| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
Purity: ≥98%
Cyclizine 2HCl (Marezine; Ciclizina; Nautazine; Valoid; Neo-devomit), the dihydrochloride salt of cyclizine, is a potent and 1st generation histamine H1 receptor antagonist of the piperazine class with anticholinergic and antiemetic properties. It has been used as a medication to treat and prevent vertigo, motion sickness, nausea, and vomiting. The exact mechanism through which cyclizine prevents vomiting and vertigo is still unknown. Cyclizine decreases the sensitivity of the labyrinthine apparatus and raises the tone of the lower oesophageal sphincter. It might suppress the area of the midbrain referred to as the emetic center.
| Targets |
Histamine H1 receptor
Histamine H1 receptor (H1R) [2] Mast cell [2] |
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| ln Vitro |
In vitro activity: Cyclizine belongs to the piperazine class of drugs that block histamine H1 receptors. It has antiemetic and anticholinergic qualities. The exact mechanism through which cyclizine prevents vomiting and vertigo is still unknown. Cyclizine decreases the sensitivity of the labyrinthine apparatus and raises the tone of the lower oesophageal sphincter. It might suppress the area of the midbrain referred to as the emetic center.
LPS (1 μg/mL)-induced RAW 264.7 macrophages were treated with Cyclizine 2HCl (10 μM-100 μM). It dose-dependently inhibited nitric oxide (NO) production, with 58% inhibition at 50 μM and 72% inhibition at 100 μM. This effect was associated with reduced iNOS mRNA expression (PCR) [1] - Human lung tissue fragments were activated with compound 48/80 (1 μg/mL) and treated with Cyclizine 2HCl (5 μM-50 μM). It inhibited histamine release by 65% at 30 μM and 80% at 50 μM, via stabilizing mast cell membranes [2] |
| ln Vivo |
Cyclizine is converted to norcyclizine, its N-demethylated derivative, which has less antihistaminic (H1) action than cycliziine. When taken orally, the effects start to manifest in 30 minutes, reach their peak in 1–2 hours, and, in the case of cyclizine, last for 4–6 hours. A single oral dose of 50 mg of cyclizine administered to healthy adult volunteers produced a peak plasma concentration of about 70 ng/mL about two hours after the drug was administered. The half-life of plasma elimination is roughly 20 hours.
Mouse spontaneous locomotor activity assay: Male ICR mice (20-25 g) were intraperitoneally injected with Cyclizine 2HCl (5 mg/kg, 10 mg/kg, 20 mg/kg). The 10 mg/kg and 20 mg/kg doses reduced spontaneous locomotor activity by 40% and 60% respectively over 60 minutes [3] - Opioid-induced hyperactivity model: Mice were intraperitoneally injected with Cyclizine 2HCl (10 mg/kg) 30 minutes before morphine (10 mg/kg, subcutaneous). It attenuated morphine-induced hyperactivity by 55% compared to morphine alone [3] - Amphetamine-induced hyperactivity model: Mice were intraperitoneally injected with Cyclizine 2HCl (10 mg/kg) 30 minutes before amphetamine (2 mg/kg, intraperitoneal). It reduced amphetamine-induced hyperactivity by 48% [3] |
| Cell Assay |
RAW 264.7 macrophage NO production assay: Seed RAW 264.7 cells in 24-well plates and incubate for 24 hours. Pre-treat with Cyclizine 2HCl (10 μM-100 μM) for 1 hour, then stimulate with LPS (1 μg/mL) for 24 hours. Collect supernatant to measure NO concentration via Griess reagent; extract total RNA to detect iNOS mRNA expression via PCR [1]
- Human lung tissue histamine release assay: Cut human lung tissue into small fragments, suspend in buffer, and pre-treat with Cyclizine 2HCl (5 μM-50 μM) for 30 minutes. Stimulate with compound 48/80 (1 μg/mL) for 60 minutes at 37°C. Centrifuge to collect supernatant and measure histamine concentration via fluorometric assay [2] |
| Animal Protocol |
Naive male CDI mice (Charles River) weighing 25-30 g
1, 10 mg/kg s.c.; locomotor activity (crossings) measured every 15 min for 2 hr. Mouse locomotor activity assay: Male ICR mice (20-25 g) were acclimated to the activity monitoring chamber for 30 minutes. Cyclizine 2HCl was dissolved in physiological saline and administered via intraperitoneal injection (5 mg/kg, 10 mg/kg, 20 mg/kg). Locomotor activity (total distance traveled) was recorded for 60 minutes post-administration [3] - Opioid/amphetamine-induced hyperactivity model: Mice were acclimated to the monitoring chamber for 30 minutes. Cyclizine 2HCl (10 mg/kg, intraperitoneal) was administered 30 minutes before subcutaneous injection of morphine (10 mg/kg) or intraperitoneal injection of amphetamine (2 mg/kg). Locomotor activity was recorded for 120 minutes post-opioid/amphetamine administration [3] |
| References |
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| Additional Infomation |
Cyclizine 2HCl is a first-generation histamine H1 receptor antagonist with anti-allergic, anti-inflammatory, and sedative effects [1,2,3]. Its core mechanisms include competitive H1R antagonism, mast cell stabilization (inhibition of histamine release), inhibition of iNOS-mediated NO production, and regulation of central nervous system motor activity [1,2,3]. Indications include allergic rhinitis, urticaria, pruritus, and motion sickness, and it can relieve allergy symptoms and vestibular dysfunction [2,3]. It exhibits sedative effects by inhibiting spontaneous and drug-induced motor activity in mice, a characteristic of first-generation antihistamines with blood-brain barrier penetration [3]. Its anti-inflammatory activity is associated with reduced NO production in activated macrophages, suggesting potential application value in mild inflammation [1]. It can stabilize mast cells. In human lung tissue cells, its efficacy in treating respiratory allergic diseases is supported [2].
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| Molecular Formula |
C18H24CL2N2
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|---|---|---|
| Molecular Weight |
339.3
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| Exact Mass |
302.155
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| Elemental Analysis |
C, 63.72; H, 7.13; Cl, 20.90; N, 8.26
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| CAS # |
5897-18-7
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| Related CAS # |
Cyclizine; 82-92-8; Cyclizine lactate; 5897-19-8; Cyclizine hydrochloride; 303-25-3
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| PubChem CID |
67533
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| Appearance |
Solid powder
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| LogP |
3.701
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
253
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3.Cl.Cl
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| InChi Key |
CKLJCUGYMOMAEJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2.2ClH/c1-19-12-14-20(15-13-19)18(16-8-4-2-5-9-16)17-10-6-3-7-11-17;;/h2-11,18H,12-15H2,1H3;2*1H
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| Chemical Name |
1-benzhydryl-4-methylpiperazine;dihydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9472 mL | 14.7362 mL | 29.4724 mL | |
| 5 mM | 0.5894 mL | 2.9472 mL | 5.8945 mL | |
| 10 mM | 0.2947 mL | 1.4736 mL | 2.9472 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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