Cyclizine Lactate

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Cat Number

API5897198

CAS Number

5897-19-8

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Product Detail Description Scientific Support Customer Q&A

CAS Number

5897-19-8

Synonyms

1-(Diphenylmethyl)-4-methylpiperazine monolactate;Piperazine, 1-(diphenylmethyl)-4-methyl-, mono(2-hydroxypropanoate)

Molecular Formula

C21H28N2O3

Molecular Weight

356.5

Smiles

CC(C(=O)O)O.CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3

General Description

Cyclizine Lactate is the lactate salt of cyclizine, a first-generation histamine H1 receptor antagonist with prominent antiemetic properties belonging to the piperazine class. The lactate salt form offers distinct solubility characteristics compared to the hydrochloride salt.

Mechanism of Action

Cyclizine Lactate acts primarily by blocking histamine H1 receptors and muscarinic cholinergic receptors in the vomiting center and chemoreceptor trigger zone of the medulla. It also exerts central anticholinergic effects on the vestibular system, contributing to antiemetic and anti-motion sickness activity.

Application

Indicated for the prevention and treatment of nausea, vomiting, and motion sickness. Cyclizine Lactate is a first-generation H1 receptor antagonist with prominent antiemetic properties, effective in postoperative nausea, vestibular disorders, and drug-induced emesis through combined H1 and muscarinic receptor blockade.

Cyclizine lactate acts as a potent and selective histamine H1 receptor antagonist. At a concentration of 100 μM, cyclizine lactate significantly inhibited nitrite accumulation in lipopolysaccharide-stimulated RAW 264.7 cell supernatants and reduced inducible nitric oxide synthase protein levels. This anti-inflammatory effect was independent of the compound's lipophilicity, as no correlation was observed between the inhibition of nitrite production and calculated logP values. Cyclizine lactate also inhibited anti-immunoglobulin E-induced histamine release from isolated human lung fragments, with an inhibitory concentration fifty value of 5.42 μM. The drug enhanced locomotor activity of mice in a dose-dependent manner at doses ranging from 1 to 10 mg/kg.

Fig. 1 Cyclizine (CYC) significantly inhibited both nitrite accumulation and iNOS protein expression. (Králová J.; et al. 2009)

References

Králová J, et al. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity. International immunopharmacology, 2009, 9(7-8): 990-995.

What makes Cyclizine Lactate distinct from other antiemetic antihistamines?

Cyclizine Lactate combines H1 receptor antagonism with significant central anticholinergic and vestibular system effects, providing broader antiemetic coverage compared to more selective H1 antagonists.

What purity specifications apply?

Cyclizine Lactate is supplied as a high-purity grade meeting pharmaceutical manufacturing and R&D requirements.

Can packaging be customized?

Custom packaging and labeling options are available upon request for R&D and production needs.

What storage conditions are recommended?

Cyclizine Lactate should be stored at room temperature in a tightly sealed container, protected from light and moisture.