Effects of Ketanserin and 3-[2-[4-(o-Methoxyphenyl)-1-piperazinyl]ethyl]-2,4(1H, 3H)-quinazolinedione Monohydrochloride (SGB-1534), Anti-hypertensive Agents, on ^3H-Serotonin and ^3H^Ketanserin Bindings to Serotonergic (5HT_1 and 5HT_2) Receptors in Dog B

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概要

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• Serotonin has an important role in the control of blood pressure, because serotonin_2 (5HT_2) antagonists ameliorate hypertension. The 5HT_2 antagonistic action may be due in part to α_1-adrenoceptor blocking action. Thus, the presetn study was designed to examine the effects of 5HT_2 antagonists (ketanserin and cinanserin) and α_1-antagonists (SGB-1534,3-[2-[4-(o-methoxyphenyl)-1-piperazinyl]ethyl]-2,4(1H, 3H)-quinazolinedione monohydrochloride, and prazosin) on the ^3H-5-hydroxytryptamine creatine sulfate (^3H-serotonin) and ^3H-ketanserin bindings to serotonin_1 (5HT_1) receptors in the dog brain and 5HT_2 receptors in the dog brain and aora by using the radioligand binding assay method. The existence of ^3H-ketanserin binding sites was definitely observed in the dog brain and aorta. The K_d and B_<max> values of ^3H-ketanserin binding to 5HT_2 receptors in the dog aorta were 1.20 nM and 36 fmol/mg protein, respectively. 5HT_1 and 5HT_2 receptors also existed in the dog brain. Inhibition of ^3H-ketanserin bindings by ketanserin and cinanserin in the dog brain and aorta was observed at very low concentrations, but inhibition by SGB-1534 and prazosin was observed only at very high concentrations. Furthermore, inhibitions of ^3H-serotonin binding by ketanserin and prazosin were observed at high concentrations, but the K_i value of SGB-1534 was found to be 371 nM, These results suggest that 5HT_2 antagonists and α_1 adrenoceptor antagonists have different effects on the ^3H-ketanserin bindings to 5HT_2 receptors in the aorta and that hypotensive effect of 5HT_2 antagonists may be largely concerned with 5HT_2 receptors. On the other hand, that of α_1-antagonists may be due to α_1-adrenoceptor blocking action in vascular tissues as described previously.

• 社団法人日本薬学会の論文
• 1988-08-25

著者

• 中村 隆志

  新潟薬大薬理

• 長友 孝文

  Department of Pharmacology, Niigata College of Pharmacy

• 土橋 洋史

  Department of Pharmacology, Niigata College of Pharmacy

• 長友 孝文

  新潟薬科大学薬学部薬理学教室

• 土橋 洋史

  ひまわり薬局

• 土橋 洋史

  新潟薬科大学 薬理学教室

• 伯耆原 玲

  Department of Pharmacology, Niigata College of Pharmacy

• 田中 裕子

  Department of Pharmacology, Niigata College of Pharmacy

• 中村 隆史

  Department of Pharmacology, Niigata College of Pharmacy

• 青野 遵一郎

  Department of Pharmacology, Niigata College of Pharmacy

• 長友 孝文

  新潟薬科大学・薬・薬理

• 田中 裕子

  Department Of Pharmacology Niigata College Of Pharmacy

• 長友 孝文

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• 伯耆原 玲

  Department Of Pharmacology Niigata College Of Pharmacy

• 青野 遵一郎

  Department Of Pharmacology Niigata College Of Pharmacy

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