulate neurotransmission. However, due to the lack of subtype-selective ligands, the physiological relevance of both subtypes has not been fully resolved. Aims: In this context, the aim of the present study was to characterize the protein expression of both α2-AR subtypes, in different synaptic fractions of postmortem human prefrontal cortex. Methods: A subcellular fractionation of the samples was performed and the protein expression of α2A- and α2C-ARs was measured in presynaptic membranes and postsynaptic density fractions by Western blot. Results: The results revealed that the α2A-AR subtype is mainly located postsynaptically (95±3%) whereas the remaining 5±3% is in the presynapse. Conversely, the α2C-AR subtype showed a similar distribution between pre- and postsynaptic membranes, with a slightly higher percentage present in the presynapse (60±2% vs. 40±2%). Conclusions: These findings could explain some contradictory effects reported for α2-AR agonists and antagonists in the human prefrontal cortex. Furthermore, the present data could contribute to elucidating the therapeutic potential of selectively targeting α2A- or α2C-AR subtypes.


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