L-689,560 Struktur

L-689,560

Bezeichnung:L-689,560

CAS-Nr139051-78-8

Englisch Name:L-689,560

CBNumberCB9236350

SummenformelC17H15Cl2N3O3

Molgewicht380.23

MOL-Datei139051-78-8.mol

L-689,560 physikalisch-chemischer Eigenschaften

Schmelzpunkt	172-173°C
Siedepunkt	549.1±50.0 °C(Predicted)
Dichte	1.51±0.1 g/cm3(Predicted)
storage temp.	Store at RT
Löslichkeit	<9.51mg/ml in DMSO; <38.02mg/ml in ethanol
Aggregatzustand	solid
pka	11.16±0.20(Predicted)
Farbe	White

L-689,560 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
L-689,560 is a potent antagonist at the glycine-NMDA receptor site.
Definition
ChEBI: 4-[[anilino(oxo)methyl]amino]-5,7-dichloro-1,2,3,4-tetrahydroquinoline-2-carboxylic acid is a member of quinolines.
Biologische Aktivität
Very potent antagonist at the glycine-NMDA site. Also available as part of the NMDA Receptor - Glycine Site Tocriset™ .
in vitro
l-689560 is described as one of the most potent nmda antagonists and [4'-3h]-l-689560 has been thought to be a highly specific radioligand for the glycine site. in consistent with the 5,7-disubstituted kynurenates, the tetrahydroquinolines are selective antagonists of glycine site nmda, l-689560 exhibiting at least 3 orders of magnitude selectivity versus the glutamate site [1].
in vivo
mdl100748 with an ed50 of 83 mg kg-1 can prevent audiogenic seizures in susceptible mice after systemic injection. as a standard l689560, its subsequent analogues have been compared; the displacement of [3h] l689560 has often been used to displace that of [3h] glycine as an alternative assay. l701252, a quinones (the retention of a keto grouping at position 3), has been against l689560 binding (ic50 of 420 nm) and against seizures (ed50 of 4.1 mg kg-1) in dba/2 mice. a group of sulfonamide analogues of kynurenic acid are also in active among the 2-quinolone series. those of a series of 3,4-dihydroquinolones and tetrahydroquinolines with a nitrosubstituent at 3-position were selective antagonists at the nmda receptor glycine site if they bore a bulky grouping in the position 4. the compound with no substitution at position 4 was proved to be one of the most effective broad-spectrum antagonists against nmda and ampa receptors [2].
Lager
Store at RT
Einzelnachweise
[1]. leeson pd, carling rw, moore kw, moseley am, smith jd, stevenson g, chan t, baker r, foster ac, grimwood s, et al. 4-amido-2-carboxytetrahydroquinolines. structure-activity relationships for antagonism at the glycine site of the nmda receptor. j med chem. 1992 may 29;35 (11): 1954-68.
[2]. stone tw. development and therapeutic potential of kynurenic acid and kynurenine derivatives for neuroprotection. trends pharmacol sci. 2000 apr; 21(4):149-54.

L-689,560 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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