Ro-24-4736
目录号 : GC32588Ro24-4736是一种长效的选择性血小板活化因子(PAF)拮抗剂。
Cas No.:125030-71-9
Sample solution is provided at 25 µL, 10mM.
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Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action.
Ro 24-4736 competes with [3H]PAF for its receptor site on dog platelets with an IC50 of 9.8±1.0 nM and selectively inhibits PAF-induced aggregation of guinea pig, dog and human platelets with concentration dependence[1].
Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50 of 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID50 of 0.004 mg/kg p.o.) induced by PAF in guinea pigs. Time course studies show complete blockade of PAF-induced platelet aggregation (ex vivo) up to 8 hr after a single p.o. dose of 0.03 mg/kg as well as a long duration of action in vivo (30 hr). The in vivo PAF antagonistic activity is specific because, even at high p.o. doses (up to 10 mg/kg), Ro 24-4736 shows no inhibitory activity toward the bronchoconstrictor effects of leukotriene D4 or histamine. In comparison with other PAF antagonists evaluated in this guinea pig model, Ro 24-4736 is markedly superior in terms of p.o. potency, bioavailability and p.o. duration of action. Studies are also performed with Ro 24-4736 in additional in vivo models. When administered p.o. to sensitized guinea pigs, the drug attenuates inhaled antigen-induced airway hyper-reactivity without effect on bronchoalveolar lavage leukocyte accumulation[1]. Ro 24-4736 is a new platelet activating factor antagonist. The tissue distribution of the 14C-label in male rats following a single intravenous dose of 1.0 mg/kg of 14C-Ro 24-4736 indicats appreciable uptake by the liver, kidney, heart and gastrointestinal tract. Peak plasma and tissue concentrations are seen at 5 minutes after dosing except for the small intestine (4 hrs) and abdominal fat, stomach and large intestine (4 hrs). At 48 hours, only 3.5% of the dose is present in the tissues, and 6.1% in the lumen of the gastrointestinal tracts[2].
[1]. Crowley HJ, et al. Pharmacology of a potent platelet-activating factor antagonist: Ro 24-4736. J Pharmacol Exp Ther. 1991 Oct;259(1):78-85. [2]. Anastasi EM, et al. Disposition and metabolism of Ro 24-4736 in the rat. Life Sci. 1994;54(26):PL483-90.
Cas No. | 125030-71-9 | SDF | |
Canonical SMILES | O=C1N(CC#CC(S2)=CC3=C2N4C(CN=C3C5=CC=CC=C5Cl)=NN=C4C)C6=CC=CC=C6C7=C1C=CC=C7 | ||
分子式 | C31H20ClN5OS | 分子量 | 546.04 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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10 mM | 0.1831 mL | 0.9157 mL | 1.8314 mL |
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An oral platelet-activating factor antagonist, Ro-24-4736, protects the rat kidney from ischemic injury
Am J Physiol 1996 Nov;271(5 Pt 2):F1061-7.PMID:8946001DOI:10.1152/ajprenal.1996.271.5.F1061.
The role of platelet-activating factor (PAF) in ischemic acute renal failure was evaluated by administering an oral PAF antagonist (Ro-24-4736) to rats prior to or after interruption of blood flow to both kidneys for 30 min. In animals treated with the PAF antagonist prior to ischemia, renal function was less impaired and histological abnormalities was less pronounced when compared with postischemic kidneys from vehicle-treated animals. Serum creatinine (mg/ dl) 24 h following renal ischemia was 1.58 +/- 0.17 in the PAF antagonist-treated rats compared with 2.19 +/- 0.15 in rats given placebo (P < 0.01). There was less necrosis in the outer medulla of kidneys of PAF antagonist-treated animals (P < 0.01). Tissue myeloperoxidase activity at 48 and 72 h postischemia was lower in kidneys of PAF antagonist-treated rats (P < 0.05). The PAF antagonist was also protective when administered 30 min but not 2 h following the ischemic insult. The coincident use of anti-intercellular adhesion molecule-1 monoclonal antibody did not confer additional protection over that observed with the oral PAF antagonist alone. These data suggest that PAF contributes to the pathophysiology of renal ischemic injury, perhaps by its effects on leukocyte-endothelial interactions. An orally active PAF antagonist can protect against the development of ischemic acute renal failure.