Chloroethylclonidine Discriminates between α1A- and α1B-Adrenoceptors in the Presence of Guanosine 5’-Triphosphate in Rabbit Thoracic Aorta

• Satoh Mitsutoshi

  Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Miyama 2-2-1, Funabashi, Chiba 274, Japan

• Kokubu Noriko

  Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Miyama 2-2-1, Funabashi, Chiba 274, Japan

• Takayanagi Issei

  Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Miyama 2-2-1, Funabashi, Chiba 274, Japan

書誌事項

タイトル別名

• Chloroethylclonidine Discriminates between .ALPHA.lA- and .ALPHA.lB-Adrenoceptors in the Presence of Guanosine 5-Triphosphate in Rabbit Thoracic Aorta.
• Chloroethylclonidine discriminates between α1A- and α1B-adrenoceptors in the presence of guanosine 5′-triphosphate in rabbit thoracic aorta

抄録

Studies on the displacement of [³H]prazosin binding by the α₁-agonist phenylephrine revealed the presence of at least high and low-affinity binding sites in membrane preparations prepared from rabbit thoracic aorta. Although the low-affinity site was reduced by the pretreatment of tissues with chloroethylclonidine, this site was unaffected by the same pretreatment of membrane preparations that did not contain the GTP analog. However, in membrane preparations with the metabolically stable GTP analog GTPγ-S (10^-5M) and single cell preparations, the low-affinity site was completely eliminated by the chloroethylclonidine pretreatment. Displacement studies with the α₁-antagonist WB4101 also revealed high- and low-affinity binding sites labeled by [³H]prazosin. Displacement curves of WB4101 obtained from membrane preparations in the presence of GTPγ-S (10^-5M) did not differ from those in the absence of GTPγ-S. These results suggest that the low affinity phenylephrine binding site labeled by [3H]prazosin was selectively bound by the chloroethylclonidine used to pretreat the tissues, membrane preparation containing GTPr-S and single cells, and that chloroethylclonidine is able to recognize these two distinct subtypes of α₁-adrenoceptors only when GTPγ-S is present.

収録刊行物

• Jpn.J.Pharmacol.

  Jpn.J.Pharmacol. 63 (1), 1-8, 1993

  公益社団法人 日本薬理学会

キーワード

• GTPγ-S
• Chloroethylclonidine
• Thoracic aorta (rabbit)

詳細情報

• CRID: 1390282679262203776
• NII論文ID: 130000840380
• NII書誌ID: AA00691188
• DOI: 10.1254/jjp.63.1
• COI: 1:CAS:528:DyaK2cXktlQ%3D
• ISSN: 13473506
• ISSN: 00215198
• PubMed: 7903716
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819359670?httpAccept=text/xml
• Web Site: https://api.elsevier.com/content/article/PII:S0021519819359670?httpAccept=text/plain
• Web Site: https://search.jamas.or.jp/link/ui/1995089252
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可