Molecular Formula | C18H24Cl2N2 |
Molar Mass | 339.30256 |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
In vitro study | Cyclidine is a histamine H1 receptor antagonist of The piperazine class. Has anticholinergic and antiemetic properties. The mechanism by which cyclidine exerts antiemetic and anti-Halo action has not been fully elucidated. Cyclidine increases the tension of the lower esophageal sphincter and reduces the sensitivity of the tortuous organs. Can inhibit a portion of the midbrain, collectively known as the emetic center. |
In vivo study | Cyclidine is metabolized to its N-desmethyl derivative, norcyclidine, which has little antihistamine (H1) activity compared to cyclidine. After oral administration of cyclidine, the effect is produced within 30 minutes, the maximum effect is achieved within 1-2 hours, which can last from 4 to 6 hours. Cyclidine was administered orally to healthy adult volunteers alone at a dose of 50 mg, and two hours after administration, a peak plasma concentration of about 70 ng/mL was produced. Plasma elimination half-life is about 20 hours. |
Biological activity | Cyclizine 2HCl is a piperazine derivative with Histamine H1 (histamine H1) receptor antagonist activity. |
target | TargetValue Histamine H1 receptor |
Target | Value |
In vitro study | Cyclizine is a histamine H1 receptor antagonist of piperazine. It has anticholinergic and antiemetic properties. The mechanism of antiemetic and antihalo action of Cyclizine has not been fully elucidated. Cyclizine increase the tension of the lower esophageal sphincter and reduce the sensitivity of tortuous organs. It can inhibit a part of the midbrain, collectively known as emetic centers. |
In vivo studies | Cyclizine metabolized into its N-demethylated derivatives, Norcyclizine, compared with Cyclizine, there is almost no antihistamine (H1) activity. After the Cyclizine is taken orally, the effect will be produced within 30 minutes, and the maximum effect will be achieved within 1-2 hours, which can last for 4 to 6 hours. Healthy adult volunteers were Cyclizine treated orally at a dose of 50 mg. After two hours of administration, a blood peak concentration of about 70 ng/mL was generated. The plasma elimination half-life is about 20 hours. |