product name Levodropropizine
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. 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.
References: Arzneimittelforschung. 1988 Aug;38(8):1144-50; Br J Pharmacol. 1996 Mar;117(5):853-8.
236.31
Formula
C13H20N2O2
CAS No.
99291-25-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 47 mg/mL (198.9 mM)
Water: 15 mg/mL (63.5 mM)
Ethanol: 47 mg/mL (198.9 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19427372
In Vitro |
In vitro activity: Levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors. Kinase Assay: Cell Assay: |
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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. |
Animal model | |
Formulation & Dosage | |
References | Arzneimittelforschung. 1988 Aug;38(8):1144-50; Br J Pharmacol. 1996 Mar;117(5):853-8. |