Piperazine, 1-diphenylmethyl-4-methyl-, dihydrochloride Chemical Properties

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

Soluble in DMSO > 10 mM

form 

Powder

Piperazine, 1-diphenylmethyl-4-methyl-, dihydrochloride Usage And Synthesis

Uses

Cyclizine dihydrochloride, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine dihydrochloride can be used for the research of nausea, vomiting, and dizziness[1][2][3].

Biological Activity

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

in vitro

Cyclizine is a piperazine histamine H1 receptor antagonist and has anticholinergic and antiemetic properties. It increases lower esophageal sphincter tone and reduces the sensitivity of tortuous organs.

in vivo

Cyclizine is metabolized to its N-desmethyl derivative, Norcyclizine, which has little antihistamine (H1) activity compared to Cyclizine. After oral administration of Cyclizine, the effect will be produced within 30 minutes, and the maximum effect will be achieved within 1-2 hours, which can last for 4-6 hours. Cyclizine administered orally at a dose of 50 mg alone in healthy adult volunteers produced peak plasma concentrations of approximately 70 ng/mL two hours after dosing. The plasma elimination half-life is about 20 hours.

target

IC 50

H₁ Receptor

References

[1] Králová J, et, al. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity. Int Immunopharmacol. 2009 Jul;9(7-8):990-5. DOI:10.1016/j.intimp.2009.04.005
[2] Church MK, et, al. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br J Pharmacol. 1980 Aug;69(4):663-7. DOI:10.1111/j.1476-5381.1980.tb07919.x
[3] Leza JC, et, al. Effects of antihistaminics on locomotor activity in mice. Comparison with opiate and amphetamine-induced hyperactivity. Gen Pharmacol. 1991;22(2):293-6. DOI:10.1016/0306-3623(91)90451-b

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