The neurokinin-1 receptor antagonist, sendide, exhibits antinociceptive activity in the formalin test

Sakurada, Tsukasa; Katsumata, Kazushige; Yogo, Hiromichi; Tan-No, Koichi; Sakurada, Shinobu; Ohba, Masataka; Kisara, Kensuke

doi:10.1016/0304-3959(94)00107-p

Cited by 39 publications

(14 citation statements)

References 42 publications

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“…Maropitant can provide analgesic effect by blocking the pharmacological action of substance P at the spinal cord and brain [1, 7, 30]. NSAIDs produce analgesic and anti-inflammatory effects by inhibiting the production of prostaglandins [35].…”

Section: Discussionmentioning

confidence: 99%

“…Substance P is an undecapeptide member of the tachykinin neuropeptide family and acts as a neurotransmitter and as a neuromodulator associated with inflammatory process and pain in the spinal cord and brain [10, 14]. Since the endogenous receptor for substance P is NK 1 receptor [13], it is anticipated that NK 1 receptor antagonists, such as maropitant, can provide analgesic effect by blocking the pharmacological action of substance P in the spinal cord and brain [1, 7, 30]. Actually, Boscan et al [6] showed that maropitant reduced the anesthetic requirement during noxious visceral stimulation of the ovary in dogs.…”

Section: Discussionmentioning

confidence: 99%

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Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs

Fukui

Ooyama

Tamura

et al. 2017

The Journal of Veterinary Medical Science

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Maropitant, a neurokinin-1 receptor antagonist, may provide analgesic effects by blocking pharmacological action of substance P. Carprofen is a non-steroidal anti-inflammatory drug commonly used for pain control in dogs. The purpose of this study was to evaluate the effect of a combination of maropitant and carprofen on the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs. Six healthy adult beagle dogs were anesthetized with sevoflurane four times with a minimum of 7-day washout period. On each occasion, maropitant (1 mg/kg) alone, carprofen (4 mg/kg) alone, a combination of maropitant (1 mg/kg) and carprofen (4 mg/kg), or saline (0.1 ml/kg) was subcutaneously administered at 1 hr prior to the first electrical stimulation for the sevoflurane MAC-BAR determination. The sevoflurane MAC-BAR was significantly reduced by maropitant alone (2.88 ± 0.73%, P=0.010), carprofen alone (2.96 ± 0.38%, P=0.016) and the combination (2.81 ± 0.51%, P=0.0003), compared with saline (3.37 ± 0.56%). There was no significant difference in the percentage of MAC-BAR reductions between maropitant alone, carprofen alone and the combination. The administration of maropitant alone and carprofen alone produced clinically significant sparing effects on the sevoflurane MAC-BAR in dogs. However, the combination of maropitant and carprofen did not produce any additive effect on the sevoflurane MAC-BAR reduction. Anesthetic premedication with a combination of maropitant and carprofen may not provide any further sparing effect on anesthetic requirement in dogs.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs

Fukui

Ooyama

Tamura

et al. 2017

The Journal of Veterinary Medical Science

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“…The nociceptive behavioral response consists of licking and biting the injected paw (21,24). BEO protects against N-methyl-D-aspartate (NMDA)-induced cell death by inducing the sustained phosphorylation of Akt kinase (5).…”

Section: Effects Of Naloxone Hydrochloride On Antinociception Inducedmentioning

confidence: 99%

<b>Effect of plantar subcutaneous administration of bergamot essential oil and linalool on formalin-induced nociceptive behavior in </b><b>mice </b>

et al. 2015

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This study investigated the effect of bergamot essential oil (BEO) or linalool, a major volatile component of BEO, on the nociceptive response to formalin. Plantar subcutaneous injection of BEO or linalool into the ipsilateral hindpaw reduced both the first and late phases of the formalininduced licking and biting responses in mice. Plantar subcutaneous injection of BEO or linalool into the contralateral hindpaw did not yield an antinociceptive effect, suggesting that the antinociceptive effect of BEO or linalool in the formalin test occurred peripherally. Intraperitoneal and plantar subcutaneous injection pretreatment with naloxone hydrochloride, an opioid receptor antagonist, significantly attenuated both BEO-and linalool-induced antinociception. Pretreatment with naloxone methiodide, a peripherally acting opioid receptor antagonists, also significantly antagonized the antinociceptive effects of BEO and linalool. Our results provide evidence for the involvement of peripheral opioids in antinociception induced by BEO and linalool. These results suggest that activation of peripheral opioid receptors may play an important role in reducing formalin-induced nociception.The essential oil of bergamot (BEO; Citrus bergamia Risso) is one of the most commonly used essential oils and is familiar to most of the general public. BEO is obtained by cold pressing of the epicarp and part of the mesocarp of the fresh bergamot fruit. BEO consists of a volatile (93-96%) and a nonvolatile fraction (4-7%); the former contains monoterpene and sesquiterpene hydrocarbons and oxygenated derivatives such as linalool and linalyl acetate, while the latter fraction contains waxes, polymethoxylated flavones, coumarins, and psoralens such as bergamottin and bergapten (6,14). BEO has been reported to minimize symptoms of stress-induced anxiety and mild mood disorders, as well as cancer pain, however the mechanistic basis for its use in such applications awaits discovery (1). A previous in vitro study showed that BEO reduced neuronal damage caused by excitotoxic stimuli (5), and significantly increased the extracellular levels of the inhibitory amino acid neurotransmitter gamma-aminobutyric acid (GABA) in rat hippocampus (15). Linalool is a monoterpene compound and is the main volatile component of the essential oils of various plants, including BEO. It has previously been reported that linalool administration produced antibacterial, anticonvulsant, and anti-inflammatory effects, as well as showing antinociceptive activity in several behavioral assays (2)(3)(4)(16)(17)(18)(19)(20). Furthermore, linalool can significantly reduce both mor-

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“…An increase of NK1 receptors has been documented in chronically painful tendon tissue [13]. The NK1 receptor received considerable scientific attention a decade ago, as animal models suggested that blockage of the NK1 receptor would reduce chronic pain [19,20,21,22]. Clinical studies of NK1 blockage in humans, however, showed little effect on pain and further research was halted [23,24].…”

Section: Introductionmentioning

confidence: 99%

PET-Scan Shows Peripherally Increased Neurokinin 1 Receptor Availability in Chronic Tennis Elbow: Visualizing Neurogenic Inflammation?

et al. 2013

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In response to pain, neurokinin 1 (NK1) receptor availability is altered in the central nervous system. The NK1 receptor and its primary agonist, substance P, also play a crucial role in peripheral tissue in response to pain, as part of neurogenic inflammation. However, little is known about alterations in NK1 receptor availability in peripheral tissue in chronic pain conditions and very few studies have been performed on human beings. Ten subjects with chronic tennis elbow were therefore examined by positron emission tomography (PET) with the NK1 specific radioligand [11C]GR205171 before and after treatment with graded exercise. The radioligand signal intensity was higher in the affected arm as compared with the unaffected arm, measured as differences between the arms in volume of voxels and signal intensity of this volume above a reference threshold set as 2.5 SD above mean signal intensity of the unaffected arm before treatment. In the eight subjects examined after treatment, pain ratings decreased in all subjects but signal intensity decreased in five and increased in three. In conclusion, NK1 receptors may be activated, or up-regulated in the peripheral, painful tissue of a chronic pain condition. This up-regulation does, however, have moderate correlation to pain ratings. The increased NK1 receptor availability is interpreted as part of ongoing neurogenic inflammation and may have correlation to the pathogenesis of chronic tennis elbow.Trial RegistrationClinicalTrials.gov NCT00888225 http://clinicaltrials.gov/

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The neurokinin-1 receptor antagonist, sendide, exhibits antinociceptive activity in the formalin test

Cited by 39 publications

References 42 publications

Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs

Interaction between maropitant and carprofen on sparing of the minimum alveolar concentration for blunting adrenergic response (MAC-BAR) of sevoflurane in dogs

<b>Effect of plantar subcutaneous administration of bergamot essential oil and linalool on formalin-induced nociceptive behavior in </b><b>mice </b>

PET-Scan Shows Peripherally Increased Neurokinin 1 Receptor Availability in Chronic Tennis Elbow: Visualizing Neurogenic Inflammation?

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