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YM 90K hydrochloride

Names

[ CAS No. ]:
154164-30-4

[ Name ]:
YM 90K hydrochloride

[Synonym ]:
N-Acetyltryptamine
C11H7N5O4
YM 90K
ym 900
2,3-Quinoxalinedione, 1,4-dihydro-6-(1H-imidazol-1-yl)-7-nitro-, hydrochloride (1:1)
6-(1H-Imidazol-1-yl)-7-nitro-1,4-dihydro-2,3-quinoxalinedione hydrochloride (1:1)

Biological Activity

[Description]:

YM90K is a potent and selective AMPA receptor antagonist with a Ki of 84 nM. YM90K is less potent in inhibiting kainate (Ki of 2.2 μM) and NMDA (Ki of 37 μM) receptors. YM90K has neuroprotective actions[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR
Research Areas >> Neurological Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

Ki: 84 nM (AMPA receptor), 2.2 μM (Kainate receptor) and 37 μM (NMDA receptor)[1]


[In Vitro]

YM90K (30 nmol) co-injected with AMPA or kainate into the rat striatum protected cholinergic neurons against AMPA- or kainate-induced neurotoxicity[1].

[In Vivo]

YM90K showes potent suppressive activity against audiogenic seizure in DBA/2 mice; ED50 values of YM90K against tonic seizure is 2.54 mg/kg (i.p.). The duration of the anticonvulsant effects of YM90K is 30 min[1]. In a global ischemia model, YM90K (15 mg/kg i.p. x 3) significantly prevents the delayed neuronal death in the hippocampal CA1 region in Mongolian gerbils when administered 1 h after 5-min ischemia. The therapeutic time window for the neuroprotective effect of YM90K (30 mg/kg i.p. x 3) is 6 h[1]. In a focal ischemia model, YM90K (30 mg/kg i.v. bolus+10 mg/kg/h for 4 h) reduces the volume of ischemic damage in the cerebral cortex in F344 rats[1].

[References]

[1]. M Shimizu-Sasamata, et al. YM90K: pharmacological characterization as a selective and potent alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainate receptor antagonist. J Pharmacol Exp Ther. 1996 Jan;276(1):84-92.

Chemical & Physical Properties

[ Boiling Point ]:
556.6ºC at 760mmHg

[ Molecular Formula ]:
C11H8ClN5O4

[ Molecular Weight ]:
309.665

[ Flash Point ]:
290.4ºC

[ Exact Mass ]:
309.026489

[ PSA ]:
129.36000

[ LogP ]:
1.63550

[ Index of Refraction ]:
1.84

Related Compounds