PD-137889
PD-137889 | |
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IUPAC名 (4aR)-N-Methyl-1,2,3,4,9,9a-hexahydro-4aH-fluoren-4a-amine | |
識別 | |
CAS號 | 95372-93-3 ![]() 147128-60-7(rel-(4aR,9aS)) ![]() |
PubChem | 10104280 |
ChemSpider | 8279807 |
SMILES |
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InChI |
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InChIKey | KQLIVVYSTDBTMZ-UHFFFAOYSA-N |
性質 | |
化學式 | C14H19N |
摩爾質量 | 201.31 g·mol−1 |
若非註明,所有數據均出自標準狀態(25 ℃,100 kPa)下。 |
PD-137889(N-甲基六氫芴胺)是一種化學化合物,中樞神經系統NMDA受體拮抗劑,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]
參考
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ Polycyclic amine derivatives useful as cerebrovascular agents (頁面存檔備份,存於互聯網檔案館) United States Patent; Coughenour, et al. Family ID: 22686445 Appl. #07/186,834
- ^ [3H]N-[1-(2-thienyl)cyclohex-yl]piperidine