Jump to content

AS-8112

From Wikipedia, the free encyclopedia
The printable version is no longer supported and may have rendering errors. Please update your browser bookmarks and please use the default browser print function instead.
AS-8112
Names
Preferred IUPAC name
5-Bromo-N-[(6R)-1-ethyl-4-methyl-1,4-diazepan-6-yl]-2-methoxy-4-(methylamino)benzamide
Identifiers
3D model (JSmol)
ChemSpider
DrugBank
  • InChI=1S/C17H27BrN4O2/c1-5-22-7-6-21(3)10-12(11-22)20-17(23)13-8-14(18)15(19-2)9-16(13)24-4/h8-9,12,19H,5-7,10-11H2,1-4H3,(H,20,23)/t12-/m1/s1 checkY
    Key: DALSFUWTAOKVTF-GFCCVEGCSA-N checkY
  • CCN2CCN(C)CC(C2)NC(=O)c1cc(Br)c(NC)cc1OC
  • CCN1CCN(CC(C1)NC(=O)c2cc(c(cc2OC)NC)Br)C
Properties
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).
checkY verify (what is checkY☒N ?)

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]

References

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.