125030-71-9
| 中文名称 | 125030-71-9 |
|---|---|
| 中文同义词 | 化合物 T16768 |
| 英文名称 | Ro 24-4736 |
| 英文同义词 | Ro 24-4736;4-(2-Chlorophenyl)-9-methyl-2-[3-[(5,6-dihydro-6-oxophenanthridin)-5-yl]-1-propynyl]-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine;6(5H)-Phenanthridinone, 5-[3-[4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl]-2-propyn-1-yl]-;Ro 24 4736,Ro244736 |
| CAS号 | 125030-71-9 |
| 分子式 | C31H20ClN5OS |
| 分子量 | 546.04 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 125030-71-9.mol |
| 结构式 |  |
125030-71-9 性质
| 熔点 | 247-249 °C |
|---|---|
| 沸点 | 819.6±75.0 °C(Predicted) |
| 密度 | 1.41±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 2.10±0.40(Predicted) |
PAF
Ro 24-4736 competes with [ 3 H]PAF for its receptor site on dog platelets with an IC 50 of 9.8±1.0 nM and selectively inhibits PAF-induced aggregation of guinea pig, dog and human platelets with concentration dependence.
Ro 24-4736 dose-dependently inhibits in vivo bronchoconstriction (ID50 of 0.006-mg/kg p.o.) and ex vivo platelet aggregation (ID 50 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. Ro 24-4736 is a new platelet activating factor antagonist. The tissue distribution of the 14 C-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.