A Classification of Opiate Receptors That Mediate Antinociception in Animals

Tyers, M.B.

doi:10.1111/j.1476-5381.1980.tb07041.x

Cited by 331 publications

(157 citation statements)

References 12 publications

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“…Based on the molar dose that produced almost equi-antinociceptive effects, the order of potency of the anti-writhing effect was ,6-endorphin, MOR, DYN and Met-enkephalin. Our results, showing that the anti-writhing potency of Met-enkephalin (delta agonist) was much lower than those of other agonists (mu or kappa-agonist) are in agreement with the re ports that antinociception against a visceral chemical nociceptive stimulus (AcOH writhing) involves agonist interaction with mu and/or kappa-receptors (28,29). The present results are also consistent with previous re ports that the antinociceptive effects of MOR, i.c.v.…”

Section: Discussionsupporting

confidence: 90%

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Dynorphin-(1-13): Antinociceptive Action and Its Effects on Morphine Analgesia and Acute Tolerance.

Kishioka¹,

Morita²,

Kitabata³

et al. 1992

Jpn.J.Pharmacol

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Antinociceptive actions and effects of intracerebroventricular (i.c.v.) dynorphin-(1-13) (DYN) on morphine (MOR) analgesia and acute tolerance were studied in male Sprague-Dawley rats. Antinociceptive effect against hind paw pressure was produced by 30 ,ug of DYN, but not by 0.5-10 ,u g. Acetic acid writhing was inhibited dose-dependently by DYN at the doses of 2 30 ,u g, and the order of potency of the anti-writhing effect was ,8-endorphin > MOR > DYN >> Met-enkephalin. The anti-writhing effect of DYN that was partially antagonized by naloxone at 10 mg/kg, s.c. in MOR tol erant rats was the same as that in MOR naive rats. The anti-writhing effect of i.c.v.-MOR was increased synergistically by DYN. Continuous s.c. (6 mg/kg/hr) and i.c.v. (7.5,ug/rat/hr) infusion of MOR pro duced antinociception against hind paw pressure, which reached maximum (MAX) and attenuated thereafter during MOR infusion for 6 hr. The attenuation of antinociception was also produced during MOR infusion combined with multiple i.c.v.-injection of DYN. The MAX and area under the anti nociceptive curve during MOR infusion was not affected by multiple injection of DYN, i.e., no effect of i.c.v.-DYN on the development of acute MOR tolerance induced by s.c. and i.c.v.-infusion was observed. In conclusion, the anti-writhing effect of i.c.v.-DYN might not be mediated via mu-receptors, although DYN increased the anti-writhing effect of i.c.v.-MOR synergistically and the development of acute tolerance to MOR (i.c.v., s.c.) was not affected by i.c.v.-DYN.

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Section: Discussionsupporting

confidence: 90%

“…As MOR analgesia can be demon strated by analgesic assays using both mechanical and hot thermal stimuli (28), it is suggested that one of the mechanisms of MOR analgesia is due to the inhibition of SP or SST release induced by noxious stimuli. Dynorphin-(1-17), i.c.v.…”

Section: Discussionmentioning

confidence: 99%

Dynorphin-(1-13): Antinociceptive Action and Its Effects on Morphine Analgesia and Acute Tolerance.

Kishioka¹,

Morita²,

Kitabata³

et al. 1992

Jpn.J.Pharmacol

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“…thresholds (Collier, Dinneen, Johnson & Schneider, 1968;Gray, Osterberg & Scuto, 1970;O'Callaghan & Holtzmann, 1975;Tyers, 1980). Although meptazinol behaved in a manner similar to that of established opioid partial agonists in the rat, the amplitude of responses to this agent in the mouse tail immersion and hot plate procedures was larger than that expected of a partial agonist.…”

Section: Discussionmentioning

confidence: 99%

The antinociceptive activity of meptazinol depends on both opiate and cholinergic mechanisms

Bill

Hartley

Stephens

et al. 1983

British J Pharmacology

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Antinociceptive responses to meptazinol, morphine and oxotremorine and the effects of pretreatment with naloxone or scopolamine on these responses in mice and rats, were examined. 2 Meptazinol evoked larger increases in nociceptive thresholds in the mouse than in the rat, whereas morphine induced large increases in both species. Oxotremorine was both a more potent and a more effective antinociceptive agent in the mouse than in the rat. 3 Antinociceptive responses to meptazinol were consistently inhibited in animals pretreated with naloxone, whereas scopolamine attenuated the effects of meptazinol in some, particularly the mouse tail immersion test, but not in all of the procedures used. 4 Naloxone inhibited all antinociceptive responses to morphine, and scopolamine inhibited all responses to oxotremorine. However, there was no significant interaction between naloxone and oxotremorine or between scopolamine and various opioid analgesic agents. 5 These results indicate that meptazinol, unlike established opioid drugs, may induce antinociception by a dual action on opiate and cholinergic mechanisms.

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“…This effect of K-agonists was investigated more formally by Tyers (1980) and Upton et al (1982) who reported that with K-(but not p-) preferring ligands, appreciably higher doses were required to suppress responses in the rat tail flick and hotplate tests than responses in inflamed paw and writhing tests. Since in these studies drugs were administered systemically, it was not clear to what extent the effects observed were mediated at supraspinal, rather than spinal, sites.…”

Section: Introductionmentioning

confidence: 99%

Spinal antinociceptive actions of μ‐ and κ‐opioids: the importance of stimulus intensity in determining ‘selectivity’ between reflexes to different modalities of noxious stimulus

Parsons

Headley

1989

British J Pharmacology

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1In electrophysiological experiments in spinalized rats, y-and K-opioids were tested intravenously on the responses of single motoneurones to electronically controlled, alternating noxious heat and noxious pinch stimuli. The effects of u-and K-opioids were compared with those of the general anaesthetic x-chloralose and the dissociative anaesthetic/PCP ligand ketamine. 2 The K-opioids U-50,488 (0.5-16 mg kg'-i.v.) and tifluadom (0.05-1.6 mg kg-1 i.v.) had very similar actions to the p-opioid fentanyl (0.5-16 pg kg '-i.v.). Thus all three agonists reduced thermal and mechanical nociceptive reflexes in parallel and in a dose-dependent manner, but only so long as neuronal responses to the alternating stimuli elicited similar excitability levels in the neurone under study. Ketamine (0.5-16mgkg-1 i.v.) had similar actions to the opioids whereas a-chloralose (20 mg kg -i.v.) had very little effect on neuronal responsiveness. 3 Apparently 'selective' depressions by both p-and K-opioids could be orchestrated by a deliberate mismatch of the intensities of alternating noxious heat and pinch stimuli; as measured by neuronal firing rate, the weaker of the responses to either type of stimulus was invariably reduced to a greater degree. 4 Similar 'selectivity' could be demonstrated for both p-and K-ligands when the weaker and stronger responses were of the same modality, being applied by the same pincher device but with alternating applied force. 5 It is concluded that the 'selective' spinal actions of K-opioids seen in non-thermal over thermal behavioural models of nociception is likely to be related to the relative intensities, rather than the modalities, of the noxious stimuli used. The validity of the interpretation of results obtained in such behavioural studies is discussed.

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A Classification of Opiate Receptors That Mediate Antinociception in Animals

Cited by 331 publications

References 12 publications

Dynorphin-(1-13): Antinociceptive Action and Its Effects on Morphine Analgesia and Acute Tolerance.

Dynorphin-(1-13): Antinociceptive Action and Its Effects on Morphine Analgesia and Acute Tolerance.

The antinociceptive activity of meptazinol depends on both opiate and cholinergic mechanisms

Spinal antinociceptive actions of μ‐ and κ‐opioids: the importance of stimulus intensity in determining ‘selectivity’ between reflexes to different modalities of noxious stimulus

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