| Bioactivity | 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. |
| Target | Ki: 0.6 nM (Adenosine A2A receptor) |
| Invitro | Sch412348 (SCH 412348) also completely antagonizes cAMP in cells expressing the recombinant human A2A receptor. Sch412348 is determined to have KB values of 0.3 nM, respectively at the A2A receptor; the value are in good agreement with the Ki values determined in radioligand binding assays. A similar functional assay with A2B receptor-expressing cells is used to demonstrate selectivity over A2B receptors. In this assay, the KB value for Sch412348 is 273 nM, indicating that Sch412348 is 910-fold selective for the A2A receptor over the A2B receptor[1]. |
| 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]. |
| Name | Sch412348 |
| CAS | 377727-26-9 |
| Formula | C22H21F2N9O |
| Molar Mass | 465.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
Sch412348
CAS: 377727-26-9 F: C22H21F2N9O W: 465.46
Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectiv
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