L-Tyrosine-induced antinociception in the mouse: involvement of central δ-opioid receptors and bulbo-spinal noradrenergic system

Kawabata, Atsufumi; Kasamatsu, Kazuyo; Takagi, Hiroshi

doi:10.1016/0014-2999(93)90058-p

Cited by 7 publications

(3 citation statements)

References 15 publications

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“…pre-injury injection of serotonin uptake inhibitor fluoxetine and α-2 adrenergic agonist clonidine, dose-dependently prevented the thermal and mechanical hyperalgesia in injured mice. The doses of methysergide and phentolamine were chosen from previous reports in mice [21]. …”

Section: Resultsmentioning

confidence: 99%

Pre-Injury Administration of Morphine Prevents Development of Neuropathic Hyperalgesia through Activation of Descending Monoaminergic Mechanisms in the Spinal Cord in Mice

Rashid

Ueda

2005

Mol Pain

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The present study examined whether pre-injury administration of morphine can prevent partial sciatic nerve injury-induced neuropathic pain in mice. We observed that pre-injury administration of subcutaneous (s.c.) and intracerebroventricular (i.c.v.) morphine dose-dependently prevented the development of both thermal and mechanical hyperalgesia at 7 days following nerve injury in mice. The pre-injury morphine (s.c.)-induced analgesia was significantly blocked by pretreatment with naloxone injected s.c. or i.c.v., but not i.t., suggesting that systemic morphine produced the pre-emptying effects mainly by acting at the supra-spinal sites. Since it is believed that activation of descending monoaminergic mechanisms in spinal cord largely contributes to the supra-spinal analgesic effects of morphine, we investigated the involvement of serotonergic and noradrenergic mechanisms in spinal cord in the pre-injury morphine-induced analgesic effects. We found that preinjury s.c. morphine-induced analgesic effect was significantly blocked by i.t. pretreatment with serotonergic antagonist, methysergide and noradrenergic antagonist, phentolamine. In addition, pre-injury i.t. injection of serotonin uptake inhibitor, fluoxetine and α2-adrenergic agonist, clonidine significantly prevented the neuropathic hyperalgesia. We next examined whether preinjury morphine prevented the expression of neuronal hyperactivity markers such as c-Fos and protein kinase C γ (PKCγ) in the spinal dorsal horn. We found that pre-injury administration of s.c. morphine prevented increased expressions of both c-Fos and PKCγ observed following nerve injury. Similar results were obtained with i.t. fluoxetine and clonidine. Altogether these results suggest that pre-injury administration of morphine might prevent the development of neuropathic pain through activation of descending monoaminergic pain inhibitory pathways.

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Section: Resultsmentioning

confidence: 99%

Pre-Injury Administration of Morphine Prevents Development of Neuropathic Hyperalgesia through Activation of Descending Monoaminergic Mechanisms in the Spinal Cord in Mice

Rashid

Ueda

2005

Mol Pain

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“…Thus, the prodrug strategy, a transient modification of physicochemical properties through chemical derivatization, is the approach of choice for such drugs [1,2]. L-Tyrosine carboxylic esters can be used as prodrugs [3][4][5] for example as antinociceptive [3], while some L-tyrosine derivatives have been proposed for the treatment of Parkinson disease [6,7].…”

Section: Introductionmentioning

confidence: 99%

Tyrosine alkyl esters as prodrug: the structure and intermolecular interactions of l-tyrosine methyl ester compared to l-tyrosine and its ethyl and n-butyl esters

et al. 2011

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L-Tyrosine alkyl esters are used as prodrugs for L-tyrosine. Although prodrugs are often designed for their behavior in solution, understanding their solid-state properties is the first step in mastering drug delivery. The crystal structure of L-tyrosine methyl ester has been determined and compared to published structures of L-tyrosine and its ethyl and n-butyl esters. It is almost isostructural with the other esters: it crystallizes in the orthorhombic chiral space group P2 1 2 1 2 1 , a = 5.7634(15) Å , b = 12.111(2) Å , c = 14.3713(19) Å , V = 1003.1(4) Å 3 with Z 0 = 1. Their main packing motif is a C(9) infinite hydrogen-bond chain, but the conformation of L-tyrosine methyl ester is different from the other two: eclipsed versus U-shaped, respectively. The published structure of the ethyl ester, which was incomplete, has been confirmed by X-ray powder diffraction data. Because L-tyrosine methyl ester is very stable (28 years stored at room temperature), and its hydrolysis rate is relatively low, it should be one of the better prodrugs among the alkyl esters of tyrosine.

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“…Reversal of clinical opiate resistance has been observed following tryptophan administration (47). In rats, tyrosine or its methylester do indeed potentiate morphine analgesia, although this effect appears to be mediated supraspinally rather than in the dorsal horn (62,63).…”

Section: Practical Potentiation Of the Easmentioning

confidence: 99%

DL-phenylalanine markedly potentiates opiate analgesia – an example of nutrient/pharmaceutical up-regulation of the endogenous analgesia system

Russell

McCarty²

2000

Medical Hypotheses

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L-Tyrosine-induced antinociception in the mouse: involvement of central δ-opioid receptors and bulbo-spinal noradrenergic system

Cited by 7 publications

References 15 publications

Pre-Injury Administration of Morphine Prevents Development of Neuropathic Hyperalgesia through Activation of Descending Monoaminergic Mechanisms in the Spinal Cord in Mice

Pre-Injury Administration of Morphine Prevents Development of Neuropathic Hyperalgesia through Activation of Descending Monoaminergic Mechanisms in the Spinal Cord in Mice

Tyrosine alkyl esters as prodrug: the structure and intermolecular interactions of l-tyrosine methyl ester compared to l-tyrosine and its ethyl and n-butyl esters

DL-phenylalanine markedly potentiates opiate analgesia – an example of nutrient/pharmaceutical up-regulation of the endogenous analgesia system

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