Sigma antagonists potentiate opioid analgesia in rats

@article{Chien1995SigmaAP,
  title={Sigma antagonists potentiate opioid analgesia in rats},
  author={C C Chien and Gavril W. Pasternak},
  journal={Neuroscience Letters},
  year={1995},
  volume={190},
  pages={137-139}
}
Sigma1 receptor modulation of opioid analgesia in the mouse.
  • J. Mei, G. Pasternak
  • Biology, Psychology
    The Journal of pharmacology and experimental therapeutics
  • 2002
TLDR
The observations confirm the importance of sigma1 receptors as a modulatory system influencing the analgesic activity of opioid drugs, and down-regulating supraspinal s Sigma1binding sites using an antisense approach potentiated mu, delta, kappa1, and kappa3 analgesia in CD-1 mice.
Potentiation of Opioid Analgesia in Dopamine2Receptor Knock-Out Mice: Evidence for a Tonically Active Anti-Opioid System
TLDR
D dopamine D2 receptors represent an additional, significant modulatory system that inhibits analgesic responses to μ and κ opioids, and are examined in a knock-out model in which the dopamine2 (D2) receptor has been disrupted.
Sigma-1 Receptor Antagonists: A New Class of Neuromodulatory Analgesics.
TLDR
Sigma-1 antagonists (in the absence of opioids) have been shown to exert antinociceptive effects in preclinical models of neuropathic pain induced by nerve trauma or chemical injury, and more recently in inflammatory and ischemic pain.
Sigma-1 receptors and animal studies centered on pain and analgesia
TLDR
The importance of sigma-1 receptors as pain generators in multiple animal models is reviewed in order to illustrate both the importance of these unique receptors in pathologic pain and the potential benefits to s Sigma-1 receptor antagonists as analgesics.
Modulation of Brainstem Opiate Analgesia in the Rat by σ1 Receptors: A Microinjection Study
  • J. Mei, G. Pasternak
  • Biology, Psychology
    Journal of Pharmacology and Experimental Therapeutics
  • 2007
TLDR
The pharmacological importance of σ1 receptors in the brainstem modulation of opioid analgesia is illustrated by studies showing their importance in the role of periaqueductal gray, rostroventral medulla, and locus coeruleus of the rat, regions previously shown to be sensitive to morphine.
Opioid adjuvant strategy: improving opioid effectiveness.
  • F. Bihel
  • Biology, Medicine
    Future medicinal chemistry
  • 2016
TLDR
This current review focuses on strategies combining opioids to other drugs that can modulate opioid-mediated effects, including N-methyl-D-aspartate receptor antagonists, 5-HT7 agonists, sigma-1 antagonists, I2-R ligands, cholecystokinin antagonists, neuropeptide FF-R antagonists and toll-like receptor 4 antagonists.
Propionamide Derivatives as Dual μ-Opioid Receptor Agonists and σ1 Receptor Antagonists for the Treatment of Pain.
TLDR
A new series of propionamide derivatives was developed as dual μ-opioid receptor agonists and σ1 receptor antagonists that showed good analgesic effects in several animal models of both acute and chronic pain, with reduced gastrointestinal effects in comparison with oxycodone.
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References

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Selective antagonism of opioid analgesia by a sigma system.
  • C. Chien, G. Pasternak
  • Biology, Psychology
    The Journal of pharmacology and experimental therapeutics
  • 1994
TLDR
Sigma 1 systems functionally antagonize opioid analgesia without affecting morphine's effects on gastrointestinal transit or lethality, and the antiopioid sigma system is tonically active and is more active against kappa analgesia than mu.
Pharmacological actions of a novel mixed opiate agonist/antagonist: naloxone benzoylhydrazone.
TLDR
Low doses of NalBzoH also partially reversed the inhibition of gastrointestinal transit in mice produced by morphine, antagonized completely morphine lethality and precipitated withdrawal in morphine-dependent mice, confirming its antagonist activity in mu receptors.
The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
TLDR
It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists.
Pharmacological mechanisms of opioid analgesics.
  • G. Pasternak
  • Biology, Medicine
    Clinical neuropharmacology
  • 1993
TLDR
The relief of pain involves the complex interaction of at least six receptor systems, and the implications of opiate receptor multiplicity on the control of pain are discussed.
Naloxone benzoylhydrazone (NalBzoH) analgesia.
TLDR
Observations confirm the opioid nature of NalBzoH analgesia and imply a supraspinal mechanism of action and antagonizes mu, delta and kappa 1 actions while retaining its ability to elicit analgesia through a novel and distinct suPRaspinal kappa 3 system.
Sigma receptors regulate contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation elicited by both electrical stimulation and exogenous serotonin
TLDR
The results suggest that there are functional sigma receptors on cholinergic nerve terminals or within the myenteric plexus and that these receptors can inhibit stimulated ACh release through an opioid receptor-independent mechanism.
Structural determinants of sigma receptor affinity.
TLDR
Conformational calculations for various compounds indicate a fairly wide range of tolerance for distances between the aromatic ring and the amine nitrogen, which may account for the potency at sigma receptors of structures of considerable diversity.
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