scholarly journals Antinociceptive effects of dehydrocorydaline in mouse models of inflammatory pain involve the opioid receptor and inflammatory cytokines

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Zhi-Yu Yin ◽  
Lu Li ◽  
Shuai-Shuai Chu ◽  
Qing Sun ◽  
Zheng-Liang Ma ◽  
...  
Keyword(s):  
Mouse Models ◽  
Opioid Receptor ◽  
Inflammatory Cytokines ◽  
Inflammatory Pain ◽  
Antinociceptive Effects

scholarly journals Antinociceptive Efficacy of the µ-Opioid/Nociceptin Peptide-Based Hybrid KGNOP1 in Inflammatory Pain without Rewarding Effects in Mice: An Experimental Assessment and Molecular Docking

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3267
Author(s):  
Maria Dumitrascuta ◽  
Marcel Bermudez ◽  
Olga Trovato ◽  
Jolien De Neve ◽  
Steven Ballet ◽  
...  
Keyword(s):  
Mouse Models ◽  
Inflammatory Pain ◽  
Formalin Test ◽  
Subcutaneous Administration ◽  
Thermal Hyperalgesia ◽  
Nop Receptor ◽  
3D Interaction ◽  
Duration Of Action ◽  
Health Crisis ◽  
Antinociceptive Effects

Opioids are the most effective analgesics, with most clinically available opioids being agonists to the µ-opioid receptor (MOR). The MOR is also responsible for their unwanted effects, including reward and opioid misuse leading to the current public health crisis. The imperative need for safer, non-addictive pain therapies drives the search for novel leads and new treatment strategies. In this study, the recently discovered MOR/nociceptin (NOP) receptor peptide hybrid KGNOP1 (H-Dmt-D-Arg-Aba-β-Ala-Arg-Tyr-Tyr-Arg-Ile-Lys-NH2) was evaluated following subcutaneous administration in mouse models of acute (formalin test) and chronic inflammatory pain (Complete Freund’s adjuvant-induced paw hyperalgesia), liabilities of spontaneous locomotion, conditioned place preference, and the withdrawal syndrome. KGNOP1 demonstrated dose-dependent antinociceptive effects in the formalin test, and efficacy in attenuating thermal hyperalgesia with prolonged duration of action. Antinociceptive effects of KGNOP1 were reversed by naltrexone and SB-612111, indicating the involvement of both MOR and NOP receptor agonism. In comparison with morphine, KGNOP1 was more potent and effective in mouse models of inflammatory pain. Unlike morphine, KGNOP1 displayed reduced detrimental liabilities, as no locomotor impairment nor rewarding and withdrawal effects were observed. Docking of KGNOP1 to the MOR and NOP receptors and subsequent 3D interaction pattern analyses provided valuable insights into its binding mode. The mixed MOR/NOP receptor peptide KGNOP1 holds promise in the effort to develop new analgesics for the treatment of various pain states with fewer MOR-mediated side effects, particularly abuse and dependence liabilities.

scholarly journals Clinical, behavioral and antinociceptive effects of crotalphine in horses

2015 ◽  
Vol 46 (4) ◽  
pp. 694-699
Author(s):  
Erica Cristina Bueno do Prado Guirro ◽  
João Henrique Perotta ◽  
Márcio de Paula ◽  
Yara Cury ◽  
Carlos Augusto Araújo Valadão
Keyword(s):  
Inflammatory Pain ◽  
Antinociceptive Effect ◽  
Behavioral Changes ◽  
Behavioral Effects ◽  
Phase Iii ◽  
Intact Skin ◽  
Kappa Opioid ◽  
Antinociceptive Effects ◽  
Analgesic Peptide ◽  
Scapular Region

ABSTRACT: Crotalphine is a novel analgesic peptide that acts on kappa opioid and delta receptors, causing powerful analgesia in rats submitted to inflammatory, neuropathic or oncologic models of pain. This study evaluated clinical, behavioral and antinociceptive effects caused by crotalphine in horses, employing 18 Arabian horses and it was divided in three phases. In Phase I, "clinical and behavioral effects", crotalphine did not change the latency to urinate and defecate; did not modify the values of cardiac or respiratory rates, intestinal motility and rectal temperature; and did not cause significant ataxia, head, eye and lip ptosis. In Phase II, "antinociceptive effect on intact skin at scapular or ischial region", crotalphine did not cause significant analgesia. In Phase III, "antinociceptive effect on incised skin at scapular or ischial region", crotalphine promoted effective antinociceptive effects for six hours and inhibited hyperalgesia state for three days in the ischial region of horses submitted to incisional model of inflammatory pain, but crotalphine did not evoke relevant analgesic effect on the scapular region. Concluding, intravenous injection of a single dose of crotalphine (3.8ngkg-1) did not cause important clinical or behavioral changes and promotes antinociceptive effect on incised ischial region for seven days in horses. Moreover, crotalphine did not evoke relevant anti nociceptive effect on the scapular region or in intact skin of horses.

The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K+ATP pathway

2015 ◽  
Vol 53 (11) ◽  
pp. 1621-1627 ◽  
Author(s):  
Sonja Vuckovic ◽  
Dragana Srebro ◽  
Katarina Savic Vujovic ◽  
Milica Prostran
Keyword(s):  
Magnesium Sulfate ◽  
Inflammatory Pain ◽  
Pain Model ◽  
Mk 801 ◽  
Antinociceptive Effects
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