PD-137889

PD-137889
IUPAC名
(4aR)-N-Methyl-1,2,3,4,9,9a-hexahydro-4aH-fluoren-4a-amine
识别
CAS号 95372-93-3  checkY
147128-60-7（rel-(4aR,9aS)）  checkY
PubChem 10104280
ChemSpider 8279807
SMILES
 
  • c12c(cccc1)C3(NC)CCCCC3C2
InChI
 
  • 1S/C14H19N/c1-15-14-9-5-4-7-12(14)10-11-6-2-3-8-13(11)14/h2-3,6,8,12,15H,4-5,7,9-10H2,1H3
InChIKey KQLIVVYSTDBTMZ-UHFFFAOYSA-N
性质
化学式 C14H19N
摩尔质量 201.31 g·mol−1
若非注明，所有数据均出自标准状态（25 ℃，100 kPa）下。

PD-137889（N-甲基六氢芴胺）是一種化學化合物，中枢神经系统NMDA受体拮抗剂，效力比氯胺酮強約30倍[1]，動物研究中可替代五氯苯酚。[2][3][4]Ki[3H]TCP[a] = 27 nM，氯胺酮Ki = 860 nM。 [5]

参考

  1. ^ Hays, Sheryl J.; Novak, Perry M.; Ortwine, Daniel F.; Bigge, Christopher F.; Colbry, Norman L.; Johnson, Graham; Lescosky, Leonard J.; Malone, Thomas C.; Michael, Andre. Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor. J Med Chem. 1993, 36 (6): 654–70. PMID 8459395. doi:10.1021/jm00058a002. 
  2. ^ Nicholson, Katherine L.; Balster, Robert L. Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats. Psychopharmacology. 2003, 170 (2): 215–224. PMID 2851738. S2CID 30803162. doi:10.1007/s00213-003-1527-6. 
  3. ^ Bigge, Christopher F. Structural requirements for the development of potent n-methyl-d-aspartic acid (NMDA) receptor antagonists. Biochemical Pharmacology. 1993, 45 (8): 1547–1561. PMID 7683469. doi:10.1016/0006-2952(93)90294-7. 
  4. ^ Bigge, Christopher F.; Malone, Thomas C. Overview: Agonists, Antagonists and Modulators of the N-methyl-D-aspartic acid (NMDA) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) Subtypes of Glutamate Receptors. Current Opinion on Therapeutic Patents. 1993, 3 (7): 951–989. doi:10.1517/13543776.3.7.951. 
  5. ^ Polycyclic amine derivatives useful as cerebrovascular agents （页面存档备份，存于互联网档案馆） United States Patent; Coughenour, et al. Family ID: 22686445 Appl. #07/186,834
  1. ^ [3H]N-[1-(2-thienyl)cyclohex-yl]piperidine