AS-8112
AS-8112 is a synthetic compound that acts as a selective antagonist at the dopamine receptor subtypes D2 and D3, and the serotonin receptor 5-HT3.[1] It has potent antiemetic effects in animal studies and has been investigated for potential medical use.[2][3]
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Preferred IUPAC name
5-Bromo-N-[(6R)-1-ethyl-4-methyl-1,4-diazepan-6-yl]-2-methoxy-4-(methylamino)benzamide | |
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Chemical formula |
C17H27BrN4O2 |
Molar mass | 399.325 g/mol |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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References
- Yoshikawa T, Yoshida N, Oka M (May 2001). "The broad-spectrum anti-emetic activity of AS-8112, a novel dopamine D2, D3 and 5-HT3 receptors antagonist". British Journal of Pharmacology. 133 (2): 253–60. doi:10.1038/sj.bjp.0704078. PMC 1572785. PMID 11350861.
- Yoshikawa T, Yoshida N, Oka M (November 2001). "Central antiemetic effects of AS-8112, a dopamine D2, D3, and 5-HT(3) receptor antagonist, in ferrets". European Journal of Pharmacology. 431 (3): 361–4. doi:10.1016/S0014-2999(01)01459-5. PMID 11730730.
- Hirokawa Y, Fujiwara I, Suzuki K, Harada H, Yoshikawa T, Yoshida N, Kato S (February 2003). "Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity". Journal of Medicinal Chemistry. 46 (5): 702–15. doi:10.1021/jm020270n. PMID 12593651.
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5-HT2 |
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