Molecular Weight(MW): 236.31
Levodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.
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Choose Selective Histamine Receptor Inhibitors
|Description||Levodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.|
|Features||Demonstrates a better tolerability index than the Racemate.|
Levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors. 
|In vivo||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 platelet activating factor. |
-  Melillo G, et al. Arzneimittelforschung, 1988, 38(8), 1144-1150.
-  Shams H, et al. Br J Pharmacol, 1996, 117(5), 853-858.
-  Malandrino S, et al. Arzneimittelforschung, 1988 , 38(8), 1141-1143.
|In vitro||DMSO||47 mg/mL (198.89 mM)|
|Ethanol||47 mg/mL (198.89 mM)|
|Water||15 mg/mL (63.47 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01573663||Completed||Healthy||Hanmi Pharmaceutical Company Limited||February 2012||Phase 1|
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