| Stereochemistry | ACHIRAL |
| Molecular Formula | C28H37N3O3 |
| Molecular Weight | 463.6117 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOCCN1C(=NC2=CC=CC=C12)C3CCN(CCC4=CC=C(C=C4)C(C)(C)C(O)=O)CC3
InChI
InChIKey=ACCMWZWAEFYUGZ-UHFFFAOYSA-N
InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33)
| Molecular Formula | C28H37N3O3 |
| Molecular Weight | 463.6117 |
| 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 |
Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine is an H1 receptor inverse agonist. Bilastine also exerts anti-inflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-α from human mast cells and granulocytes. Common side effects are headache and drowsiness.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Bilastine gave mild positive results for two uptake transporters, OATP2B1 and OCT1, mainly located in liver and intestine. Bilastine IC50 was determined for these two transporters and (based in previous knowledge), also for P-gp. The assay was carried out at seven bilastine concentrations ranging from 0.41 to 300 M. Bilastine showed poor inhibition, as values of IC50 obtained for all the three transporters were ≥ 300 M.
