Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H24BrN5O |
| Molecular Weight | 442.352 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC=C(CC2=CNC(NCCCCC3=C(C)C=C(Br)C=N3)=NC2=O)C=C1
InChI
InChIKey=OGEAASSLWZDQBM-UHFFFAOYSA-N
InChI=1S/C21H24BrN5O/c1-14-9-18(22)13-25-19(14)5-3-4-8-23-21-26-12-17(20(28)27-21)10-16-7-6-15(2)24-11-16/h6-7,9,11-13H,3-5,8,10H2,1-2H3,(H2,23,26,27,28)
Temelastine (also known as SK&F 93944) is a competitive histamine H1-receptor antagonist, which does not penetrate the central nervous system. This drug was studied as an anti-allergic agent. Experiments on animals have shown that the drug was efficacious vs. pharmacologic and antigen-induced bronchoconstriction.
CNS Activity
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The effect of intracerebroventricular injection of histamine in visceral nociception induced by acetic acid in rats. | 2010-10 |
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| Evaluation of mechanisms inducing thyroid toxicity and the ability of the enhanced OECD Test Guideline 407 to detect these changes. | 2005-07 |
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| Design, synthesis and antihistaminic (H1)activity of some condensed 2-(substituted)arylaminoethylpyrimidin-4(3H)-ones. | 2001 |
|
| Temelastine, a new H1-receptor antagonist. | 1986 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2875907
In twelve subjects single oral doses of 50, 100 and 200 mg of temelastine produced dose-dependent reductions in wheal areas.
Route of Administration:
Oral
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NCI_THESAURUS |
C29578
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5868
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ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)