中文名 | 富马酸卢帕他定 |
英文名 | Rupatadine fumarate |
别名 | 富马酸泸帕他 富玛酸卢帕他定 富马酸鲁帕他定 富马酸卢帕他定 富马酸泸帕他定 8-氯-6,11-二氢-11-[1-[(5-甲基-3-吡啶基)甲基]-4-哌啶亚基]-5H-苯并[5,6]环庚烷并[1,2-B] 8-氯-11-(1-((5-甲基吡啶-3-基)甲基)哌啶-4-亚基)-6,11-二氢-5H-苯并[5,6]环庚[1,2-B]吡啶富马酸盐 8-氯-6,11-二氢-11-[1-[(5-甲基-3-吡啶基)甲基]-4-哌啶亚基]-5H-苯并[5,6]环庚烷并[1,2-b]吡啶富马酸盐 |
英文别名 | Rupax FuMarate Rupafin FuMarate Pafinur FuMarate Rinialer FuMarate Rupatadine Fumarate RUPATADINE FUMARATE Rupatadine fumarate Alergoliber FuMarate 8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate 8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5h-benzo[5,6]cyclohepta[1,2-b]pyridine fumarate |
CAS | 182349-12-8 |
EINECS | 1592732-453-0 |
化学式 | C26H26ClN3.C4H4O4 |
分子量 | 532.03 |
InChI | InChI=1/C26H26ClN3.C4H4O4/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25;5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1- |
熔点 | 196-198°C |
溶解度 | 甲醇 (微溶加热) |
存储条件 | Sealed in dry,2-8°C |
外观 | 固体 |
颜色 | White to Pale Brown |
体外研究 | Rupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits 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 inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α. |
体内研究 | Rupatadine blocks 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 μg/kg i.v.). Moreover, it potently inhibits 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.). Rupatadine's duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.88 ml | 9.398 ml | 18.796 ml |
5 mM | 0.376 ml | 1.88 ml | 3.759 ml |
10 mM | 0.188 ml | 0.94 ml | 1.88 ml |
5 mM | 0.038 ml | 0.188 ml | 0.376 ml |
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