Biphasic effect of apomorphine on rat nociception and effect of dopamine D2 receptor antagonists

Laurido, Claudio; Hernández, Alejandro; Constandil, Luís; Eschalier, Alain

doi:10.1016/j.ejphar.2006.06.081

Cited by 32 publications

(25 citation statements)

References 47 publications

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“…Therefore, it seems likely that apomorphine injection can induce a TRPA1-mediated excitation of nociceptive neurons in vivo, possibly contributing to local reactions at the injection site. This conclusion is further supported by a study that demonstrated a hyperalgesic effect of subcutaneously administered apomorphine on formalin-induced pain in rodents (Pelissier et al, 2006).…”

Section: Discussionsupporting

confidence: 70%

Apomorphine Is a Bimodal Modulator of TRPA1 Channels

et al. 2012

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Apomorphine is a non-narcotic derivative of morphine, which acts as a dopamine agonist and is clinically used to treat "offstates" in patients suffering from Parkinson's disease. Adverse effects of apomorphine treatment include severe emesis and nausea, and ulceration and pain at the injection site. We wanted to test whether sensory transient receptor potential (TRP) channels are a molecular target for apomorphine. Here, we show that rTRPV1, rTRPV2, rTRPV3, and mTRPV4, as well as hTRPM8, and rTRPM3, which are expressed in dorsal root ganglion neurons, are insensitive toward apomorphine treatment. This also applied to the cellular redox sensor hTRPM2. On the contrary, human TRPA1 could be concentrationdependently modulated by apomorphine. Whereas the addition of apomorphine in the low micromolar range produced an irreversible activation of the channel, application of higher concentrations caused a reversible voltage-dependent inhibition of heterologously expressed TRPA1 channels, resulting from a reduction of single-channel open times. In addition, we provide evidence that apomorphine also acts on endogenous TRPA1 in cultured dorsal root ganglion neurons from rats and in the enterochromaffin model cell line QGP-1, from which serotonin is released upon activation of TRPA1. Our study shows that human TRPA1 is a target for apomorphine, suggesting that an activation of TRPA1 might contribute to adverse side effects such as nausea and painful injections, which can occur during treatment with apomorphine.

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Section: Discussionsupporting

confidence: 70%

Apomorphine Is a Bimodal Modulator of TRPA1 Channels

et al. 2012

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“…There is evidence that striatal dopaminergic neurotransmission is specifically involved in antagonizing nociceptive responses Mansikka et al, 2005;Martikainen et al, 2005;Pelissier et al, 2006), since lesioning striatal dopaminergic neurons increases pain sensitivity, whereas activating these neurons inhibits pain responses (Lin et al, 1984). Furthermore, the infusion of D2DR agonists and antagonists reduced and augmented nociception, respectively.…”

Section: Discussionmentioning

confidence: 99%

A New Scenario for Negative Functional Magnetic Resonance Imaging Signals: Endogenous Neurotransmission

Shih¹,

Chen²,

Shyu³

et al. 2009

J. Neurosci.

116

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“…For instance, administration of the dopamine precursor, L-3,4-dihydroxyphenylalanine (L-DOPA), or DA reuptake blockers were shown to elicit antinociception. In addition, some DA receptor antagonists (Bittencourt and Takahashi 1997;Gilbert and Franklin 2001;Pelissier et al 2006;Shimizu et al 2004;Zarrindast et al 1999) have also been described to produce nociception; although other studies have reported either no effect or hyperalgesia with DA receptor agents Fig. 1 The chemical structures of l-THP and l-SPD.…”

Section: Dopaminergic Systems In Regulating Nociceptionmentioning

confidence: 97%

Recent Development in Studies of Tetrahydroprotoberberines: Mechanism in Antinociception and Drug Addiction

et al. 2007

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The tetrahydroprotoberberines (THPBs) are compounds isolated from Chinese herbs that possess a unique pharmacological profile as D2 dopamine receptor antagonists and D1 receptor agonists. l-Tetrahydropalmatine (l-THP) and l-stepholidine (SPD), members of the THPB family, were shown to have potential clinical use in the treatment of pain. However, their mechanism of action is not clear. In the past decades, Chinese scientists have made a great deal of effort to explore the mechanisms by which the THPBs and its analogues elicit antinociception and their potential utility in treating drug abuse. It is now clear that the antinociception produced by l-THP is related to inhibition of D(2) dopamine receptors. The present review focuses on the recent progress made in understanding the mechanisms of l-THP- and l-SPD-mediated antinociception and the sequel of drug addiction.

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Biphasic effect of apomorphine on rat nociception and effect of dopamine D2 receptor antagonists

Cited by 32 publications

References 47 publications

Apomorphine Is a Bimodal Modulator of TRPA1 Channels

Apomorphine Is a Bimodal Modulator of TRPA1 Channels

A New Scenario for Negative Functional Magnetic Resonance Imaging Signals: Endogenous Neurotransmission

Recent Development in Studies of Tetrahydroprotoberberines: Mechanism in Antinociception and Drug Addiction

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