PD-137889
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| Nazivi | |
|---|---|
| IUPAC naziv
(4aR)-N-Metil-1,2,3,4,9,9a-heksahidro-4aH-fluoren-4a-amin
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| Identifikacija | |
3D model (Jmol)
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| ChemSpider | |
| UNII | |
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| Svojstva | |
| C14H19N | |
| Molarna masa | 201,31 g·mol−1 |
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa). | |
| Reference infokutije | |
PD-137889 (N-metilheksahidrofluorenamin) je hemijsko jedinjenje koje je aktivno kao antagonist NMDA receptora u centralnom nervnom sistemu sa oko 30 puta većom pontentnošću od „glavnog predstavnika” svoje klase, ketamina,[3] i koristi se kao zamena za fenciklidin u studijama na životinjama.[4][5][6] Ki [3H]TCP[а] vezivanje = 27 nM u odnosu na ketamin sa Ki = 860 nM.[7]
Napomene
[уреди | уреди извор]- ^ [3H]N-[1-(2-tienil)cikloheks-il]piperidin
Reference
[уреди | уреди извор]- ^ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today. 15 (23-24): 1052—7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.
- ^ Evan E. Bolton; Yanli Wang; Paul A. Thiessen; Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry. 4: 217—241. doi:10.1016/S1574-1400(08)00012-1.
- ^ 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 (1993). „Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor”. J Med Chem. 36 (6): 654—70. PMID 8459395. doi:10.1021/jm00058a002.
- ^ Nicholson, Katherine L.; Balster, Robert L. (2003). „Evaluation of the phencyclidine-like discriminative stimulus effects of novel NMDA channel blockers in rats”. Psychopharmacology. 170 (2): 215—224. PMID 2851738. S2CID 30803162. doi:10.1007/s00213-003-1527-6.
- ^ Bigge, Christopher F. (1993). „Structural requirements for the development of potent n-methyl-d-aspartic acid (NMDA) receptor antagonists”. Biochemical Pharmacology. 45 (8): 1547—1561. PMID 7683469. doi:10.1016/0006-2952(93)90294-7.
- ^ Bigge, Christopher F.; Malone, Thomas C. (1993). „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. 3 (7): 951—989. doi:10.1517/13543776.3.7.951.
- ^ Polycyclic amine derivatives useful as cerebrovascular agents Архивирано на сајту Wayback Machine (3. фебруар 2018) United States Patent; Coughenour, et al. Family ID: 22686445 Appl. #07/186,834
