MibaMpator
MibaMpator Basic information
- Product Name:
- MibaMpator
- Synonyms:
-
- MIBAMPATOR;LY 451395;LY-451395
- CS-1234
- MibaMpator
- [(2R)-2-[4-[4-[2-[(Methylsulfonyl)amino]ethyl]phenyl]phenyl]propyl][(1-methylethyl)sulfonyl]amine
- LY 451395
- 2-Propanesulfonamide, N-[(2R)-2-[4'-[2-[(methylsulfonyl)amino]ethyl][1,1'-biphenyl]-4-yl]propyl]-
- Mibampator?(LY451395)
- (R)-N-(2-(4'-(2-(Methylsulfonamido)ethyl)-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonamide
- CAS:
- 375345-95-2
- MF:
- C21H30N2O4S2
- MW:
- 438.6
- Mol File:
- 375345-95-2.mol
MibaMpator Chemical Properties
- Boiling point:
- 609.4±65.0 °C(Predicted)
- Density
- 1.205±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 11.05±0.40(Predicted)
- color
- White to off-white
MibaMpator Usage And Synthesis
Uses
Mibampator (LY451395) is a potent and highly selective potentiator of the AMPA receptors.
Biological Activity
ly451395 (mibampator) is a powerful, highly selective and biarylsulfonamide potentiator of ampa receptors [1].ly451395 (mibampator) has been found to be a potent, selective and centrally active positive allosteric modulators of ampa receptor-mediated neurotransmission, which enhances ion channel flux in the presence of agonist by inhibiting desensitization and deactivation of the receptors. in addition, ly451395 has been revealed to enhance synaptic transmission. besides, ly451395 has been reported to attenuate the response to acute ethanol administration in the rat in vivo [1]. moreover, the in vivo metabolisms of ly451395 in mouse, rat, dog and human have produced several phase 1 oxidative metabolites [2].
in vivo
Incubation of Mibampator (LY451395) with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies of the preclinical species [1]. LY404187 and Mibampator (LY451395) reverses the central effects of an acutely intoxicating dose of ethanol in the rat. Mibampator (LY451395) significantly and dose-dependently reversed ethanol-induced deficits in both motor coordination and disruptions in an operant task where animals were trained to press a lever for food reward [2].
References
[1] jones n1, messenger mj, o'neill mj, oldershaw a, gilmour g, simmons rm, iyengar s, libri v, tricklebank m, williams sc. ampa receptor potentiation can prevent ethanol-induced intoxication. neuropsychopharmacology. 2008 jun;33(7):1713-23. epub 2007 sep 12.
[2] zmijewski m1, gillespie ta, jackson da, schmidt df, yi p, kulanthaivel p. application of biocatalysis to drug metabolism: preparation of mammalian metabolites of a biaryl-bis-sulfonamide ampa (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor potentiator using actinoplanes missouriensis. drug metab dispos. 2006 jun;34(6):925-31. epub 2006 feb 28.
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