Pharmacological Characterization of an 18-kDa Protein Associated With the Peripheral-Type Benzodiazepine Receptor in Salivary Glands

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Pharmacological characterization of peripheral type benzodiazepine receptors in rat, rabbit, mouse and human salivary glands was determined by receptor binding and photoaffinity labeling analysis using [<SUP>3</SUP>H]PK14105(1-(2-fluoro-5-nitrophenyl)-3-isoquinolinecarboxylic acid).[<SUP>3</SUP>H]PK14105 bound to the membranes of salivary glands in rats, rabbits, mice and humans with high affinity at the nanomolar level.The rank order of receptor density in submandibular glands among several species was as follows:human≥rat≥mouse>rabbit.Competitive potency of receptor ligands against[<SUP>3</SUP>H]PK14105 was as follows:PK11195≥Ro5-4864>deazepam>clonazepam>Ro15-1788.The rank order of potency against calcium channel ligands and co-transport inhibitors was as follows:nitrendipine>BAY K 8644>bumetanide>furosemide.Pretreatment with nitrendipine or BAY K 8644 decreased the affinity of[<SUP>3</SUP>H]PK14105 binding to rat parotid gland membranes, without changing the density.The photoaffinity labeling with[<SUP>3</SUP>H]PK14105 indicated the presence of the 18-kDa protein in all salivary glands of our experiment.The inhibition of photolabeling by some receptor ligands was the same results as the receptor binding assay.In conclusion, the peripheral type benzodiazepine receptors include the 18-kDa protein photolabeled with[<SUP>3</SUP>H]PK14105 in salivary glands of rat, mouse, rabbit and human.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 82(2), 110-115, 2000-02-01

    公益社団法人 日本薬理学会

参考文献:  19件中 1-19件 を表示

被引用文献:  3件中 1-3件 を表示

各種コード

  • NII論文ID(NAID)
    10008183011
  • 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
    5283884
  • 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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