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编 号:F748843
分子式:C11H16N2O5
分子量:256.26
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生物活性:
DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.

体内研究:
DL-TBOA ammonium (10 nmol; i.c.v.) to morphine-dependent rats significantly facilitates the expression of naloxone-precipitated somatic signs and conditioned place aversion.Animal Model:Male Sprague-Dawley rats (180-250 g)
Dosage:1 nmol, 3 nmol, 10 nmol
Administration:Intracerebroventricularly injection (i.c.v.)
Result:Dose dependently facilitated various somatic signs induced by Naloxone (0.1 mg/kg)-precipitated morphine withdrawal.

体外研究:
DL-TBOA ammonium (70-350 μM; 48 hours) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability.DL-TBOA ammonium (350 μM; 24 hours) decreases p53 induction by SN38 and oxaliplatin.
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