Enhanced κ-opioid receptor-mediated analgesia by antisense targeting the σ(1) receptor Journal Article

  


Authors: King, M.; Pan, Y. X.; Mei, J.; Chang, A.; Xu, J.; Pasternak, G. W.
Article Title: Enhanced κ-opioid receptor-mediated analgesia by antisense targeting the σ(1) receptor
Abstract: In the current study, we used an antisense oligodeoxynucleotide targeting the recently cloned σ1 receptor to assess its functions within the nervous system. σ1 antagonists potentiate the analgesic actions of opioids. Similarly, the antisense probe targeting the σ1 receptor enhanced the analgesic activity of the κ1-opioid receptor agonist U50,488H (trans-3,4-dichloro-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeacetamidel) and the κ3-opioid receptor agonist naloxone benzoylhydrazone. A mismatch control was inactive. These results confirm the role of σ1 receptors in an anti-opioid analgesic system and illustrate the utility of antisense approaches towards the elucidation of σ receptor functions.
Keywords: controlled study; nonhuman; mouse; animals; mice; animal experiment; molecular sequence data; short survey; analgesics; opioid; drug sensitivity; analgesia; naloxone; opiate receptor; analgesic activity; oligonucleotides, antisense; pyrrolidines; receptor subtype; receptors, opioid, delta; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; naloxone benzoylhydrazone; kappa opiate receptor; antisense oligodeoxynucleotide; narcotic antagonists; subcutaneous drug administration; intracerebroventricular drug administration; male; priority journal; receptors, opioid, kappa; sigma opiate receptor; 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-isomer; σ receptor
Journal Title: European Journal of Pharmacology
Volume: 331
Issue: 1
ISSN: 0014-2999
Publisher: Elsevier B.V.  
Date Published: 1997-07-16
Start Page: R5
End Page: R6
Language: English
DOI: 10.1016/s0014-2999(97)01064-9
PUBMED: 9274937
PROVIDER: scopus
DOI/URL:

https://www.scopus.com/inward/record.uri?eid=2-s2.0-0030814282&doi=10.1016%2fS0014-2999%2897%2901064-9&partnerID=40&md5=b57d17e06ba1ad1386b024029f9d4904
Notes: Short Survey -- Export Date: 17 March 2017 -- Source: Scopus
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MSK Authors
  1. Michael A King
    24 King
  2. Yingxian Pan
    132 Pan
  3. Gavril W Pasternak
    414 Pasternak
  4. Albert H Chang
    19 Chang
  5. Jianfeng Mei
    5 Mei
  6. Jin Xu
    60 Xu
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