Analog of neuropeptide FF attenuates morphine tolerance

Lake, John R.; Hebert, Kathleen M.; Payza, Kemal; Deshotel, Karen D.; Hausam, David D.; Witherspoon, Wendi E.; Arcangeli, K'Anne R.; Malin, David H.

doi:10.1016/0304-3940(92)90078-l

Cited by 47 publications

(14 citation statements)

References 18 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Enhanced activities of anti-opioid neurons are suggested to be involved in the development of tolerance to central morphine. There are several antiopioid neuronal systems in the central nervous system, such as cholecystokinin (34), neuropeptide FF (35), and nociceptin systems (36). Since a complicated neuronal network is not present in the peripheral nervous system, peripheral opioid analgesia may be resistant to the development of tolerance.…”

Section: Discussionmentioning

confidence: 99%

Effects of Loperamide on Mechanical Allodynia Induced by Herpes Simplex Virus Type-1 in Mice

Sasaki¹,

Nakashima²,

Takasaki³

et al. 2007

J Pharmacol Sci

View full text Add to dashboard Cite

Abstract. In the present study, we investigated whether the peripherally acting µ-opioid receptor agonist loperamide would inhibit allodynia in the non-inflamed dermatome of mice with herpetic pain. Subcutaneous (s.c.) injection of loperamide (1 and 3 mg / kg) inhibited allodynia. Local (intraplantar) injection of loperamide (1 and 5 µg / site) also produced an anti-allodynic effect. The peripheral opioid receptor antagonist naloxone methiodide (0.1 mg / kg, s.c.) and the µ-opioid receptor-selective antagonist β-funaltrexamine (40 nmol / site, intraplantar and 20 mg / kg, s.c.) antagonized the anti-allodynic effects of systemic and local loperamide. Local injection of loperamide into the contralateral hind paw was without effect, suggesting that the effect is mediated through local action, not systemic action. Acute and subacute tolerance did not develop to the anti-allodynic effect of loperamide. In addition, there were no cross-tolerance between local opioids (morphine and loperamide) and systemic morphine. These results suggest that stimulation of peripheral µ-opioid receptors suppresses herpetic allodynia without tolerance development. The non-narcotic µ-opioid receptor agonist loperamide may relieve acute herpetic pain in patients with herpes zoster.

show abstract

Section: Discussionmentioning

confidence: 99%

Effects of Loperamide on Mechanical Allodynia Induced by Herpes Simplex Virus Type-1 in Mice

Sasaki¹,

Nakashima²,

Takasaki³

et al. 2007

J Pharmacol Sci

View full text Add to dashboard Cite

show abstract

“…Conversely, antibodies and antagonists to NPFF administered i.c.v. or s.c. have attenuated morphine tolerance in the rat [8][9][10][11]. On the other hand, spinal administration of NPFF has been shown to potently intensify morphine analgesia [12].…”

Section: Introductionmentioning

confidence: 98%

Reversal of morphine tolerance by a compound with NPFF receptor subtype-selective actions

Malin

Henceroth

Izygon

et al. 2015

Neuroscience Letters

Self Cite

View full text Add to dashboard Cite

Neuropeptide FF (NPFF) modulates opiate actions. It has pro-nociceptive effects, primarily through the NPFF receptor 1 subtype, and anti-nociceptive effects, primarily through the NPFFR2 subtype. AC-263093 is a small l, organic, systemically active molecule that was previously shown to functionally activate NPFFR2, but not NPFFR1. It was hypothesized that AC-263093 would attenuate morphine tolerance. Rats were tested for radiant heat tail-flick latency before and after 5 mg/kg morphine sulfate s.c. They were then rendered morphine-tolerant by continuous subcutaneous infusion of 17.52 mg/kg/day morphine sulfate. On the seventh day of infusion, they were retested for analgesia 10 and 20 min after 5mg/kg morphine sulfate s.c. Tolerance was indicated by reduction of morphine analgesia from the pre-infusion test. Fifty minutes prior to morphine challenge, rats received either 10 mg/kg i.p. AC-263093 or injection vehicle alone. AC-2623093-treated rats had far smaller tolerance scores than control rats. This drug effect was significant, p = 0.015. The same dose of AC-263093 had almost no analgesic effect in non-tolerant, saline-infused rats. In vitro experiments revealed that AC-263093 had equal affinity for NPFFR1 and NPFFR2, and functionally inactivated NPFFR1, in addition to its previously shown ability to activate NPFFR2. Thus, altering the balance between activation of NPFF receptor subtypes may provide one approach to reversing opiate tolerance.

show abstract

“…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

View full text Add to dashboard Cite

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.

show abstract

Analog of neuropeptide FF attenuates morphine tolerance

Cited by 47 publications

References 18 publications

Effects of Loperamide on Mechanical Allodynia Induced by Herpes Simplex Virus Type-1 in Mice

Effects of Loperamide on Mechanical Allodynia Induced by Herpes Simplex Virus Type-1 in Mice

Reversal of morphine tolerance by a compound with NPFF receptor subtype-selective actions

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

Contact Info

Product

Resources

About