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]
Quick Facts PD-137889, 識別 ...
PD-137889
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IUPAC名 (4aR)-N-Methyl-1,2,3,4,9,9a-hexahydro-4aH-fluoren-4a-amine
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識別
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CAS號
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95372-93-3 Y 147128-60-7(rel-(4aR,9aS)) Y
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PubChem
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10104280
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ChemSpider
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8279807
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SMILES
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- c12c(cccc1)C3(NC)CCCCC3C2
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InChI
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- 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
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InChIKey
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KQLIVVYSTDBTMZ-UHFFFAOYSA-N
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性質
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化學式
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C14H19N
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摩爾質量
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201.31 g·mol−1
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若非註明,所有數據均出自標準狀態(25 ℃,100 kPa)下。
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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.
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.
[3H]N-[1-(2-thienyl)cyclohex-yl]piperidine