| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 100mg | 电议 |
| 500mg | 电议 |
[3H]-Pyrilamine binding to histamine (H1) receptors in guinea pig cerebellum membranes | Antagonists were incubated with guinea pig cerebellum membranes (0.6 mg/mL) and [3H]-pyrilamine (1.2 nM) in 0.5 mL 50 mM PBS, pH 7.5, for 30 mins at 25 ℃. The incubation was ended by the addition of 5 mL of ice-cold PBS containing 2 μM Pyrilamine and the collection of membranes was on Whatman GF/B filters. Then the filters were washed with 3 × 5 mL of ice-cold PBS plus 2 μM Pyrilamine and transferred to counting vials. The radioactivity retained by each filter was measured by liquid scintillation counting in 3 mL of HiSafe 3. Specific binding was determined from the difference between the [3H]-pyrilamine bound in the absence and in the presence of a large molar excess (10 μM) of unlabeled Promethazine. |
Cell lines | Platelets |
Preparation method | The solubility of this compound in warm ethanol is >12.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months. |
Reacting condition | Up to 100 μM; 5 mins |
Applications | Rupatadine Fumarate competitively inhibited platelet-activating factor (PAF)-induced platelet aggregation in washed rabbit platelets (pA2 = 6.68 ± 0.08) and in human platelet-rich plasma (IC50 = 0.68 μM). However, Rupatadine Fumarate did not affect ADP- or arachidonic acid (AA)-induced platelet aggregation. |
Animal models | Mice and rats |
Dosage form | i.v. or p.o |
Applications | Rupatadine Fumarate (i.v.) blocked histamine- and PAF-induced hypotension in rats with the ID50 values of 1.4 and 0.44 mg/kg, respectively. Moreover, Rupatadine Fumarate potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg, respectively, for the i.v. and p.o. administrations) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg, respectively. i.v.). |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| 产品描述 | Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. References: |
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