research use only
Cat.No.S4139
| Related Targets | Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR |
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| Other Histamine Receptor Inhibitors | GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Mianserin HCl Astemizole Ciproxifan Maleate Lafutidine Mizolastine Dimethindene maleate Rupatadine |
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In vitro |
Water : 68 mg/mL
DMSO
: 7 mg/mL
(20.63 mM)
Ethanol : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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| Molecular Weight | 339.3 | Formula | C18H22N2.2HCl |
Storage (From the date of receipt) | |
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| CAS No. | 5897-18-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3.Cl.Cl | ||
| Targets/IC50/Ki |
Histamine H1 receptor
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| 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.
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| 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.
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