Spinal effect of a neuropeptide FF analogue on hyperalgesia and morphine‐induced analgesia in mononeuropathic and diabetic rats

Courteix, Christine; Coudoré-Civiale, Marie-Ange; Privat, Alain; Zajac, Jean‐Marie; Eschalier, Alain; Fialip, J.

doi:10.1038/sj.bjp.0702682

Cited by 29 publications

(16 citation statements)

References 49 publications

(75 reference statements)

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“…In contrast to ICV injection, intrathecally applied NPFF induces a long lasting naloxone reversible analgesia in both thermal and mechanical tests and, furthermore, NPFF at subeffective doses can potentiate morphine analgesia (Gouarderes et al, 1993). Following this very first report on the antinociceptive activity of NPFF, some additional studies have confirmed this observation in normal rats and in rats with inflammatory or neuropathic pain, for both NPFF or its analogues (Altier et al, 2000;Courteix et al, 1999;Gouarderes et al, 1996a;Gouarderes et al, 1993). A qualitatively similar but more potent effect was observed for the NPFF analogue D-Tyr 1 ,(NMe)Phe 3 -NPFF.…”

Section: Pain and Morphine Modulating Activities And Receptor Bindingsupporting

confidence: 48%

“…In other studies (Altier et al, 2000;Courteix et al, 1999), intrathecal injections of NPFF were found to have no effect on acute thermal or mechanical pain in normal rats; whereas in rats with inflammatory or neuropathic pain, a potent antiallodynic effect was observed. It seems that the antinociceptive effect of NPFF or its analogue, D-Tyr 1 ,(NMe)Phe…”

Section: Pain and Morphine Modulating Activities And Receptor Bindingmentioning

confidence: 99%

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Modulatory role of neuropeptide FF system in nociception and opiate analgesia

2008

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The tetra-peptide FMRF-NH 2 is a cardioexcitatory peptide in the clam. Using the antibody against this peptide, FMRF-NH 2 -like immunoreactive material was detected in mammalian CNS. Subsequently, mammalian FMRF-NH 2 immunoreactive peptides were isolated from bovine brain and characterized to be FLFQPQRF-NH 2 (NPFF) and AGEGLSSPFWSLAAPQRF-NH 2 (NPAF). The genes encoding NPFF precursor proteins and NPFF receptors 1 and 2 are expressed in all vertebrate species examined to date and are highly conserved. Among many biological roles suggested for the NPFF system, the possible modulatory role of NPFF in nocicetion and opiate analgesia has been most widely investigated. Pharmacologically, NPFF-related peptides were found to exhibit analgesia and also potentiate the analgesic activity of opiates when administered intrathecally but attenuate the opiate induced analgesia when administered intracerebroventricularly. RF-NH 2 peptides including NPFF-related peptides were found to delay the rate of acid sensing ion channels (ASIC) desensitization resulting in enhancing acid gated currents, raising the possibility that NPFF also may have a pain modulatory role through ASIC. The genes for NPFF as well as NPFF-R2, preferred receptor for NPFF, are highly unevenly expressed in the rat CNS with the highest levels localized to the superficial layers of the dorsal spinal cord. These two genes are also present in the dorsal root ganglia (DRG), though at low levels in normal rats. NPFF and NPFF-R2 mRNAs were found to be coordinately up-regulated in spinal cord and DRG of rats with peripheral inflammation. In addition, NPFF-R2 immunoreactivity in the primary afferents was increased by peripheral inflammation. The findings from the early studies on the analgesic and morphine modulating activities suggested a role for NPFF in pain modulation and this possibility is further supported by the distribution of NPFF and its receptor and the regulation of the NPFF system in vivo. Published by Elsevier Ltd.

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Section: Pain and Morphine Modulating Activities And Receptor Bindingsupporting

confidence: 48%

Section: Pain and Morphine Modulating Activities And Receptor Bindingmentioning

confidence: 99%

Modulatory role of neuropeptide FF system in nociception and opiate analgesia

2008

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“…In the rat intestine, no NPFF immunoreactivity was seen in the autonomic nervous system or endocrine cells (23). Interestingly, recent investigations have indicated that NPFF can function as an endogenous anti-opioid agent or a pro-opioid agent depending on the animal species (24). There are also species differences in the distribution of NPFF receptors between the human and rat (19).…”

Section: Discussionmentioning

confidence: 89%

Effect of 1DMe, a Neuropeptide FF Analog, on Acetylcholine Release From Myenteric Plexus of Guinea Pig Ileum

Takeuchi

Fujita

Roumy

et al. 2001

Japanese Journal of Pharmacology

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ABSTRACT-Since neuropeptide FF (NPFF) is a putative neurotransmitter to exert anti-opioid activity, we examined the effects of [D-Tyr 1 , (NMe)Phe 3]neuropeptide FF (1DMe), a stable NPFF analog, on acetylcholine (ACh) release from a longitudinal muscle-myenteric plexus (LMMP) preparation of guinea pig ileum in which opioids were known to inhibit ACh release when muscarinic autoinhibition was not fully activated. In the presence of atropine, 1DMe increased spontaneous and electrical field stimulation (EFS)-evoked ACh release in a concentration-dependent manner. Naloxone also increased ACh release. The stimulatory effects of 1DMe and naloxone were not additive. In the absence of atropine, 1DMe did not affect ACh release. Morphine decreased spontaneous and EFS-evoked ACh release in the presence of 1 mM atropine. 1DMe as well as naloxone counteracted the inhibitory effects of morphine on EFS-evoked ACh release. The combination of 1DMe and naloxone was not more inhibitory than either drug alone. 1DMe had no appreciable effect on norepinephrine-induced inhibition of spontaneous and EFS-evoked ACh release. These results first demonstrated the effects of a NPFF analog on neurotransmitter release: 1DMe had a stimulatory effect on spontaneous and EFS-induced ACh release from the LMMP preparation of guinea pig ileum, probably by counteracting the inhibitory effect of endogenous opioids on ACh release.Keywords: Neuropeptide FF, Acetylcholine release, Morphine, Muscarinic autoinhibition, Myenteric plexusThe important role of an octapeptide neuropeptide FF (Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH 2; NPFF) has been demonstrated in the central nervous system (1). NPFF exerts modulatory action on morphine-induced analgesia in rodents (2, 3). Namely, the intracerebroventricular administration of NPFF reverses morphine-induced analgesia in rats (1). NPFF antagonizes the modulation of Ca 2+ channels by mu-opioids in isolated rat spinal ganglion and dorsal raphe neurons (4, 5) and by nociceptin in rat dorsal raphe neurons (5). NPFF modulates the excitatory synaptic transmission through an interaction with presynaptic delta-opioid receptors in the pontine parabrachial nucleus in vitro (6). Although these results suggest that NPFF reverses the effect of morphine or endogenous opioids, the exact mechanism of the action of NPFF at the neuronal and cellular level remains unknown.It is well known that morphine has a marked inhibitory effect on the motility of the gastrointestinal tract in the human as well as experimental animals (7). The inhibitory effect of morphine is mainly due to reduction in acetylcholine (ACh) release from enteric cholinergic neurons (8, 9). In a previous report, we demonstrated that morphine inhibited ACh release from longitudinal muscle with myenteric plexus (LMMP) preparations of the guinea pig ileum when muscarinic autoinhibition was not fully activated (10). We also demonstrated that endogenous opioids are involved in the regulation of ACh release, because naloxone increases electrical field stimulation (EFS)-evoke...

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“…5 mg/rat, and 0.75 mg/rat) [22,23] and four other groups received NMDA receptor antagonist MK801 (0.25 mg/rat, 0.5 mg/rat, 0.75 mg/rat, and 1 mg/rat) [22] and were compared with saline control group. Experiment 2: effects of d-opioid receptor agonist and antagonist on anxiety-like behavior Four groups of rats received bilateral dorsal hippocampus injection (intra-CA1) of selective d receptor agonist enkephalin (1 mg/rat, 2 mg/rat, 5 mg/rat, and 10 mg/rat) [24,25], and four other groups received d receptor antagonist naltrindole hydrochloride (0.25 mg/rat, 0.5 mg/rat, 1 mg/rat, and 2 mg/ratdintra-CA1) [26,27]. These rats were thereafter compared with a saline control group.…”

Section: Drugsmentioning

confidence: 99%

Dorsal hippocampal N‐methyl‐d‐aspartate glutamatergic and δ‐opioidergic systems modulate anxiety behaviors in rats in a noninteractive manner

Solati

2011

The Kaohsiung J of Med Scie

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The present study aimed to investigate the effects of N-methyl-d-aspartate (NMDA)-type glutamate receptor agonist, NMDA, on anxiety-like behavior induced by δ-opioid receptor agents in rats, using the elevated plus maze instrument. The dorsal hippocampus (CA1) is known to play an important role in anxiety formation and modulation. Bilateral administration of different doses of δ-opioid receptor agonist, [d-pen2,5] enkephalin acetate hydrate (1 μg/rat, 2 μg/rat, 5 μg/rat, and 10 μg/rat; 1 μL/rat; 0.5 μL/rat in each side), into CA1 area induced an anxiolytic-like effect, demonstrated by substantial increases in the percent of open arm time (OAT%) and percent of open arm entries (OAE%). Intra-CA1 injection of different doses of δ-opioid receptor antagonist, naltrindole hydrochloride (0.25 μg/rat, 0.5 μg/rat, 1 μg/rat, and 2 μg/rat), produced significant anxiogenic-like behavior. Furthermore, intra-CA1 administration of NMDA glutamate receptor agonist, NMDA (0.125 μg/rat, 0.25 μg/rat, 0.5 μg/rat, and 0.75 μg/rat), increased the OAT% and OAE%, indicating anxiolytic-like behavior. However, administration of different doses of NMDA glutamatergic antagonist, MK801 (0.125 μg/rat, 0.25 μg/rat, 0.5 μg/rat, and 1μg/rat), showed no significant effect on the OAT% but decreased the OAE% significantly. The ineffective dose of NMDA (0.125 μg/rat), when coadministered with enkephalin (1 μg/rat, 2 μg/rat, 5 μg/rat, and 10 μg/rat), did not decrease the anxiety behavior significantly. An effective dose of NMDA (0.5 μg/rat), in combination with different doses of naltrindole hydrochloride (0.25 μg/rat, 0.5 μg/rat, 1 μg/rat, and 2 μg/rat), demonstrated no significant interaction with the OAT%, OAE%, and locomotor activity. These results suggest that CA1 δ-opioid and NMDA glutamatergic systems modulate anxiety behaviors in a noninteractive manner.

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Spinal effect of a neuropeptide FF analogue on hyperalgesia and morphine‐induced analgesia in mononeuropathic and diabetic rats

Cited by 29 publications

References 49 publications

Modulatory role of neuropeptide FF system in nociception and opiate analgesia

Modulatory role of neuropeptide FF system in nociception and opiate analgesia

Effect of 1DMe, a Neuropeptide FF Analog, on Acetylcholine Release From Myenteric Plexus of Guinea Pig Ileum

Dorsal hippocampal N‐methyl‐d‐aspartate glutamatergic and δ‐opioidergic systems modulate anxiety behaviors in rats in a noninteractive manner

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