Diversity of Thyrotropin-Releasing Hormone Receptors in the Pituitaryand Discrete Brain Regions of Rats

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In order to analyze the receptor properties of central nervous system (CNS)-stimulant thyrotropin-releasing hormone (L-pyroglutamyl-L-histidyl-L-prolinamide, TRH), we evaluated the binding of TRH and its analog taltirelin hydrate ((-)-<I>N</I>-[(<I>S</I>)-hexahydro-1-methyl-2, 6-dioxo-4-pyrimidinylcarbonyl]-L-histidyl-L-prolinamide tetrahydrate; taltirelin, TA-0910) in rat anterior pituitary and several brain regions. There was a specific binding of [<SUP>3</SUP>H]methyl TRH (MeTRH) in the anterior pituitary, hypothalamus, brain stem, cerebral cortex and cerebellum with K<SUB>d</SUB> values of 1.0 - 1.6 nM. The inhibition of [<SUP>3</SUP>H]MeTRH binding by TRH and taltirelin was monophasic in the anterior pituitary, hypothalamus and brain stem with K<SUB>i</SUB> values of 6.3 - 8.0 nM and 145.5 - 170.4 nM for TRH and taltirelin, respectively. In contrast, the biphasic inhibition was revealed in the cerebral cortex and cerebellum. The K<SUB>i</SUB> values for TRH and taltirelin were 4.1 - 4.3 nM and 67.8 - 73.4 nM for the high affinity binding site and 3.6 - 4.2 μM and 82.3 - 197.5 μM for the low affinity binding site, respectively. Addition of 100 μM GTP or its analog 5′-guanylylimidodiphosphate (Gpp[NH]p) affected neither the biphasic inhibition by TRH nor that by taltirelin. Thus the results suggest the presence of distinct high and low affinity TRH receptors in the CNS in contrast to the pituitary.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 79(3), 313-317, 1999-03-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008682784
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    REV
  • ISSN
    00215198
  • NDL 記事登録ID
    4699235
  • 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  NDL  J-STAGE 
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