| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Diazoline targets the histamine H1 receptor, blocking the action of histamine. By antagonizing the H1 receptor, it prevents histamine-induced effects such as vasodilation, increased vascular permeability, and smooth muscle contraction. This mechanism provides relief from allergic symptoms.
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|---|---|
| ln Vitro |
The effects of mebHydrolin, a particular histamine H1 receptor antagonist, were contrasted with those of chlorpromazine, a common phenothiazine [1]. MebHydrolin has been shown in ethanol interaction experiments to have antihistamine properties [2].
In vitro, Diazoline acts as a specific histamine H1-receptor antagonist. Its binding affinity and antagonistic activity are characterized in receptor binding assays and functional assays. It is used as a reference compound in studies of histamine receptor pharmacology. |
| ln Vivo |
In vivo, Diazoline is used for the symptomatic relief of allergic symptoms caused by histamine release. It is effective in treating nasal allergies and allergic dermatosis. Its antihistamine activity helps reduce symptoms such as itching, sneezing, and runny nose.
|
| Enzyme Assay |
In vitro receptor binding assays for Diazoline typically measure its affinity for the histamine H1 receptor. Radiolabeled histamine or H1 ligands are displaced by increasing concentrations of the compound to determine binding affinity (Ki). Functional assays measure the compound's ability to inhibit histamine-induced signaling, such as calcium mobilization.
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| Cell Assay |
Cell-based assays for Diazoline involve treating cells expressing H1 receptors with the compound and measuring its effects on receptor-mediated signaling. Cells are treated with the compound and stimulated with histamine. Inhibition of signaling is quantified. These studies help characterize the compound's potency and selectivity as an H1 antagonist.
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| Animal Protocol |
In vivo animal studies for Diazoline are typically conducted in models of allergic reactions. The compound is administered, and its ability to inhibit histamine-induced responses, such as wheal formation or bronchoconstriction, is assessed. These studies help evaluate its efficacy and safety as an antihistamine.
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| ADME/Pharmacokinetics |
Diazoline has a molecular weight of 564.7 g/mol and a molecular formula of C29H28N2O6S2. It is a heterocyclic organic compound characterized by its five-membered ring structure containing two nitrogen atoms.
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| Toxicity/Toxicokinetics |
The toxicological profile of Diazoline is consistent with that of other antihistamines. Common side effects include drowsiness, dry mouth, and dizziness. The compound should be used with caution in patients with certain medical conditions. As a research compound, it should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
Methionyl naphthalene disilicate is a polymer.
See also: Methionyl naphthalene (note moved to). Diazoline (Mebhydrolin) is an antihistamine used for the symptomatic relief of allergic symptoms. It is a histamine H1-receptor antagonist that is used in the treatment of nasal allergies and allergic dermatosis. It is also used as a research tool for studying histamine receptor pharmacology. |
| Molecular Formula |
C48H48N4O6S2
|
|---|---|
| Molecular Weight |
841.0479
|
| Exact Mass |
840.301
|
| CAS # |
6153-33-9
|
| Related CAS # |
Mebhydrolin;524-81-2
|
| PubChem CID |
22529
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| Appearance |
White to off-white solid powder
|
| Density |
0.9799 (rough estimate)
|
| Boiling Point |
457.3ºC at 760 mmHg
|
| Melting Point |
280°C (rough estimate)
|
| Flash Point |
230.4ºC
|
| Index of Refraction |
1.8676 (estimate)
|
| LogP |
10.725
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
60
|
| Complexity |
799
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CJUOSBUQOWKEKJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/2C19H20N2.C10H8O6S2/c2*1-20-12-11-19-17(14-20)16-9-5-6-10-18(16)21(19)13-15-7-3-2-4-8-15;11-17(12,13)9-5-1-3-7-8(9)4-2-6-10(7)18(14,15)16/h2*2-10H,11-14H2,1H3;1-6H,(H,11,12,13)(H,14,15,16)
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| Chemical Name |
5-benzyl-2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indole;naphthalene-1,5-disulfonic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~5.56 mg/mL (~6.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (0.67 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 5.6 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: ≥ 0.56 mg/mL (0.67 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 5.6 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: ≥ 0.56 mg/mL (0.67 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 | 1.1890 mL | 5.9449 mL | 11.8899 mL | |
| 5 mM | 0.2378 mL | 1.1890 mL | 2.3780 mL | |
| 10 mM | 0.1189 mL | 0.5945 mL | 1.1890 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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