Home Neuronal Signaling Histamine Receptor inhibitor Levodropropizine

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Levodropropizine Histamine Receptor inhibitor

Cat.No.S4131

Levodropropizine((S)-(-)-Dropropizine,DF-526) possess anti-allergic and inhibits histamine receptor, this compound reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.
Levodropropizine Histamine Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 236.31

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Quality Control

Batch: S413101 DMSO]47 mg/mL]false]Ethanol]47 mg/mL]false]Water]15 mg/mL]false Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (198.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : 15 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 236.31 Formula

C13H20N2O2

 Storage (From the date of receipt)
CAS No. 99291-25-5 Download SDF Storage of Stock Solutions

Synonyms (S)-(-)-Dropropizine,DF-526 Smiles C1CN(CCN1CC(CO)O)C2=CC=CC=C2

Mechanism of Action

Features
Demonstrates a better tolerability index than the Racemate.
Targets/IC50/Ki
Histamine receptor
In vitro

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. This compound (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. It is shown to have good antitussive activity in anaesthetized guinea-pigs and rabbits. This chemical (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. It (orally) is comparable with those of both dropropizine and codeine against coughing induced by irritant aerosols. This compound (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. It has a peripheral site of action which is related to sensory neuropeptides. This chemical (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. It (200 mg/kg) inhibits also substance P-evoked extravasation, whereas it does not affect the extravasation evoked by platelet activating factor.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/1611233/
  • [5] https://pubmed.ncbi.nlm.nih.gov/7504629/

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