| Stereochemistry | RACEMIC |
| Molecular Formula | C22H28ClNO.ClH |
| Molecular Weight | 394.378 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(OCCN1CCCCCC1)(C2=CC=CC=C2)C3=CC=C(Cl)C=C3
InChI
InChIKey=YFCVXQAEHQJKQG-UHFFFAOYSA-N
InChI=1S/C22H28ClNO.ClH/c1-22(19-9-5-4-6-10-19,20-11-13-21(23)14-12-20)25-18-17-24-15-7-2-3-8-16-24;/h4-6,9-14H,2-3,7-8,15-18H2,1H3;1H
| Molecular Formula | C22H28ClNO |
| Molecular Weight | 357.917 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Setastine (Loderix) is a potent antagonist of histamine H1-receptor mediated responses. Setastine inhibits anaphylactic shock in guinea-pigs sensitized by horse serum. No antiserotonin, anticholinergic and antiadrenergic effect of the compound can be detected. Setastine has a long lasting (up to 16 h) antihistamine effect with a good oral effectiveness. It shows no cardiovascular effects in cats. Setastine shows a much weaker CNS depressant activity than clemestine fumarate. In displacement studies (3H-mepyramine) setastine had significantly weaker affinity for the central nervous system (CNS) H1-receptors than clemastine fumarate. It is concluded that setastine is a non-sedative highly active H1-antagonist.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
PubMed
Patents
Sample Use Guides
For prolonged use a dose of 2 mg three times/day (t.i.d.) is recommended. The antihistaminic effect of setastine almost equalled that of clemastine given in a dose of 1 mg t.i.d.
Route of Administration:
Oral
At low concentrations Setastine (Loderix) preincubated with rat peritoneal mast cells for 10 min prior to the addition of various stimulants (immune aggregates, ionophore A23187 and compound 48/80) produced a concentration-dependent inhibition of histamine release, while at high concentrations it induced the release of histamine. The IC50 values were calculated as 0.2, 15 and 50 uM by using immune aggregate, (rat IgG2 alpha + anti rat IgG) calcium ionophore and 48/80 as stimulants, respectively.
