PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca exchanger in guinea pig airway smooth muscle.
体外研究
PPADS tetrasodiuma (1-30 μM; 10-50 minutes) inhibits Na+/Ca2+ exchanger reverse mode (NCXREV) in a time- and concentration dependent manner.
PPADS tetrasodiuma is effective at other native and recombinant P2XRs. At human P2XRs sensitivity to PPADS tetrasodiuma depended on the subtype and is highest at the hP2X1, -2, -3, -5, and -7Rs with an IC50 of ~1-3 and ~30 μM for the hP2X4R.
体内研究
PPADS tetrasodiuma (15-60 mg/100g body weight (BW); i.p.; every 12 hours for 8 days) inhibits glomerular mesangial cells (MC) proliferation without altering proliferation of non-MC in vivo in mesangial proliferative glomerulonephritis.
Animal Model:
Male Sprague-Dawley ratsweighing 160 to 200 g (anti-Thy1 disease mode)
Dosage:
15 mg/100g BW, 30 mg/100g BW, 60 mg/100g BW
Administration:
i.p.; every 12 hours for 8 days (the first PPADS injection was administered 60 minutes after disease induction, and the loading dose always contained double the amount of PPADS compared to the following injections.)
Result:
Specifically and dose-dependently reduced early (day 3) glomerular mesangial cell proliferation without altering proliferation of non-MC.
分子式
C14H10N3O12PS2-4.4[Na+]
分子量
599.30
CAS号
192575-19-2
运输条件
Room temperature in continental US; may vary elsewhere.