Levodropropizine99291-25-5

Levodropropizine
分子式：C13H20N2O2   分子量：236.31
 
產(chǎn)品描述
Levodropropizine 可以抗過敏并抑制組胺受體, 通過干擾外圍感覺神經(jīng)末端的刺激激活以及調(diào)節(jié)參與咳嗽反射的神經(jīng)肽來減輕咳嗽。
靶點
           
IC50
           
體外研究
Levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors without affinity for H1-histaminic and alpha-adrenergic receptors.
體內(nèi)研究
Levodropropizine has weaker central sedative effects than the racemate and it does not induce physical dependence in rats. Levodropropizine (15 mg/kg, i.v.) reduces both the duration of apnoea and the response of the C-fibre to phenylbiguanide. The LVDP-induced inhibition of the C-fibre response to PBG is on average 50% in pulmonary and 25% in non-pulmonary fibres. Levodropropizine is shown to have good antitussive activity in anaesthetized guinea-pigs and rabbits. Levodropropizine (i.v.) is 1/10 to 1/20 as active as codeine and comparable to dropropizine on mechanically and electrically induced coughing in rabbits and guinea-pigs. Levodropropizine (orally) is comparable with those of both dropropizine and codeine against coughing induced by irritant aerosols. Levodropropizine (40 μg/50 μL i.c.v.) does not prevent electrically-induced cough, while Codeine (5 μg/50 μl i.c.v.) markedly prevents coughing in guinea-pigs. Levodropropizine has a peripheral site of action which is related to sensory neuropeptides. Levodropropizine (10 mg/kg, 50 mg/kg and 200 mg/kg) reduces in a dose-dependent manner the extravasation of Evans blue dye evoked by capsaicin in the rat trachea. Levodropropizine (200 mg/kg) inhibits also substance P-evoked extravasation, whereas it does not affect the extravasation evoked by plaet activating factor.
溶解性
DMSO 47 mg/mL，水 15 mg/mL，乙醇 47 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO
特征
Levodropropizine have a better tolerability index than the Racemate.