product name Cyclizine 2HCl
Description: 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.
References: Anaesthesia. 2013 Dec;68(12):1284; J Pain Symptom Manage. 2013 May;45(5):e5-7.
339.3
Formula
C18H22N2.2HCl
CAS No.
5897-18-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 7 mg/mL (20.6 mM)
Water: 68 mg/mL (200.41 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427958
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References |
