375345-95-2 Usage
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 375345-95-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,7,5,3,4 and 5 respectively; the second part has 2 digits, 9 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 375345-95:
(8*3)+(7*7)+(6*5)+(5*3)+(4*4)+(3*5)+(2*9)+(1*5)=172
172 % 10 = 2
So 375345-95-2 is a valid CAS Registry Number.
375345-95-2Relevant articles and documents
Suppression of a palladium-mediated homocoupling in a Suzuki cross-coupling reaction. Development of an impurity control strategy supporting synthesis of LY451395
Miller, William D.,Fray, Andrew H.,Quatroche, John T.,Sturgill, Christa D.
, p. 359 - 364 (2007)
Described herein is the development of a control strategy resulting in exclusion of a persistent impurity (6) formed by a palladium (II)-mediated homocoupling of boronic acid (3) during a Suzuki cross-coupling reaction. Nearly complete suppression of the undesired homocoupling reaction was achieved through two process modifications. Thus, addition of a mild reducing agent, potassium formate, and use of a facile nitrogen subsurface sparge prior to introduction of the catalyst resulted in nearly complete exclusion of homocoupling dimer 6. These modifications apparently minimized the concentration of free Pd(II) in the reaction mixture without causing significant reduction of the oxidative addition product. In addition, use of palladium black as a heterogeneous coupling catalyst rendered the palladium control strategy trivial. Thus, the catalyst was separated from the product solution through use a clarifying filtration, resulting in near quantitative separation of palladium from LY 451395 (5). These conditions were successfully executed in three campaigns using 3-, 5-, 12-, and 22-L glassware.
Combination therapy for treatment of depression
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, (2008/06/13)
The present invention provides a method for treating depression, comprising administering to a patient an effective amount of a first component which is a suitable antidepressant, in combination with an effective amount of a second component which is a suitable AMPA receptor potentiator.
