VUF6990 | 1225033-19-1

• 英文名称: VUF6990
• CAS: 1225033-19-1
• 化学式: C₁₂H₁₈N₆
• 分子量: 246.315
• InChiKey: MSBFIVNLDFBBPJ-UHFFFAOYSA-N

反应信息

• 作为产物：
  描述：

  环丙基甲胺 、 N-cyano-N'-<3-(imidazol-4-yl)propyl>-S-methylisothiourea 反应 0.5h， 以23%的产率得到VUF6990
  参考文献：
  名称：

  Inhibition of brain [3H]cimetidine binding by improgan-like antinociceptive drugs

  摘要：

  [H-3]cimetidine, a radiolabeled histamine H-2 receptor antagonist, binds with high affinity to an unknown hemoprotein in the brain which is not the histamine H-2 receptor. Improgan, a close chemical congener of cimetidine, is a highly effective pain-relieving drug following CNS administration, yet its mechanism of action remains unknown. To test the hypothesis that the [H-3]cimetidine-binding site is the improgan antinociceptive target, improgan, cimetidine, and 8 other chemical congeners were studied as potential inhibitors of [H-3]cimetidine binding in membrane fractions from the rat brain. All compounds produced a concentration-dependent inhibition of [H-3]cimetidine binding over a 500-fold range of potencies (K-i values were 14.5 to >8000 nM). However, antinociceptive potencies in rats did not significantly correlate with [H-3] cimetidine-binding affinities (r=0.018, p=0.97, n=10). These results suggest that the [H-3]cimetidine-binding site is not the analgesic target for improgan-like drugs. (C) 2010 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.ejphar.2010.01.026