医薬品設計
出典: フリー百科事典『ウィキペディア（Wikipedia）』 (2024/04/08 09:26 UTC 版)
医薬品設計（いやくひんせっけい、英: Drug design; ドラッグデザイン）とは、生物学的標的の知識に基づいて新しい薬物を見出す創意に富んだ手法である[1]。しばしば合理的医薬品設計または単に合理的設計とも呼ばれる。薬物は、タンパク質などの生体分子の機能を活性化または阻害する有機低分子が最も一般的であり、これにより患者に治療効果をもたらす。最も基本的な意味での医薬品設計は、相互作用する生体分子標的と相補的な形状と電荷を持ち、標的に結合する分子を設計することを含む。その他にも、通常の経路を強化するために、病気の場合に影響を受けているであろう特定の分子の働きを促進する方法もある。
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[続きの解説]
「医薬品設計」の続きの解説一覧
医薬品設計
出典: フリー百科事典『ウィキペディア（Wikipedia）』 (2022/07/06 06:23 UTC 版)
nAChRに影響を与える薬物には、作動薬、部分作動薬、遮断薬がある。ニコチン等の作動薬は、nAChRに暫くの間（濃度やnAChRサブタイプによって数秒から数分）接触すると脱分極剤として作用するが、作動薬に慢性的に接触すると、急速かつ持続的な脱感作が起こり、長期的な機能停止に陥る事もある。部分的nAChR作動薬は、禁煙に役立つと思われるので研究されている。部分作動薬は、nAChRに結合し、作動薬よりも少量のドーパミンの放出を刺激する事で、ニコチンの不在を補うと考えられている。ニコチン作動薬の中には、特異性がないものがある事はよく知られており、nAChRの特定のサブタイプを標的とする必要がある病気の治療に使用する際に問題となる可能性がある。これらの非特異的な作動薬には、例えばアセチルコリン、ニコチン、エピバチジン等があり、いずれも複数のサブタイプのnAChRを標的としている。
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