Sch412348
Sch412348 Basic information
- Product Name:
- Sch412348
- Synonyms:
-
- Sch412348
- 7H-Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, 7-[2-[4-(2,4-difluorophenyl)-1-piperazinyl]ethyl]-2-(2-furanyl)-
- Sch412348,Sch-412348
- CAS:
- 377727-26-9
- MF:
- C22H21F2N9O
- MW:
- 465.46
- Mol File:
- 377727-26-9.mol
Sch412348 Chemical Properties
- Density
- 1.62±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 5.88±0.10(Predicted)
Sch412348 Usage And Synthesis
Uses
Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
in vivo
Oral administration of Sch412348 (0.1-1 mg/kg) to rats potentiates 3,4-dihydroxy-L-phenylalanine (L-Dopa)-induced contralateral rotations after 6-hydroxydopamine lesions in the medial forebrain bundle and potently attenuates the cataleptic effects of haloperidol. Sch412348 (1 and 3 mg/kg) dose-dependently attenuates haloperidol-induced catalepsy 1 h [F(3,20)=3.9, p<0.05] and 4 h [F(3,20)=7.5, p<0.01] after dosing. Sch412348 [F(2,51) =10.6, p<0.01] (0.1-1 mg/kg) reduces immobility time in the mouse tail suspension test (TST) at 1 mg/kg. Sch412348 (SCH 412348) significantly increases activity levels in the mouse [F(4,27)=2.9, p<0.05]. Both the 0.3 and 3 mg/kg treatment groups are significantly more active than vehicle-treated mice. The 1 mg/kg group approached significance (p=0.052)[1].
References
[1] Hodgson RA, et al. Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression. J Pharmacol Exp Ther. 2009 Jul;330(1):294-303. DOI:10.1124/jpet.108.149617
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