α2-Adrenoceptor modulation of nociception in rat spinal cord: location, effects and interactions with morphine

Sullivan, Ann F.; Dashwood, Michael R.; Dickenson, Anthony H.

doi:10.1016/0014-2999(87)90430-4

Cited by 182 publications

(79 citation statements)

References 29 publications

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“…In agreement with the inferences from the in vitro studies, anpirtoline also behaved as a 5-HTIB receptor agonist in these two tests since it reversed the isolation-induced social behaviour deficit in mice, as did the 5-HT1B receptor agonist TFMPP (Titeler et al, 1987;Schechter, 1988; see Table 4), and increased the nociceptive threshold in the electrostimulated pain-test, as previously found with the potent 5-HTIB receptor agonists, TFMPP and m-chlorophenyl-piperazine (Zemlan et al, 1988). In addition to 5-HT1B receptor agonists, opiates and x2-adrenoceptor agonists also exhibit antinociceptive properties in relevant animal tests (Sullivan et al, 1987;Yaksh & Stevens, 1988 Another interesting property of anpirtoline is its antidepressant-like action in the forced swimming test (Porsolt et al, 1977) in rats. Indeed, anpirtoline was at least as potent as classical antidepressants such as imipramine and desipramine in reducing the immobility time.…”

Section: Discussionsupporting

confidence: 64%

Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Schlicker

Ulrich²,

Hamon

et al. 1992

British J Pharmacology

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3 Like 5-HT, anpirtoline concentration-dependently inhibited forskolin-stimulated adenylate cyclase activity in homogenates from the rat substantia nigra. Both effects were not additive, and could be prevented by 5-HTlB receptor antagonists such as propranolol and penbutolol.4 In superfused rat and pig brain cortex slices preincubated with [3H]-5-HT, the electrically evoked tritium overflow was inhibited by anpirtoline and 5-HT. Whereas 5-HT was equipotent in both tissues (EC50 = 69 nM), anpirtoline was markedly less potent in pig brain cortex slices (EC50 = 1190 nM) than in rat brain cortex slices (EC50 = 55 nM). The concentration-response curve for anpirtoline was shifted to the right by metitepine in both preparations. 5 In the social behaviour deficit test, anpirtoline and trifluoromethylphenyl-piperazine were effective in reversing the isolation-induced impairments in mice, an effect shown only by compounds with agonist properties at the 5-HTIB receptor.6 In the electrostimulated pain test using mice, anpirtoline dose-dependently increased the pain threshold with an ED50 of 0.52mgkg-1, i.p. The antinociceptive activity of anpirtoline was abolished by pretreatment with cyproheptadine or propranolol. 7 In the forced swimming test in rats, anpirtoline induced a dose-related increase in swimming activity. With an ED50 value of 4.6mgkg-1, i.p., anpirtoline was 4 times more potent than the two standard compounds imipramine and desipramine. The decrease of immobility time or the increase of active periods in this model of behavioural despair is suggested to be characteristic of ant-depressant drugs. 8 Anpirtoline exhibits both antinociceptive and antidepressant-like activities in animals. It is probable that anpirtoline elicits these pharmacological effects via its agonist effect on 5-HT1B and 5-HT1A receptors.

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Section: Discussionsupporting

confidence: 64%

Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Schlicker

Ulrich²,

Hamon

et al. 1992

British J Pharmacology

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“…Clonidine, combined with a local anesthetic, increases the quality and duration of epidural analgesia through a mechanism that involves spinal 2 -adrenoreceptors, 5 without interfering with proprioception and without causing the respiratory depression, nausea or pruritus that opioids do. However, 2 -receptor agonist induces hypotension by inhibiting the sympathetic tone.…”

Section: Introductionmentioning

confidence: 99%

Labor analgesia with ropivacaine added to clonidine: a randomized clinical trial

et al. 2008

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CONTEXT AND OBJECTIVE:Previous studies have led to speculation that the association between ropivacaine and clonidine might be more effective than ropivacaine alone. We examined the maternal-fetal effects of two pharmacological approaches: a low dose of ropivacaine or a lower dose of ropivacaine plus clonidine for epidural analgesia during labor. DESIGN AND SETTING:Prospective study at Department of Anesthesiology, Faculdade de Medicina de Botucatu, Universidade Estadual Paulista. METHODS:Thirty-two pregnant women in American Society of Anesthesiologists physical status I and II randomly underwent epidural analgesia using 15 ml of ropivacaine 0.125% (R group) or 15 ml of ropivacaine 0.0625% plus 75 µg clonidine (RC group). Pain intensity, sensory block level, latency time, motor block intensity, duration of labor analgesia and duration of epidural analgesia were evaluated. The newborns were evaluated using Apgar scores and the Amiel-Tison method (neurological and adaptive capacity score). RESULTS:There were no statistically signifi cant differences between the groups regarding pain score, sensory block level, duration of epidural analgesia or Apgar score. The latency time, duration of labor analgesia and motor block were R group < RC group. The half-hour and twohour neurological and adaptive capacity scores were higher in the R group. All of the R group newborns and 75% of the RC group newborns were found to be neurologically healthy at the 24-hour examination. CONCLUSION:Both low-dose ropivacaine and a lower dose plus clonidine relieved maternal pain during obstetric labor. Newborns of mothers who received only ropivacaine showed better neurological and adaptive capacity scores.

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“…The existence of alpha-type receptors, which take part in the transmission of nociceptive stimuli at the spinal level, emphasizes a possible direct action of alpha-adrenergic agonists on neural tissues.3 These receptors are of the alpha2-type. [4][5][6][7] Several experimental and clinical studies have shown that alpha2 adrenergic agonists were able to prolong the dura-CAN J ANAESTH 1991 / 38:7/pp 870-5 tion of action of local anaesthetics and/or to produce analgesia after epidural and intrathecal administration. [8][9][10][11][12][13][14] Recent reports also pointed out that clonidine, an alpha2 agonist, may have benefited patients when it was injected at peripheral nerve sites: after femoral nerve blocks with either lidocaine or bupivacaine, the analgesia obtained with clonidine lasted longer than analgesia obtained with epinephrine.…”

mentioning

confidence: 99%

Brachial plexus block with bupivacaine: effects of added alpha-adrenergic agonists: comparison between clonidine and epinephrine

et al. 1991

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α2-Adrenoceptor modulation of nociception in rat spinal cord: location, effects and interactions with morphine

Cited by 182 publications

References 29 publications

Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Labor analgesia with ropivacaine added to clonidine: a randomized clinical trial

Brachial plexus block with bupivacaine: effects of added alpha-adrenergic agonists: comparison between clonidine and epinephrine

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α2-Adrenoceptor modulation of nociception in rat spinal cord: location, effects and interactions with morphine

Cited by 182 publications

References 29 publications

Anpirtoline, a novel, highly potent 5‐HT1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Anpirtoline, a novel, highly potent 5‐HT1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Labor analgesia with ropivacaine added to clonidine: a randomized clinical trial

Brachial plexus block with bupivacaine: effects of added alpha-adrenergic agonists: comparison between clonidine and epinephrine

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Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents

Anpirtoline, a novel, highly potent 5‐HT_1B receptor agonist with antinociceptive/antidepressant‐like actions in rodents