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Aprepitant CAS# 170729-80-3 阿瑞吡坦

Aprepitant is a small molecule, high-affinity substance P antagonist (SPA) with antiemetic activity. Crossing the blood brain barrier, aprepitant binds selectively to the human substance P/neurokinin 1 receptor in the central nervous system (CNS), thereby inhibiting receptor binding of endogenous substance P and substance P-induced emesis. This agent has little or no affinity for serotonin type 3 (5-HT3), dopamine, and corticosteroid receptors.
📌 参考资料/链接:
Brands, Karel M. J.; Payack, Joseph F.; Rosen, Jonathan D.; Nelson, Todd D.; Candelario, Alexander; Huffman, Mark A.; Zhao, Matthew M.; Li, Jing; Craig, Bridgette; Song, Zhiguo J.; Tschaen, David M.; Hansen, Karl; Devine, Paul N.; Pye, Philip J.; Rossen, Kai; Dormer, Peter G.; Reamer, Robert A.; Welch, Christopher J.; Mathre, David J.; Tsou, Nancy N.; McNamara, James M.; Reider, Paul J.Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation. Journal of the American Chemical Society. Volume 125. Issue 8. Pages 2129-2135. 2003.

📄 详细内容

CAS No. 170729-80-3 阿瑞吡坦Aprepitant synthetic routes


Brands, Karel M. J.; Payack, Joseph F.; Rosen, Jonathan D.; Nelson, Todd D.; Candelario, Alexander; Huffman, Mark A.; Zhao, Matthew M.; Li, Jing; Craig, Bridgette; Song, Zhiguo J.; Tschaen, David M.; Hansen, Karl; Devine, Paul N.; Pye, Philip J.; Rossen, Kai; Dormer, Peter G.; Reamer, Robert A.; Welch, Christopher J.; Mathre, David J.; Tsou, Nancy N.; McNamara, James M.; Reider, Paul J.Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation. Journal of the American Chemical Society. Volume 125. Issue 8. Pages 2129-2135. 2003.
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