Characterization of a potent agonist for NPFF receptors: Binding study on rat spinal cord membranes

Jp, Devillers; Mazarguil, Honoré; Allard, Michèle; Dickenson, AH; Jm, Zajac; Simonnet, Guy

doi:10.1016/0028-3908(94)90172-4

Cited by 35 publications

(17 citation statements)

References 23 publications

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“…It is possible that sites targeted by intrathecal NPFF analogues form part of an endogenous mechanism modulating nociceptive transmission at the spinal level. The presence of a high density of NPFF immunoreactivity Allard et al, 1991;Kivipelto et al, 1991;Kivipelto & Panula, 1991a, b) as well as binding sites Devillers et al, 1994), that are partly localized on terminals of the primary afferents (Gouarderes et al, 1993b), supports this notion. Furthermore, in cultured spinal neurones, NPFF has been found to produce both depolarizing and hyperpolarizing responses (Guzman et al, 1989).…”

Section: Discussionmentioning

confidence: 89%

“…NPFF is widely distributed in the rat central nervous system Kivipelto et al, 1989;Kivipelto & Panula, 1991a, b;Allard et al, 1991) and in porcine spinal cord (Wasowicz & Panula, 1994). This neuropeptide binds with high affinity to specific sites Payza et al, 1993;Devillers et al, 1994) that are localized in the superficial laminae of the rat , mouse (Desprat & Zajac, 1994) and human spinal cord .…”

Section: Introductionmentioning

confidence: 99%

“…injection in mice (Gicquel et al, 1992;Desprat & Zajac, 1994) or in rats (Million et al, 1993). Both IDMe and 3D were shown to bind with a high affinity to rat spinal cord NPFF binding sites (Gicquel et al, 1992;Devillers et al, 1994). Therefore, to gain additional insight into the role of NPFF in spinal nociception, we have investigated the effects of intrathecally administered NPFF analogues, IDMe and 3D, using the tail-flick and paw-pressure tests.…”

Section: Introductionmentioning

confidence: 99%

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Role of opioid receptors in the spinal antinociceptive effects of neuropeptide FF analogues

Gouardères

Jhamandas

Sutak

et al. 1996

British J Pharmacology

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1 Neuropeptide FF (NPFF) has been shown to produce antinociceptive effects and enhance morphineinduced antinociception after intrathecal (i.t.) injection. In this study, the spinal effects of two NPFF analogues, [D-Tyr',(NMe) (11 nmol 5 The results of this study show that spinal ,-and 6-opioid receptors play a role in antinociception produced by NPFF analogues. These results also suggest a role for NPFF in modulation of nociceptive signals at the spinal level.

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Section: Discussionmentioning

confidence: 89%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Role of opioid receptors in the spinal antinociceptive effects of neuropeptide FF analogues

Gouardères

Jhamandas

Sutak

et al. 1996

British J Pharmacology

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“…The SB in the presence of various concentrations of test compounds was expressed as percentage of control SB, which was obtained as the TB in the absence of any competing compound minus NSB. Analysis of competition binding experiments was carried out by nonlinear least squares curve fitting with Hill slopes (n H ) being set to unity (Devillers et al, 1994). Affinity constants (K i ) were calculated from the IC 50 values according to the Cheng-Prusoff equation (Cheng and Prusoff, 1973).…”

Section: Methodsmentioning

confidence: 99%

Prolactin Releasing Peptide Has High Affinity and Efficacy at Neuropeptide FF2 Receptors

Engström¹,

Brandt²,

Wurster³

et al. 2003

The Journal of Pharmacology and Experimental Therapeutics

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Neuropeptide FF (NPFF) and prolactin-releasing peptide (PrRP) are two members of the RFamide peptide family. In this study we investigated whether these RFamide peptides, which have common structural features in their C-terminal RFamide motif and share several physiologically important functions, could exert their effects through the same set of receptors. The affinity and functional activity of several related RFamide peptides were determined at the human neuropeptide FF receptor subtype 2 (hNPFF2) and the human prolactin-releasing peptide (hPrRP) receptors. The full-length human prolactin releasing peptide 31 (hPrRP31) had significantly higher efficacy compared with NPFF and its stable analog, (1DMe)Y8Fa, at the hNPFF2 receptor. In contrast, NPFF and (1DMe)Y8Fa were not efficacious at the hPrRP receptor. Our study indicated a generally relatively low level of discrimination for RFamide peptides at the NPFF receptor, whereas the hPrRP receptor clearly preferred PrRP or very closely related peptides. The seemingly promiscuous binding of the RFamide peptides to the NPFF receptor was further confirmed by receptor autoradiography. PrRP may thus signal through the NPFF receptors in vivo.

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“…125 I]YLFQPQRF-NH 2 to rat spinal cord membranes is not affected by opiates (Allard et al, 1989;Devillers et al, 1994) and, furthermore, NPFF does not show significant affinity for any of the opiate receptor subtypes (Raffa et al, 1994). Subsequently the [ 125 I]YLFQPQRF-NH 2 binding site was demonstrated to be G-protein coupled Payza and Yang, 1993).…”

Section: Introductionmentioning

confidence: 92%

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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Characterization of a potent agonist for NPFF receptors: Binding study on rat spinal cord membranes

Cited by 35 publications

References 23 publications

Role of opioid receptors in the spinal antinociceptive effects of neuropeptide FF analogues

Role of opioid receptors in the spinal antinociceptive effects of neuropeptide FF analogues

Prolactin Releasing Peptide Has High Affinity and Efficacy at Neuropeptide FF2 Receptors

Modulatory role of neuropeptide FF system in nociception and opiate analgesia

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