Importance of sex and relative efficacy at the µ opioid receptor in the development of tolerance and cross-tolerance to the antinociceptive effects of opioids

2001 ◽  
Vol 158 (2) ◽  
pp. 154-164 ◽  
Author(s):  
Andrew Barrett ◽  
Charles Cook ◽  
Jolan Terner ◽  
Rebecca Craft ◽  
Mitchell Picker
Keyword(s):  
Opioid Receptor ◽  
Relative Efficacy ◽  
Cross Tolerance ◽  
Antinociceptive Effects ◽  
Development Of Tolerance

Antinociceptive and morphine modulatory actions of spinal orphanin FQ

1998 ◽  
Vol 76 (3) ◽  
pp. 314-324 ◽  
Author(s):  
K H Jhamandas ◽  
M Sutak ◽  
G Henderson
Keyword(s):  
Opioid Receptor ◽  
Dose Range ◽  
Antinociceptive Effect ◽  
Intrathecal Injection ◽  
Tail Flick ◽  
Orphanin Fq ◽  
Cross Tolerance ◽  
Indwelling Catheters ◽  
Antinociceptive Effects ◽  
Pressure Tests

Orphanin FQ (nociceptin, OFQ), a heptadecapeptide peptide, has been designated as an endogenous ligand at the orphan receptor ORL1, which lacks affinity for opioid receptor ligands. OFQ-like immunoreactivity has been localized in spinal cord areas that are involved in the processing of nociceptive signals. In this study, the effects of spinally administered OFQ on thermal and mechanical nociceptive stimuli were investigated following intrathecal (i.t.) injection in unanesthetized rats bearing chronic indwelling catheters in the subarachnoid space. Intrathecal OFQ produced two distinct acute actions: an opioid-like antinociceptive effect, and antagonism of morphine-induced antinociception. Chronic administration produces tolerance. Acute actions were as follows. First, injection of OFQ alone in the dose range 10-100 nmol produced sustained antinociceptive effects in the tail-flick (baseline latency 1.5-2 s) and paw-pressure tests. These effects peaked at 45-60 min post-injection, were fully reversible, and were observed in absence of discernable motor impairments. Intrathecal naloxone (5 nmol) significantly attenuated the antinociceptive effects of OFQ (50 nmol i.t.) in tail-flick and paw-pressure tests. A 24-h pretreatment with the irreversible opioid receptor antagonist, beta -flunatrexamine (2 nmol i.t.), also attenuated the antinociceptive effects of OFQ (50, 100 nmol i.t.) and of morphine (7.5 nmol i.t.) in both tests. Low doses (1, 5 nmol) of OFQ, which failed to produce antinociception in the tail-flick test involving a baseline latency of 1.5-2 s, produced a strong antinociceptive response when the baseline latency was increased to 5-6 s. Second, intrathecal OFQ, at doses (0.5, 1.0, and 5.0 nmol) that had no antinociceptive activity in the tail-flick (baseline latency 1.5-2 s) and paw-pressure tests, attenuated the antinociceptive effect of morphine (7.5 nmol i.t.) in these tests. However, a threshold OFQ dose (10 nmol) significantly extended the duration of antinociception induced by morphine (7.5 nmol i.t.) or deltorphin (20 nmol i.t.). Chronic actions were as follows. In rats that were rendered tolerant to spinal morphine, by a continuous intrathecal infusion (7.5 nmol/h) of the agonist for 5 days, the OFQ dose-response curves for its antinociceptive effect in the tail-flick and paw-pressure tests were significantly shifted to the right. In separate experiments, repeated intrathecal injection of OFQ (50 nmol) or morphine (7.5 nmol) produced a significant decline in their antinociceptive effects. Thus, intrathecally administered OFQ produces both development of tolerance to its antinociceptive actions and cross-tolerance to the action of morphine.Key words: orphanin FQ, nociceptin, spinal antinociception, opioid antagonism, tolerance, cross-tolerance.

Development of tolerance to antinociceptive effects of an intrathecal morphine/clonidine combination in rats

1995 ◽  
Vol 351 (6) ◽  
pp. 618-623 ◽  
Author(s):  
John L. Plummer ◽  
Patricia L. Cmielewski ◽  
Stephen Tallents ◽  
Pauline De La M. Hall ◽  
John Odontiadis ◽  
...  
Keyword(s):  
Intrathecal Morphine ◽  
Antinociceptive Effects ◽  
Development Of Tolerance

scholarly journals The antinociceptive effects of a dual kappa-delta opioid receptor agonist in the mouse formalin test

2020 ◽  
Vol 31 (2&3) ◽  
pp. 174-178 ◽  
Author(s):  
Esad Ulker ◽  
Wisam Toma ◽  
Alyssa White ◽  
Rajendra Uprety ◽  
Susruta Majumdar ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Formalin Test ◽  
Delta Opioid Receptor ◽  
Opioid Receptor Agonist ◽  
Antinociceptive Effects

The intrinsic antinociceptive effects of oxycodone appear to be κ-opioid receptor mediated

Pain ◽  
1997 ◽  
Vol 73 (2) ◽  
pp. 151-157 ◽  
Author(s):  
Fraser B Ross ◽  
Maree T Smith
Keyword(s):  
Opioid Receptor ◽  
Antinociceptive Effects

Ghrelin receptor agonist, GHRP-2, produces antinociceptive effects at the supraspinal level via the opioid receptor in mice

Peptides ◽  
2014 ◽  
Vol 55 ◽  
pp. 103-109 ◽  
Author(s):  
Ping Zeng ◽  
Shu Li ◽  
Yue-hui Zheng ◽  
Fu-Yan Liu ◽  
Jing-lei Wang ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Ghrelin Receptor ◽  
Antinociceptive Effects ◽  
Ghrelin Receptor Agonist
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