Levodropropizine

Catalog No.S4131

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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Levodropropizine Chemical Structure

Levodropropizine Chemical Structure
Molecular Weight: 236.31

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Product Information

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Product Description

Biological Activity

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.
Targets Histamine receptor [1]
In vitro Levodropropizine has affinity for H1-histaminic and alpha-adrenergic receptors. [1]
In vivo Levodropropizine has weaker central sedative effects than the racemate and it does not induce physical dependence in rats. [1] 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. [2] 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. [3] 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. [4] 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. [5]
Features Demonstrates a better tolerability index than the Racemate.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Melillo G, et al. Arzneimittelforschung, 1988, 38(8), 1144-1150.

[2] Shams H, et al. Br J Pharmacol, 1996, 117(5), 853-858.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-05-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01573663 Completed Healthy Hanmi Pharmaceutical Company Limited February 2012 Phase 1
NCT01573663 Completed Healthy Hanmi Pharmaceutical Company Limited February 2012 Phase 1
NCT01416480 Completed Acute Bronchitis Ahn-Gook Pharmaceuticals Co.,Ltd May 2010 Phase 3
NCT01416480 Completed Acute Bronchitis Ahn-Gook Pharmaceuticals Co.,Ltd May 2010 Phase 3

Chemical Information

Download Levodropropizine SDF
Molecular Weight (MW) 236.31
Formula

C13H20N2O2

CAS No. 99291-25-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 47 mg/mL (198.89 mM)
Ethanol 47 mg/mL (198.89 mM)
Water 15 mg/mL (63.47 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1,2-Propanediol, 3-(4-phenyl-1-piperazinyl)-, (2S)-

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