Contributions of peripheral and central opioid receptors to antinociception in rat muscle pain models

Sánchez, Esteban Fernández; Bagüés, Ana; Martín, M. I. Fernández San

doi:10.1016/j.pbb.2010.07.009

Cited by 34 publications

(41 citation statements)

References 37 publications

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“…We chose a model of orofacial pain in rat (nocive stimulation of the masseter by injection of hypertonic saline); it is known that, in this model, other drugs, such as opioids, can induce antinociception by peripheral mechanisms. [45-46] In this test, 13a was able to reduce the nociceptive response. It is interesting to remark the different result obtained using this test with respect to the results recorded when the hot plate test was performed.…”

Section: Discussionmentioning

confidence: 91%

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Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties

et al. 2012

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The unwanted psychoactive effects of cannabinoid receptor agonists have limited their development as medicines. These CB 1 mediated side effects are due to the fact that CB 1 receptors are largely expressed in the Central Nervous System (CNS). Since it is known that CB 1 receptors are also located peripherally, there is a growing interest in targeting cannabinoid receptors located outside the brain. A library of chromenopyrazoles designed in analogy to the classical cannabinoid cannabinol were synthesized, characterized and tested for cannabinoid activity. Radiolabeled binding assays were used to determine their affinities at CB 1 and CB 2 receptors. Structural features required for CB 1 /CB 2 affinity and selectivity were explored using molecular modeling. Within the chromenopyrazoles series, some of them showed to be selective CB 1 ligands. These modeling studies suggest that CB 1 full selectivity over CB 2 can be accounted for the presence of a pyrazole ring in the structure. The functional activities of selected chromenopyrazoles were evaluated in isolated tissues. Behavioral tests, in vivo, were then carried on the most effective CB 1 cannabinoid agonist (13a). Chromenopyrazole 13a did not induce modifications in any of the tested parameters on the mouse cannabinoid tetrad, discarding CNS-mediated effects. This lack of agonistic activity in the CNS suggests that it does not readily cross the blood-brain barrier.* nadine@iqm.csic.es. Moreover, compound 13a can induce antinociception in a peripheral model of orofacial pain in rat. Taking into account the negative results obtained in the hot plate test, it could be suggested that the antinociception induced by 13a in the orofacial test may be mediated through peripheral mechanisms. NIH Public Access

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Section: Discussionmentioning

confidence: 91%

“…[46, 52-53] Separated groups of rats (n ≥ 10) were intraperitoneally (i.p.) treated with the vehicle, and compound 13a (1-3 mg/kg) and 30 min after HS was injected in the masseter.…”

Section: Biological Studiesmentioning

confidence: 99%

Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties

et al. 2012

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“…Picard et al 12 reported that there is no evidence of the role of opioids in the peripheral analgesia for acute pain; however, it is worth mentioning that they did not evaluate the role of opioid drugs of intra-articular action, being different from the present study which tried to evaluate the antinociceptive effect of exercise and whether it could occur via peripherally and intra-articular opioid, since the naloxone injection followed different dose and via recommended for systemic action [13][14][15] . Sensitization of articular primary afferent nociceptors (peripheral sensitization) and of neurons of the spinal cord (central sensitization) are basic neuronal processes in pain and mechanical hyperalgesia.…”

Section: Local Pressure (G) Local Pressure (G) Discussionmentioning

confidence: 59%

Uso do exercício resistido antagonizado por naloxone como fator de analgesia em sinovite aguda de joelho de ratos Wistar

Bertolini

Rosa

Silva

et al. 2012

Rev Bras Med Esporte

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Analgesia arising from exercising can occur via release of endogenous opioids in the central nervous system and periphery. However, the literature remains controversial about exercise ways and actions in pain. Thus, the aim of this study was to evaluate whether resistance exercise produces changes on the nociception and suffers interference by applying an opioid inhibitor. 18 rats divided into three groups were used: G1 -hyperalgesia on right knee and untreated; G2 -hyperalgesia and treated with jump sin water; G3-hyperalgesia with previous injection of naloxone and subsequent jumps. To produce hyperalgesia,100µl of 5% formalin was injected in the tibio femoral joint space. Pain was assessed using a digital von Frey filament on the right medial tibiofemoral joint. The evaluation periods were: pre-injury (EV1) after 15 minutes (EV2) and 30 minutes (EV3) and one hour (EV4). The applied exercise was jumpingin water and it occurred after EV2. The animal performed 4 sets of 5 jumps, with an interval of 3 minutes and overload of 50% of body weight. In G1, nociceptive increase was observed, with significant decrease and return to initial baseline values in AV4; G2 showed threshold restoration after exercise and return to baseline; G3 reduced thresholds, without restoration or significant increase in them. We concluded that there was analgesia withuse of exercise and that it was altered by blocking beta-endorphin.

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“…The behavioural assessment of craniofacial muscle nociception was performed in lightly anaesthetised rats; the level of 'light' anaesthesia was determined by providing a noxious pinch to the tail or the hindpaw with serrated forceps (Sanchez et al, 2010;Ro et al, 2003). Animals typically responded to the noxious pinch of the tail with an abdominal constriction and to the noxious pinch of the hindpaw with a withdrawal reflex.…”

Section: Masseter Muscle Proceduresmentioning

confidence: 99%

“…To evaluate the antinociceptive effect of THC in a spinally innervated muscle, the gastrocnemius pain model was used, as previously described (Sanchez Robles et al, 2012;Sanchez et al, 2010); the injection of 500 μl of HS in the mid-region of the gastrocnemius evokes a nociceptive behaviour which consists in withdrawal or flexing of the affected paw. Once HS was injected in the muscle, the animal was kept in a Plexiglas box and two mirrors were positioned underneath and behind it to permit unobstructed viewing of the paw.…”

Section: Gastrocnemius Muscle Proceduresmentioning

confidence: 99%

Involvement of central and peripheral cannabinoid receptors on antinociceptive effect of tetrahydrocannabinol in muscle pain

Bagüés

Martı́n

Sánchez

2014

European Journal of Pharmacology

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Contributions of peripheral and central opioid receptors to antinociception in rat muscle pain models

Cited by 34 publications

References 37 publications

Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties

Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties

Uso do exercício resistido antagonizado por naloxone como fator de analgesia em sinovite aguda de joelho de ratos Wistar

Involvement of central and peripheral cannabinoid receptors on antinociceptive effect of tetrahydrocannabinol in muscle pain

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Contributions of peripheral and central opioid receptors to antinociception in rat muscle pain models

Cited by 34 publications

References 37 publications

Chromenopyrazoles: Non‐psychoactive and Selective CB1 Cannabinoid Agonists with Peripheral Antinociceptive Properties

Chromenopyrazoles: Non‐psychoactive and Selective CB1 Cannabinoid Agonists with Peripheral Antinociceptive Properties

Uso do exercício resistido antagonizado por naloxone como fator de analgesia em sinovite aguda de joelho de ratos Wistar

Involvement of central and peripheral cannabinoid receptors on antinociceptive effect of tetrahydrocannabinol in muscle pain

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Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties

Chromenopyrazoles: Non‐psychoactive and Selective CB₁ Cannabinoid Agonists with Peripheral Antinociceptive Properties