Bremazocine Recognizes the Difference in Four Amino Acid Residues to Discriminate Between a Nociceptin/Orphanin FQ Receptor and Opioid Receptors

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We investigated the molecular basis of the discrimination between nociceptin/orphanin FQ receptor (NociR) and opioid receptors (OPRs) by bremazocine, a non-type-selective opioid ligand. Construction of several chimeric receptors between NociR and κ-opioid receptor (KOPR) and mutant NociRs followed by binding experiments with [<SUP>3</SUP>H]bremazocine showed that the mutation of only four amino acid residues of NociR, Ala<SUP>216</SUP>, Val<SUP>279</SUP>, Gln<SUP>280</SUP> and Val<SUP>281</SUP>, to the amino acid residues located at the corresponding position of KOPR, Lys<SUP>227</SUP>, Ile<SUP>290</SUP>, His<SUP>291</SUP> and Ile<SUP>292</SUP>, made it possible for the resultant mutant NociR to bind bremazocine with high affinity. Considering that these four amino acid residues are conserved among μ-, δ- and κ-OPRs, the present result suggests that bremazocine recognizes the difference in these four amino acid residues to discriminate between NociR and OPRs.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 77(4), 301-306, 1998-08-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008193474
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    00215198
  • NDL 記事登録ID
    4547530
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  CJP引用  NDL  J-STAGE 
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