Analog of neuropeptide FF attenuates morphine abstinence syndrome

Malin, David H.; Lake, John R.; Leyva, Juan E.; Hammond, Maria V.; Rogillio, Robert B.; Arcangeli, K'Anne R.; Ludgate, Karen; Moore, Guy M.; Payza, Kemal

doi:10.1016/0196-9781(91)90052-q

Cited by 53 publications

(18 citation statements)

References 11 publications

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“…Furthermore, NPFF has been implicated in opioid tolerance and dependence (Malin et al, 1990). These findings have led to the suggestion that NPFF may function as an endogenous anti-opioid agent (Yang et al, 1985;Malin et al, 1991;Lake et al, 1992;Rothman, 1992).…”

Section: Introductionmentioning

confidence: 99%

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: Introductionmentioning

confidence: 99%

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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“…However, N/OFQ in the present study is approximately 50 times more potent than NPFF in inducing a QMAS, with 200 ng N/OFQ inducing an effect similar to 10 µg NPFF (Malin et al 1991a(Malin et al , 1996. Another difference is that NPFF was five or ten times more potent in precipitating an abstinence syndrome in morphine dependent rats than it was in inducing a QMAS in non-dependent rats (Malin et al 1990a(Malin et al , 1991b. In contrast, N/OFQ, over a wide dose range, failed to precipitate more behavioral signs in morphine dependent than in non-dependent rats.…”

Section: Discussionmentioning

confidence: 49%

“…This might possibly reflect the central route of administration. In an earlier experiment, third ventricle injection of 10 µg naloxone precipitated numerous types of abstinence signs but failed to precipitate any diarrhea in morphine dependent rats (Malin et al 1991b). Another indicator of severe opiate abstinence is weight loss.…”

Section: Discussionmentioning

confidence: 97%

“…This treatment has previously resulted in marked dependence, as indicated by a subsequent robust morphine abstinence syndrome (Malin et al 1990a(Malin et al , 1990b(Malin et al , 1991b. Morphine dependence produced by this regimen also induced a 5-to 10-fold increase in the abstinence-precipitating potency of NPFF (Malin et al 1990a(Malin et al , 1991b(Malin et al , 1996. The morphine dependent rats were then injected in the third ventricle with various N/OFQ doses ranging from 10-4000 ng in an effort to find a dose region where morphine dependence had a major impact on N/OFQ potency.…”

Section: Effects Of N/ofq In Morphine Dependent Ratsmentioning

confidence: 99%

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Nociceptin/orphanin FQ (N/OFQ) induces a quasi-morphine abstinence syndrome in the rat

et al. 2000

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Nociceptin/orphanin FQ (N/OFQ) is a neuropeptide that exerts antiopiate effects under some circumstances, and there is evidence that it contributes to opiate tolerance. This raises the question, might N/OFQ also contribute to opiate dependence and abstinence? Twenty-two male Sprague-Dawley rats were cannulated in the third ventricle and challenged 7 days later by third ventricle injection of 50, 200 or 1,000 ng N/OFQ or saline alone. Each rat was observed under "blind" conditions for 30 min beginning 15 min after onset of the third ventricle injection. There was a significant positive linear trend of signs as a function of N/OFQ dose. Subjects receiving saline had 18.0+/-2.0 (mean+/-SEM) overall abstinence-like signs, whereas subjects receiving 50, 200 or 1000 ng N/OFQ had 35.2+/-3.6, 49.8+/-2.6 and 63.5+/-9.7 signs, respectively. In 16 additional rats, abstinence-like signs induced by 1000 ng N/OFQ were significantly attenuated by low SC doses of morphine or clonidine. These results raise the possibility that N/OFQ might contribute to opiate dependence and subsequent abstinence syndrome. On the other hand, N/OFQ over a wide dose range induced abstinence signs with similar potency in morphine dependent and non-dependent rats.

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“…compounds derived from endogenous NPFF ligands. Development of antagonists for the NPFFR/GnIH system included N-terminally truncated peptides, like desaminotyrosyl-FLFQRFamide, dansyl-PQRamide and PFR(Tic)amide [42,146-149]. Unfortunately, most of them act as partial agonists with a low affinity and thus limit their use as pharmacological tools.…”

Section: Crosstalk/therapeutical Potentialmentioning

confidence: 99%

RFamide Peptides: Structure, Function, Mechanisms and Pharmaceutical Potential

2011

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Different neuropeptides, all containing a common carboxy-terminal RFamide sequence, have been characterized as ligands of the RFamide peptide receptor family. Currently, five subgroups have been characterized with respect to their N-terminal sequence and hence cover a wide pattern of biological functions, like important neuroendocrine, behavioral, sensory and automatic functions. The RFamide peptide receptor family represents a multiligand/multireceptor system, as many ligands are recognized by several GPCR subtypes within one family. Multireceptor systems are often susceptible to cross-reactions, as their numerous ligands are frequently closely related. In this review we focus on recent results in the field of structure-activity studies as well as mutational exploration of crucial positions within this GPCR system. The review summarizes the reported peptide analogs and recently developed small molecule ligands (agonists and antagonists) to highlight the current understanding of the pharmacophoric elements, required for affinity and activity at the receptor family. Furthermore, we address the biological functions of the ligands and give an overview on their involvement in physiological processes. We provide insights in the knowledge for the design of highly selective ligands for single receptor subtypes to minimize cross-talk and to eliminate effects from interactions within the GPCR system. This will support the drug development of members of the RFamide family.

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Analog of neuropeptide FF attenuates morphine abstinence syndrome

Cited by 53 publications

References 11 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

Nociceptin/orphanin FQ (N/OFQ) induces a quasi-morphine abstinence syndrome in the rat

RFamide Peptides: Structure, Function, Mechanisms and Pharmaceutical Potential

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