Blockade of U50,488H analgesia by antisense oligodeoxynucleotides to a κ-opioid receptor Journal Article

  


Authors: Chien, C. C.; Brown, G.; Pan, Y. X.; Pasternak, G. W.
Article Title: Blockade of U50,488H analgesia by antisense oligodeoxynucleotides to a κ-opioid receptor
Abstract: The recently cloned κ-opioid receptor has binding characteristics consistent with those of a κ1-opioid receptor. Repeated intrathecal administration of an antisense oligodeoxynucleotide against the κ1-opioid receptor selectively lowers U50,488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetemide) analgesia (P < 0.02) without affecting μ or δ analgesia. A mismatched antisense oligodeoxynucleotide in which 4 bases had been switched is inactive against U50,488H analgesia. These studies confirm at the molecular level traditional pharmacological studies implying a distinct receptor mechanisms for κ1 analgesia and demonstrate the utility of antisense approaches in studies of opioid pharmacology. © 1994.
Keywords: controlled study; nonhuman; mouse; animal; animal experiment; molecular cloning; drug antagonism; molecular sequence data; base sequence; binding sites; analgesics; analgesia; mu opiate receptor; receptors, opioid, mu; injections, spinal; enkephalin[2,5 dextro penicillamine]; oligonucleotides, antisense; pyrrolidines; delta opiate receptor; receptor subtype; receptors, opioid, delta; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; kappa opiate receptor; opioid analgesia; antisense oligodeoxynucleotide; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; guinea pigs; male; priority journal; article; receptors, opioid, kappa; κ-opioid receptor; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; enkephalins; 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-isomer; enkephalin, d-penicillamine (2,5)-; intrathecal drug administration
Journal Title: European Journal of Pharmacology
Volume: 253
Issue: 3
ISSN: 0014-2999
Publisher: Elsevier B.V.  
Date Published: 1994-03-03
Start Page: R7
End Page: R8
Language: English
DOI: 10.1016/0014-2999(94)90209-7
PROVIDER: scopus
PUBMED: 8200413
DOI/URL:

https://www.scopus.com/inward/record.uri?eid=2-s2.0-0028207063&doi=10.1016%2f0014-2999%2894%2990209-7&partnerID=40&md5=1f7df49f8523e7bcc119b54d148f7be0
Notes: Export Date: 14 January 2019 -- Article -- Source: Scopus
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MSK Authors
  1. Yingxian Pan
    132 Pan
  2. Gavril W Pasternak
    414 Pasternak
  3. George P. Brown
    16 Brown
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