非ペプチドアルギニン・バソプレシン・アンタゴニスト:ヴァプタンス
Guy Decaux1, Alain Soupart, Gilbert Vassart
1Department of Internal Medicine, Erasmus University Hospital, Brussels, Belgium. guy.decaux@skynet.be
Lancet (London, England)
|May 13, 2008
まとめ
Vaptansは,V1a,V1b,V2受容体を標的にする新しいバソプレシン受容体対抗剤です. これらの薬は,低血圧症,精神疾患,血管疾患などの疾患の治療に有望であることが示されています.
科学分野:
- 内分泌学と薬理学について
- Gタンパク質結合受容体の研究
背景:
- アルギニン=バソプレシンは,循環器と水のホメオスタシスに不可欠です.
- ヴァソプレシン受容体 (V1a,V1b,V2) は,Gタンパク質結合受容体ファミリーに属しています.
研究 の 目的:
- ヴァソプレシン受容体アンタゴニスト (ヴァプタン) の開発と治療の可能性をレビューする.
- 異なるヴァプタンの選択的および非選択的行動を強調する.
主な方法:
- バプタンに関する薬理学的データのレビュー.
- 選択的および非選択的バソプレシン受容体抗剤の臨床応用に関する分析.
主要な成果:
- 選択的V1aアンタゴニスト (例えば,レルコバプタン) は,レイノード病,不妊症,トコリスの治療に潜在力を示しています.
- セレクティブV1bアンタゴニスト (SSR-149415など) は,精神疾患に有益である可能性があります.
- V2アンタゴニスト (例えば,トルバプトン) は,低血圧性尿路症を誘発することによって,低血圧症を効果的に治療します.
- 非選択的V1a/V2抗体 (例えばコニバプトン) は,低血圧症の治療に承認されています.
結論:
- Vaptansは,バソプレシン受容体のサブタイプを標的とした重要な進歩を表しています.
- 異なるヴァプタンには,さまざまな疾患に対する標的の治療戦略があります.
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