| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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| Other Sizes |
| Targets |
H1 Receptor
H1 histamine receptor (primary target). Thonzylamine acts as an orally bioactive antagonist (inhibitor) at the H1 histamine receptor. It also exhibits anticholinergic activity by interacting with acetylcholine receptors (AChR). |
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| ln Vitro |
Thonzylamine functions as a potent H1 histamine receptor antagonist, effectively blocking the effects of histamine at this receptor. Its antianaphylactic properties have been demonstrated, showing efficacy in reducing hypersensitivity reactions. As an antihistamine, it competitively inhibits histamine binding to H1 receptors, thereby preventing the downstream effects of histamine release, such as vasodilation, increased vascular permeability, and smooth muscle contraction in the airways. The compound's additional anticholinergic activity is attributed to its interaction with muscarinic acetylcholine receptors, which can lead to side effects such as dry mouth and blurred vision. Thonzylamine's biological activity has been characterized through various in vitro and in vivo studies, confirming its role as a potent antihistamine and antiallergic agent.
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| ln Vivo |
Thonzylamine has been shown to be effective in animal models and clinical settings for the treatment of allergic conditions. Its orally bioactive nature allows for convenient administration. In vivo, it exerts its therapeutic effects by antagonizing H1 receptors in peripheral tissues, thereby reducing the symptoms of allergic reactions, such as sneezing, itching, and rhinorrhea. It also has the ability to cross the blood-brain barrier, leading to central nervous system effects, including sedation, which is a common feature of first-generation antihistamines. Its anticholinergic properties can also manifest in vivo as dry mouth, constipation, and urinary retention.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Thonzylamine typically involve radioligand binding studies to determine its affinity for the H1 histamine receptor. These assays use membrane preparations from cells or tissues expressing the H1 receptor. The compound's ability to displace a specific radiolabeled H1 antagonist, such as [3H]-mepyramine, is measured to calculate its binding affinity (Ki). Functional assays may also be employed to assess its antagonistic activity by measuring its ability to inhibit histamine-induced responses, such as calcium mobilization or smooth muscle contraction in isolated tissue preparations. These protocols are standard for characterizing the receptor binding profile of antihistamines.
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| Cell Assay |
In vitro cell-based assays for Thonzylamine are conducted to evaluate its functional antagonism at the H1 receptor. Cells expressing the human H1 receptor (e.g., CHO or HEK-293 cells) are treated with histamine in the presence or absence of varying concentrations of Thonzylamine. The inhibition of histamine-induced intracellular calcium mobilization or other downstream signaling events is measured to quantify the antagonist activity. The IC50 or Ki values are determined from the concentration-response curves. These assays are crucial for confirming the compound's potency and efficacy as a H1 receptor antagonist.
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| Animal Protocol |
In vivo animal studies for Thonzylamine are typically conducted in rodent models to evaluate its antihistamine and antiallergic properties. The compound is administered orally or via intraperitoneal injection. Its efficacy is assessed in models of allergic reactions, such as histamine-induced bronchoconstriction or passive cutaneous anaphylaxis. The protective effect of Thonzylamine against histamine-induced lethality or other allergic responses is measured. Additionally, its sedative effects can be evaluated using behavioral tests such as the open field test or locomotor activity monitoring. These studies help to confirm the in vivo efficacy and pharmacological profile of the compound.
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| ADME/Pharmacokinetics |
Thonzylamine is an orally bioavailable compound, but detailed pharmacokinetic parameters such as half-life, volume of distribution, and clearance are not extensively documented in publicly available literature. As a first-generation antihistamine, it is known to be well-absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. It is widely distributed throughout the body, including the central nervous system, due to its lipophilic nature. The compound is metabolized by hepatic cytochrome P450 enzymes and excreted primarily in the urine as metabolites. Its duration of action is typically several hours, and it may accumulate with repeated dosing due to its lipophilic properties.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for Thonzylamine. However, as a first-generation antihistamine, its toxicity profile is expected to be consistent with other drugs in this class. Common side effects include sedation, drowsiness, dizziness, and anticholinergic effects such as dry mouth, blurred vision, constipation, and urinary retention. At high doses, it may cause more severe central nervous system depression, hallucinations, or seizures. In cases of overdose, cardiovascular effects such as tachycardia and arrhythmias may occur. Thonzylamine is a controlled substance and not for sale in certain territories.
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| References | |
| Additional Infomation |
Toniracene is an oily liquid. It is used as an antihistamine in its hydrochloride form. N'-[(4-methoxyphenyl)methyl]-N,N-dimethyl-N'-(2-pyrimidinyl)ethane-1,2-diamine belongs to the methoxyphenyl family of compounds. Toniracene is an antihistamine and anticholinergic drug. It is used in combination with [DB04837] or [DB00388] to provide temporary relief for symptoms of the common cold, hay fever (allergic rhinitis), or other upper respiratory tract allergies.
Indications Toniracene is indicated for the control of allergic rhinitis or other upper respiratory tract allergy symptoms. It is often an ingredient in over-the-counter combination medications. FDA LabelMechanism of Action Toniracene competitively binds to the H1 histamine receptor. Binding of histamine to this receptor stimulates vasodilation and increased vascular permeability, leading to nasal congestion and runny nose. Histamine can also stimulate nerve endings, causing itching, which in turn leads to sneezing. Tonilacamine can reduce or eliminate the symptoms of allergic rhinitis by blocking these effects. Pharmacodynamics Tonilacamine is a first-generation antihistamine. It antagonizes the effects of histamine, thereby relieving allergy symptoms such as nasal congestion, runny nose, itchy eyes, itchy nasopharynx, and sneezing. Thonzylamine (Neohetramine) is an orally active H1 histamine receptor antagonist that exhibits good antihistaminic and antianaphylactic properties. It is used in the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis, and other allergic diseases. The compound is a first-generation antihistamine with sedative and anticholinergic properties. Thonzylamine is structurally an ethylenediamine derivative and is available as the hydrochloride salt. It is not approved for clinical use as a standalone therapeutic agent and is strictly for research purposes only. Thonzylamine is a controlled substance in some regions. |
| Molecular Formula |
C16H22N4O
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|---|---|
| Molecular Weight |
286.37
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| Exact Mass |
286.179
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| CAS # |
91-85-0
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| Related CAS # |
63-56-9 (mono-hydrochloride)
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| PubChem CID |
5457
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| Appearance |
Colorless to light yellow viscous liquid
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| Density |
1.121g/cm3
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| Boiling Point |
440.6ºC at 760 mmHg
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| Melting Point |
173-176
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| Flash Point |
220.3ºC
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| Index of Refraction |
1.584
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| LogP |
2.053
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
21
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| Complexity |
274
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCN(CC1=CC=C(C=C1)OC)C2=NC=CC=N2
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| InChi Key |
GULNIHOSWFYMRN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H22N4O/c1-19(2)11-12-20(16-17-9-4-10-18-16)13-14-5-7-15(21-3)8-6-14/h4-10H,11-13H2,1-3H3
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| Chemical Name |
N'-[(4-methoxyphenyl)methyl]-N,N-dimethyl-N'-pyrimidin-2-ylethane-1,2-diamine
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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 |
| 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) |
DMSO: 100 mg/mL (349.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.73 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.73 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4920 mL | 17.4599 mL | 34.9199 mL | |
| 5 mM | 0.6984 mL | 3.4920 mL | 6.9840 mL | |
| 10 mM | 0.3492 mL | 1.7460 mL | 3.4920 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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