Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H24N2.C4H4O4 |
| Molecular Weight | 408.4901 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C/C(O)=O.C[C@@H](C1=C(CCN(C)C)CC2=CC=CC=C12)C3=CC=CC=N3
InChI
InChIKey=SWECWXGUJQLXJF-HFNHQGOYSA-N
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-/t15-;/m1./s1
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12593665 | https://www.drugbank.ca/drugs/DB08801 | https://www.drugs.com/international/dimetindene.html
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12593665 | https://www.drugbank.ca/drugs/DB08801 | https://www.drugs.com/international/dimetindene.html
Dimethindene (+)- is one of Dimethindene enantiomer that is a subtype-selective M2 muscarinic receptor antagonist. Dimetindene (trade name Fenistil; other name dimethindene maleate) is a potent antipruritic antihistamine, characterized by the small size of its effective dose and its rapidity of action. Dimetindene is an antihistamine/anticholinergic that is a selective H1 antagonist. Its effect sets in after 20 to 60 minutes and lasts several hours. Dimetindene drops as well as Dimetindene syrup is particularly indicated in pediatric practice. Dimetindene is indicated as symptomatic treatment of allergic reactions: urticaria, allergies of the upper respiratory tract such as hay fever and perennial rhinitis, food, and drug allergies; pruritus of various origins, except pruritus due to cholestasis; insect bites. Dimetindene is also indicated for pruritus in eruptive skin diseases such as chickenpox. Dimetindene can be as an adjuvant in eczema and other pruriginous dermatoses of allergic origin.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL211 |
30.2 nM [Ki] | ||
Target ID: CHEMBL1821 |
295.1 nM [Ki] | ||
Target ID: CHEMBL2035 |
758.6 nM [Ki] | ||
Target ID: CHEMBL216 |
190.6 nM [Ki] | ||
Target ID: CHEMBL245 |
138.0 nM [Ki] | ||
Target ID: CHEMBL231 |
69.2 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Fenistil Approved UseUnknown |
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| Primary | Fenistil Approved UseUnknown |
|||
| Primary | Fenistil Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: http://pcm.me/fenistil-%C2%AE/
Drops: Infants up to 1 year, 10-30 drops; Infants of 1 to 3 years, 30-45 drops; Children over 3 years, 45-60 drops; Adults, 60-120 drops.
Syrup: Infants up to 1 year, 1-3 teaspoons; Infants of 1 to 3 years, 3-4 teaspoons; Children over 3 years, 4-6 teaspoons; Adults, 6-12 teaspoons. 1 teasponful Fenistil syrup = 5ml = 0.5mg
Coated tablets: Adults, 3-6 tablets.
Route of Administration:
Oral
Rabbit vas deferens, Rat duodenum and Guinea-pig atria were used for activity evaluation. The tissues were allowed to equilibrate for 30 min. Then, concentration-response curves to the agonists were constructed in the absence (control) and in the presence of at least three concentrations (log interval = 0.48) of antagonists (Dimethindene (+)-), allowing 30-60 rain equilibration time. Preliminary experiments indicated that these intervals were sufficient for equilibration of the antagonist concentration used. The rat duodenum was exposed to only one concentration of antagonists. Each concentration of antagonist was tested 3-5 times and the ratios of agonist molar EC50 values obtained in the presence and absence of antagonists were calculated. The ECs0 values were determined by fitting the data to a non-linear iterative curve fitting procedure.
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SUBSTANCE RECORD
