Bilastine
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Grundinformationen
- CAS
202189-78-4- Standard-SMILES
CCOCCn1c(C2CCN(CCc3ccc(C(C)(C)C(=O)O)cc3)CC2)nc2ccccc21- InChIKey
ACCMWZWAEFYUGZ-UHFFFAOYSA-N- Summenformel
- C28H37N3O3
- Durchschnittliche Molmasse
- 463,6 g/mol
- Monoisotopische Masse
- 463,28349204
Überblick
Bilastine is a member of benzimidazoles.
Namen und Bezeichner
- Bevorzugter Name
- Bilastine
- IUPAC
- 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
- Englischer Name
- Bilastine
- Summenformel
- C28H37N3O3
- Molmasse
- 463.62
Namen und Synonyme
Bilastine202189-78-4Ilaxten2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acidBilastinaDTXSID5057678PA1123N395DTXCID6031467Bilastinump-(2-(4-(1-(2-Ethoxyethyl)-2-benzimidazolyl)piperidino)ethyl)-alpha-methylhydratropic acid2-[4-(2-{4-[1-(2-ethoxyethyl)-1H-1,3-benzodiazol-2-yl]piperidin-1-yl}ethyl)phenyl]-2-methylpropanoic acid2-(4-(2-(4-(1-(2-ethoxyethyl)-1H-1,3-benzodiazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acid
Weitere Namen anzeigen
Bilastin2-(4-(2-(4-(1-(2-ETHOXYETHYL)-1H-BENZO[D ]IMIDAZOL-2-YL) PIPERIDIN-1-YL)ETHY)PHEN YL)-2-METHYLPROPANOIC ACIDBilatexBilastenBilestinBilasteneD6-Bilastine
2-(4-(2-(4-(1-(2-ethoxyethyl)benzimidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acidRefChem:568338R06AX292-(4-(2-(4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)ethyl)phenyl)-2-methylpropanoic acidBilaxtenBilastine [INN]MFCD09837814GTPL11579
Eigenschaften
Berechnete StruktureigenschaftenWird ergänzt
- XLogP
- 2,3
- Polarare Oberfläche (TPSA)
- 67,6 Ų
- H-Brücken-Donoren
- 1
- H-Brücken-Akzeptoren
- 5
- Frei drehbare Bindungen
- 10
- Schwere Atome
- 34
- Formalladung
- 0
- Komplexität
- 641
Experimentelle und physikochemische Eigenschaften
Drugs
Pharmaceuticals -> Listed in ZINC15
Pharmaceuticals -> Used in Switzerland
Human DrugsBreast Feeding; Lactation; Milk, Human; Antihistamines; Nonsedating Antihistamines; Histamine Antagonists
Physikochemische Eigenschaften
- Schmelzpunkt
- 202 °C · 202 °C
- Siedepunkt
- 639.1 · 639.1±55.0 °C(Predicted)
- Dichte
- 1.16 · 1.16±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Room Temperature
- Wasserlöslichkeit
- Insoluble in water
- Löslichkeit
- 49.3 · DMSO:49.3(Max Conc. mg/mL);106.34(Max Conc. mM)
- pka
- 4.4 · 4.40±0.10(Predicted)
- Aggregatzustand
- powder to crystal
- Farbe
- White to Light yellow
Sicherheit und Regulatorisches
Sicherheitsangaben dienen nur zur Orientierung und ersetzen weder das Sicherheitsdatenblatt (SDB) des Lieferanten noch geltende Vorschriften oder eine fachliche Bewertung.
GHS-Klassifizierung
GHS Classification
Warning
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P261, P264, P270, P271, P280, P301+P317, P302+P352, P304+P340, P317, P321, P330, P362+P364, and P501 (click each P-code to see the statement)
The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
Gefahrenhinweise
Hazard Classes and CategoriesAcute Tox. 4 (100%)
Toxikologische Informationen
Effects During Pregnancy and Lactation◉ Summary of Use during Lactation
Sicherheitsdaten
- wgk
- WGK 3
- hs_code
- 2933.39.4100
- Speicherklasse
- 11 - Combustible Solids
Chemie und Industrie
Pharmakologische Informationen
ATC Code
R06AX29
R - Respiratory system
S - Sensory organs
QR - Respiratory system
QS - Sensory organs
Protein BindingBilastine is 84-90% bound to human plasma proteins.
PharmacodynamicsBilastine is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria.
Mechanism of Action
Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM). During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.
Biological Half-LifeThe mean half life of elimination is 14.5h.
Metabolism/MetabolitesBilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans.
Absorption, Distribution and Excretion
Bilastine has a Tmax of 1.13 h. The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%.
Bilastine is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%). Nearly all is excreted as the parent compound.
Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h.
Metabolite PathwaysBilastine H1-Antihistamine Action
Anwendungen
Zugehörige Reaktionen
11
Notizen zur Verbindung
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