Levodropropizine99291-25-5

Levodropropizine99291-25-5

Levodropropizine
分子式：C13H20N2O2   分子量：236.31
 
产品描述
Levodropropizine 可以抗过敏并抑制组胺受体, 通过干扰外围感觉神经末端的刺激激活以及调节参与咳嗽反射的神经肽来减轻咳嗽。
靶点
           
IC50
           
体外研究
Levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors without affinity for H1-histaminic and alpha-adrenergic receptors.
体内研究
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
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO
特征
Levodropropizine have a better tolerability index than the Racemate.