Cinnarizine is an antihistamine and calcium channel blocker. Its mechanism involves the inhibition of calcium influx and H1 receptor antagonism. It is used as a research tool to study these pathways.

In vitro, Cinnarizine acts as a calcium channel blocker. It inhibits calcium ion entry, which leads to relaxation of vascular smooth muscle and reduction of peripheral vascular resistance. It also blocks H1 receptors, exhibiting antihistamine properties.

In vivo, Cinnarizine is used for the treatment of vertigo, nausea, vomiting, and motion sickness. It is also useful for vestibular symptoms of other origins. Its vasodilating properties may contribute to its effects on vestibular disorders.

In vitro assays for Cinnarizine typically measure its calcium channel blocking activity. This can be assessed using patch-clamp electrophysiology or by measuring calcium influx using fluorescent indicators. Its H1 receptor antagonism is assessed using radioligand binding assays or functional assays.

Cellular assays for Cinnarizine are performed using cells expressing calcium channels or H1 receptors. Cells are treated with the compound, and calcium influx or histamine-induced responses are measured. Its effects on cell viability and proliferation are also assessed.

In vivo animal studies with Cinnarizine are conducted in models of motion sickness and vertigo. The compound is administered orally. Its efficacy in preventing vomiting and nausea is assessed. Its effects on vestibular function are evaluated.

Metabolism / Metabolites
Known human metabolites of cinnarizine include 4-{3-[4-(diphenylmethyl)piperazin-1-yl]prop-1-en-1-yl}phenol, benzophenone, 1-diphenylmethylpiperazine, 4-{phenyl[4-(3-phenylprop-2-en-1-yl)piperazin-1-yl]methyl}phenol, 1-cinnamylpiperazine, and cinnamaldehyde.
Cinnarizine is orally active. Its molecular weight is 368.51 g/mol and its formula is C26H28N2. It is soluble in chloroform. For research use, it is typically dissolved in DMSO for in vitro studies. Its half-life and metabolic profile have been characterized.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Cinnarizine has not been approved for marketing by the U.S. Food and Drug Administration (FDA), but it is available in other countries. There is currently no information regarding the use of cinnarizine during lactation. Experts advise that breastfeeding women should not use cinnarizine to prevent migraines. Other medications are recommended, especially when breastfeeding newborns or premature infants.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.
Cinnarizine is generally well tolerated but can cause side effects including drowsiness, headache, and gastrointestinal disturbances. It can induce parkinsonian disorders, particularly in elderly patients. It should be used with caution in patients with Parkinson's disease.

Cinnarizine is an N-alkylpiperazine, diarylmethane, and olefin compound. It possesses a variety of pharmacological effects, including antiemetic, histamine antagonist, calcium channel blocker, muscarinic receptor antagonist, anti-allergic, H1 receptor antagonist, and anti-aging properties. First synthesized by Janssen Pharmaceuticals in 1955, cinnarizine is an antihistamine primarily used to treat vestibular dysfunction and motion sickness. As a specific calcium channel blocker, cinnarizine acts mainly on the central vestibular system, interfering with signal transmission between the inner ear vestibular organs and the hypothalamic vomiting center. Due to its vasodilatory effect (primarily through calcium channel blockade), cinnarizine can also be considered a nootropic, acting primarily in the brain. Combining cinnarizine with other nootropics (such as piracetam) can enhance its effect on promoting brain oxygen supply. Cinnarizine is a piperazine derivative with histamine H1 receptor and calcium channel blocking activity, exhibiting vasodilatory and antiemetic effects, but it can induce Parkinson's syndrome. Indications Cinnarizine is used to treat vertigo/Meniere's disease, nausea and vomiting, motion sickness, and can also be used to treat vestibular symptoms caused by other reasons. Mechanism of Action Cinnarizine inhibits the contraction of vascular smooth muscle cells by blocking L-type and T-type voltage-gated calcium channels. Cinnarizine also binds to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors. Pharmacodynamics Cinnarizine is an antihistamine and calcium channel blocker. Histamine mediates various physiological activities, such as airway and gastrointestinal smooth muscle contraction, vasodilation, cardiac excitation, gastric acid secretion, promotion of interleukin release, and eosinophil and mast cell chemotaxis. Competitive antagonists of histamine H1 receptors can be divided into first-generation (sedative) and second-generation (non-sedative) drugs. Some drugs, such as cinnarizine, also block muscarinic acetylcholine receptors and are used as antiemetics. Cinnarizine can also inhibit the excitation of the vestibular system through its calcium channel blocking effect.
Cinnarizine is an antihistamine and calcium channel blocker used for the treatment of motion sickness, vertigo, and nausea. It has vasodilating properties. The compound is available in many countries as an over-the-counter medication for motion sickness. It is not approved by the FDA for use in the United States.

C26H28N2

368.51

368.225

298-57-7

Cinnarizine-d8;1185242-27-6

1547484

White to off-white solid powder

1.1±0.1 g/cm3

509.2±38.0 °C at 760 mmHg

117-120ºC

229.8±14.6 °C

0.0±1.3 mmHg at 25°C

1.626

4.63

0

2

6

28

429

0

C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=CC=C3)C4=CC=CC=C4

DERZBLKQOCDDDZ-JLHYYAGUSA-N

InChI=1S/C26H28N2/c1-4-11-23(12-5-1)13-10-18-27-19-21-28(22-20-27)26(24-14-6-2-7-15-24)25-16-8-3-9-17-25/h1-17,26H,18-22H2/b13-10+

1-benzhydryl-4-[(E)-3-phenylprop-2-enyl]piperazine

Dimitronal; Stugeron; Cinnarizine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~7.14 mg/mL (~19.38 mM)

Solubility in Formulation 1: ≥ 0.71 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 0.71 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 0.71 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 12 mg/mL (32.56 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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 (Please use freshly prepared in vivo formulations for optimal results.)