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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Dimethindene targets the histamine H1 receptor as an antagonist (Ki = 1.5 nM). It is selective for H1 receptors over M1 muscarinic acetylcholine receptors (Ki = 64 nM) and the serotonin 5-HT2A receptor (Ki = 2,400 nM). It has anticholinergic properties.
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| ln Vitro |
Dimethindenemaleate (1-1000 μM) has an IC50 value of 29.5 μM and inhibits glibenclamide-sensitive K+ currents that are induced by cromakalim in a concentration-dependent and reversible manner[2]. The glyburide-sensitive K+ current induced by Y-26763 is inhibited by dimethindenemaleate (1-1000 μM) with an IC50 value of 49 μM[2].
In vitro, dimethindene is a selective histamine H1 receptor antagonist. It has antihistamine activity. It is selective for H1 receptors over M1 mAChRs and 5-HT2A receptors. |
| ln Vivo |
Mice's ability to repair wounds is impacted by intraperitoneal injection of 0.25 mg of dimethylindadine maleate [1].
In vivo, dimethindene maleate is used for the research of hypersensitivity reactions. It is an antihistamine/anticholinergic used orally. It has been studied for its effects on allergic reactions. |
| Enzyme Assay |
In vitro receptor binding assays for dimethindene maleate typically use membrane preparations from cells expressing histamine H1 receptors. Radiolabeled histamine or H1 ligands are displaced by increasing concentrations of the compound to determine binding affinity (Ki). Non-specific binding is determined in the presence of excess unlabeled ligand.
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| Cell Assay |
Cell-based functional assays for dimethindene maleate involve measuring its ability to inhibit histamine-induced calcium mobilization or signaling in cells expressing H1 receptors. Cells are treated with the compound and stimulated with histamine. Inhibition of signaling is quantified. EC50 values are calculated.
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| Animal Protocol |
Animal/Disease Models: Wound-healing C57BL/6 mice [1]
Doses: 0.25 mg Route of Administration: intraperitoneal (ip) injection; 0.25 mg One-time Experimental Results: Skin wounds were Dramatically delayed, and wound closure disorders only occurred in the early stages of wound healing. In vivo animal studies for dimethindene maleate typically involve administration to animal models of allergic reactions. The compound's ability to inhibit histamine-induced responses, such as wheal formation or bronchoconstriction, is assessed. Antihistamine efficacy is evaluated. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of dimethindene maleate are characteristic of orally active antihistamines. The compound is absorbed following oral administration. It is distributed to tissues. Metabolism occurs in the liver. Excretion occurs through renal pathways.
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| Toxicity/Toxicokinetics |
Dimethindene maleate is generally well-tolerated. Common side effects include drowsiness, dry mouth, and dizziness. It should be used with caution in patients with glaucoma or urinary retention.
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| References |
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| Additional Infomation |
Dimetindene maleate is an indene compound, belonging to the histamine H1 receptor antagonist class. It is used to treat allergic reactions, rhinitis, pruritus, and some common cold remedies.
Dimethindene maleate is a selective histamine H1 receptor antagonist. It is used for the research of hypersensitivity reactions. It is an antihistamine/anticholinergic. It is not widely used clinically but is a valuable research tool for studying histamine receptor pharmacology. It is also known as Fenistil. |
| Molecular Formula |
C24H28N2O4
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|---|---|
| Molecular Weight |
408.49
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| Exact Mass |
408.204
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| CAS # |
3614-69-5
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| Related CAS # |
(S)-(+)-Dimethindene maleate;136152-65-3;Dimethindene;5636-83-9
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| PubChem CID |
5282414
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| Appearance |
White to off-white solid powder
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| Boiling Point |
416.3ºC at 760mmHg
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| Melting Point |
159-161℃
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| Flash Point |
205.6ºC
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| LogP |
3.858
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
518
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1=CC=CC=N1)C2=C(CC3=CC=CC=C32)CCN(C)C.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
SWECWXGUJQLXJF-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C20H24N2.C4H4O4/c1-15(19-10-6-7-12-21-19)20-17(11-13-22(2)3)14-16-8-4-5-9-18(16)20;5-3(6)1-2-4(7)8/h4-10,12,15H,11,13-14H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;N,N-dimethyl-2-[3-(1-pyridin-2-ylethyl)-1H-inden-2-yl]ethanamine
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| Synonyms |
SU-6518; SU 6518; Dimethindene maleate
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~306.01 mM)
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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 | 2.4480 mL | 12.2402 mL | 24.4804 mL | |
| 5 mM | 0.4896 mL | 2.4480 mL | 4.8961 mL | |
| 10 mM | 0.2448 mL | 1.2240 mL | 2.4480 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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