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

• Yamagishi Hisako

  Department of Pharmacology, Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan Department of Oral Health Science Center,Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan

• Watanabe Masahito

  Department of Pharmacology, Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan Environment & Safety Research Department,Research & Development Division,Nihon Bayer Agrochem K.K.,Yuki Research Center,9511-4,Yuki,Yuki-shi,Ibaraki 307-0001,Japan

• Yazaki Kinya

  Department of Pharmacology, Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan Department of Oral Health Science Center,Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan

• Sawaki Kohei

  Department of Pharmacology, Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan Department of Oral Health Science Center,Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan

• Kawaguchi Mitsuru

  Department of Pharmacology, Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan Department of Oral Health Science Center,Tokyo Dental College,1-2-2 Masago,Mihamaku,Chiba 261-8502,Japan

抄録

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 [³H]PK14105(1-(2-fluoro-5-nitrophenyl)-3-isoquinolinecarboxylic acid).[³H]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[³H]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[³H]PK14105 binding to rat parotid gland membranes, without changing the density.The photoaffinity labeling with[³H]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[³H]PK14105 in salivary glands of rat, mouse, rabbit and human.

収録刊行物

• Jpn.J.Pharmacol.

  Jpn.J.Pharmacol. 82 (2), 110-115, 2000

  公益社団法人 日本薬理学会

キーワード

• Peripheral type benzodiazepine receptor
• Salivary gland
• Photoaffinity labeling
• [<SUP>3</SUP>H]PK14105

詳細情報

• CRID: 1390001204286870656
• NII論文ID: 10008183011
• NII書誌ID: AA00691188
• DOI: 10.1254/jjp.82.110
• COI: 1:CAS:528:DC%2BD3cXhsVOgtbs%3D
• ISSN: 13473506
• ISSN: 00215198
• NDL書誌ID: 5283884
• PubMed: 10877528
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I5283884
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819307048?httpAccept=text/xml
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819307048?httpAccept=text/plain
• Web Site: https://www.jstage.jst.go.jp/article/jjp/82/2/82_2_110/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2000141027
• 本文言語コード: en
• データソース種別:
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