ArticlePsychopharmacology2005
Antinociceptive effects of haloperidol and its metabolites in the formalin test in mice.
Article in Psychopharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22 citing papers in PubMed, 88 citations in OpenAlex.
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- Haloperidol drug repurposing unveils ferroptosis involvement in breast cancer cells.Scientific reports · 2025Article
- Novel drug treatments for pain in advanced cancer and serious illness: a focus on neuropathic pain and chemotherapy-induced peripheral neuropathy.Palliative care and social practice · 2024Review
- Fentanyl Structure as a Scaffold for Opioid/Non-Opioid Multitarget Analgesics.International journal of molecular sciences · 2022Review
- Structures of the σNature · 2021Article
- Development of New Benzylpiperazine Derivatives as σACS chemical neuroscience · 2021Article
- Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Effects of Tetrodotoxin in Mouse Models of Visceral Pain.Marine drugs · 2017Article
- The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats.Scientific reports · 2016Article
- Sigma-1 receptor inhibition reverses acute inflammatory hyperalgesia in mice: role of peripheral sigma-1 receptors.Psychopharmacology · 2014Article
- The antagonistic effect of the sigma 1 receptor ligand (+)-MR200 on persistent pain induced by inflammation.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2014Article
- Genetic inactivation and pharmacological blockade of sigma-1 receptors prevent paclitaxel-induced sensory-nerve mitochondrial abnormalities and neuropathic pain in mice.Molecular pain · 2014Article
- The use of very-low-dose methadone for palliative pain control and the prevention of opioid hyperalgesia.Journal of palliative medicine · 2013Article
- Intraoperative haloperidol does not improve quality of recovery and postoperative analgesia.Advanced biomedical research · 2013Article
- Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization.British journal of pharmacology · 2012Article
- The role of antipsychotics in the management of fibromyalgia.CNS drugs · 2012Review
- Antagonism by haloperidol and its metabolites of mechanical hypersensitivity induced by intraplantar capsaicin in mice: role of sigma-1 receptors.Psychopharmacology · 2009Article
- Pharmacology and therapeutic potential of sigma(1) receptor ligands.Current neuropharmacology · 2008Article
- Activation of the spinal sigma-1 receptor enhances NMDA-induced pain via PKC- and PKA-dependent phosphorylation of the NR1 subunit in mice.British journal of pharmacology · 2008Article
- Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice.British journal of pharmacology · 2006Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
rationaleFormalin-induced pain is reduced in sigma-1 (sigma1) receptor knockout mice; therefore, we hypothesized that haloperidol and its metabolites I and II, which have affinity for sigma1 receptors, may modulate formalin-induced pain.
resultsIntraplantar administration of formalin (2.5%) to CD-1 mice produced a biphasic period of pain. Haloperidol (0.03-1 mg/kg, s.c.) and reduced haloperidol (metabolite II, 0.25-8 mg/kg, s.c.) dose-dependently inhibited both phases of formalin-induced pain. Haloperidol metabolite I (4-128 mg/kg, s.c.) also produced dose-dependent antinociception in the second phase of the formalin test, but was less potent and effective against first-phase pain. Haloperidol metabolite III (16 and 128 mg/kg) and (-)sulpiride (200 mg/kg), which have no affinity for sigma1 receptors, did not produce significant antinociception in either phase of the formalin test. The order of potency of the drugs to produce their antinociceptive effect [haloperidol>metabolite II>metabolite I>>metabolite III= (-)sulpiride=inactive] correlated with their affinity for sigma1 receptors, but not with their affinity for sigma2 or dopamine D2 receptors. Naloxone (1 mg/kg, s.c.) did not antagonize the antinociception induced by haloperidol and its metabolites. None of the antinociceptive drugs in the formalin test produced any antinociception in the tail flick test.
conclusionThese results suggest that the antinociceptive effect of haloperidol and its metabolites in the formalin test is not due to unspecific/generalised inhibition of nociception or modulation of opioid receptors, and that it may be related, at least partially, to the ability of these drugs to interact with sigma1 receptors.
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