Cyclizine 2HCl

Catalog No.S4139

Cyclizine 2HCl Chemical Structure

Molecular Weight(MW): 339.3

Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.

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Biological Activity

Description Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
Targets
Histamine H1 receptor [1]
In vitro

Cyclizine is a histamine H1 receptor antagonist of the piperazine class. It possesses anticholinergic and antiemetic properties. The mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated. Cyclizine increases lower oesophageal sphincter tone and reduces the sensitivity of the labyrinthine apparatus. It may inhibit the part of the midbrain known collectively as the emetic centre. [1]

In vivo Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine. Following oral administration effects develop within 30 minutes, are maximal within 1-2 hours and last, for cyclizine, for 4-6 hours. In healthy adult volunteers the administration of a single oral dose of 50 mg cyclizine resulted in a peak plasma concentration of approximately 70 ng/mL occurring at about two hours after drug administration. The plasma elimination half-life is approximately 20 hours. [1]

Protocol

References

Solubility (25°C)

In vitro Water 68 mg/mL (200.41 mM)
DMSO 7 mg/mL (20.63 mM)
Ethanol 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 Information

Molecular Weight 339.3
Formula

C18H22N2.2HCl

CAS No. 5897-18-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02905019 Recruiting Malaria University of Oxford August 2016 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID