Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats

Berrocoso, Esther; Benito, M. Dolores De; Micó, Juan Antonio

doi:10.1007/s00213-007-0761-8

Cited by 56 publications

(33 citation statements)

References 46 publications

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“…Previous studies showed that the 5-HT 1A receptor is involved in the anti-nociceptive effect of the 5-HTnoradrenaline reuptake inhibitor venlafaxine (25) and the anti-allodynic effect of the analgesic tramadol (26). We have found that osemozotan inhibited capsaicininduced nociception (licking behavior) (27) and Freund's complete adjuvant (FCA)-induced mechanical allodynia (28) in mice.…”

Section: Hypoalgesiamentioning

confidence: 96%

The Potential Role of Serotonin1A Receptors in Post-weaning Social Isolation–Induced Abnormal Behaviors in Rodents

2014

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Abstract. Post-weaning social isolation in mice induces behavioral abnormalities such as hyperactivity, aggression, depression-and anxiety-like behaviors, deficits of prepulse inhibition, and reduced pain sensitivity to the noxious stimuli. Then, this mouse is considered to be a model of psychiatric disorders including schizophrenia. We have found that serotonin (5-HT) 1A -receptor ligands attenuate these abnormalities, suggesting the pharmacological role of the receptor in treatment of psychiatric disorders. Furthermore, we have recently found that isolation-reared mice show social encounter-induced hyperactivity, a novel phenotype of the abnormal behaviors, and the hyperactivity is triggered by activation of the serotonergic system from the dorsal raphe to the frontal cortex. This review summarizes the effects of 5-HT 1A receptor ligands on aggressive behavior, deficits of prepulse inhibition, reduced pain sensitivity to the noxious stimuli, and encounter-induced hyperactivity in social isolation-reared mice. These findings suggest that the 5-HT 1A receptor is a potential target molecule for treatment of psychiatric disorders and pain.

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Section: Hypoalgesiamentioning

confidence: 96%

The Potential Role of Serotonin1A Receptors in Post-weaning Social Isolation–Induced Abnormal Behaviors in Rodents

2014

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“…Tramadol, in addition to its affinity to opioid receptors, inhibits the neuronal uptake of 5-HT (5-hydroxytryptamine) and NA (noradrenaline) (Berrocoso et al, 2007;Oliva et al, 2002;Reimann and Hennies, 1994). Because compounds known to block monoamine uptake potentially have the antinociceptive effects of opioid including tramadol, the antinociceptive potency and profile of tramadol may derive from its combined opioid binding activity and inhibition of monoamine uptake (Sacerdote et al, 1997).…”

Section: Evaluation Of the Non-opioid Component Of Tramadol On The Prmentioning

confidence: 99%

Effect of tramadol on immune responses and nociceptive thresholds in a rat model of incisional pain

Liu

Zhu

Wang

et al. 2008

J. Zhejiang Univ. Sci. B

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Abstract:Objective: To evaluate the effects of tramadol on the proinflammatory responses in a rat model of incisional pain by investigating its effects on nociceptive thresholds and serum interleukin-6 (IL-6) and IL-2 levels. Methods: Forty-two male Sprague-Dawley (SD) rats scheduled for plantar incision were randomly divided into 7 groups (n=6 in each group). Rats in Group 1 receiving general anesthesia with no incision were served as control; At 30 min before skin incision, Groups 2~5 were given 5 ml normal saline or 1, 10, and 20 mg/kg tramadol, respectively, intraperitoneally (i.p.); Group 6 received 10 mg/kg tramadol after operation; Group 7 received 10 mg/kg tramadol before incision, followed by 200 μg/kg naloxone after operation. Mechanical allodynia was measured by electronic von Frey filament to evaluate the nociceptive thresholds 1 h before incision, and 1 h and 2 h after operation. Serum IL-6 and IL-2 levels were measured by enzyme-linked immunosorbent assay (ELISA) 2 h after operation. Results: Mechanical thresholds decreased significantly and serum IL-6 level increased significantly after operation in Group 2 compared with control (P<0.01), and these changes were reversed respectively by tramadol in a dose-dependent manner (P<0.05 and P<0.01, respectively). IL-2 level remained unchanged after operation in Group 2, but decreased in Group 3 (P<0.05), then gradually returned to the normal level in Groups 4 and 5. The intraperitoneally injected tramadol (10 and 20 mg/kg) produced a potent and dose-dependent antinocicptive effect on the lesioned paw. The antinocicptive effects of tramadol were partially antagonized by naloxone (200 μg/kg), suggesting an additional non-opioid mechanism. Conclusion: The results suggest that tramadol could be a good choice for the treatment of pain under the conditions that immunosuppression may be particularly contraindicated.

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“…104 Interestingly, tramadol, a drug successfully used in pain management, acts through a combination of μ-pioid receptor and 5-HT 1A receptors. 105 Opioids produce their antinociceptive effect partly via activation on central serotonergic neurons. 106 Systemic administration of morphine causes the release of 5-HT in different brainstem locations and the spinal cord dorsal horn.…”

Section: Serotonin Receptors and Opioid Antinociceptive Tolerancementioning

confidence: 99%

The pathophysiological role of serotonin receptor systems in opioid analgesia and tolerance

Özdemir

2017

Int J Basic Clin Pharmacol

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Continuous treatment with opioid analgesics, such as morphine, leads to the development of ant nociceptive tolerance in patients. Although a lot of information about antinociceptive, the pathophysiological mechanisms of tolerance to opioid analgesia are not yet completely understood. Proposed mechanisms for opioid analgesic tolerance comprise down-regulation of opioid receptors, reduction of sensitivity G-proteins, altered intracellular signalling pathway including nitric oxide, adenyl cyclase, and protein kinase C. Numerous physiological and behavioural studies have shown an interaction of the serotonergic system and opioid antinociception. The serotonin (5-HT) receptor system is a necessary component of the spinal and midbrain pain modulation circuit mediating opioid analgesia. Various types of serotonin receptors demonstrate different effects on morphine analgesia. Systemic administration of opioids rise 5-HT levels in the spinal cord dorsal horn and contribute to opioid analgesia in the normal state but reduce that in neuropathic pain via spinal 5-HT3 receptors. Spinal and supraspinal serotonergic neurons may also play a pathophysiological role in the development of morphine analgesic tolerance. Serotonin receptor subtypes show different effects on opioid tolerance. This review paper focus on the current understanding of the role of serotonin receptor systems in opioid analgesia and tolerance.

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Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats

Cited by 56 publications

References 46 publications

The Potential Role of Serotonin1A Receptors in Post-weaning Social Isolation–Induced Abnormal Behaviors in Rodents

The Potential Role of Serotonin1A Receptors in Post-weaning Social Isolation–Induced Abnormal Behaviors in Rodents

Effect of tramadol on immune responses and nociceptive thresholds in a rat model of incisional pain

The pathophysiological role of serotonin receptor systems in opioid analgesia and tolerance

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