Bradanicline tosylate
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline tosylate exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline tosylate possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline tosylate requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline tosylate is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.
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- CAS. Nr.: 1111942-11-0
- Formel: C29H31N3O5S
- Molecular Weight:533.64
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Bradanicline tosylate potently and selectively activates human α7 nAChRs in vitro, with an EC50 of 17 nM[1].
Bradanicline tosylate does not induce desensitization of α7 nAChRs in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Bradanicline tosylate (30 mg/kg; i.p.; 30 min prior to challenge) inhibits citric acid-induced cough in male Hartley guinea pigs, but shows no such effect when delivered directly to the airways via aerosol at a concentration of 3 mg/mL (concurrently with citric acid challenge)[1].
Bradanicline tosylate (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) inhibits bradykinin-induced cough in male Hartley guinea pigs[1].
Bradanicline tosylate (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) inhibits nicotine-induced cough in male Hartley guinea pigs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley Guinea pigs (male, 200-400 g)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose; 60 minutes pre-challenge
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Result:Produced statistically significant decreases in cumulative citric acid-evoked coughs at 10 mg/kg, 30 mg/kg, and 100 mg/kg compared to vehicle control.
Did not produce a statistically significant reduction in cumulative citric acid-evoked coughs at 3 mg/kg compared to vehicle control.
Reached peak plasma concentrations of 100-500 ng/mL at antitussive doses, with brain concentrations reaching 10-20% of simultaneously measured plasma concentrations 1-2 hours after administration.
Chemical Information
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CAS. Nr. 1111942-11-0
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Molecular Weight 533.64
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Formel C29H31N3O5S
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SMILES
O=S(O)(C1=CC=C(C=C1)C)=O.O=C(C2=CC3=CC=CC=C3O2)N[C@H](C4CCN5CC4)[C@@H]5CC6=CN=CC=C6
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Synonyms
TC-5619 tosylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Bradanicline tosylate Related Classifications
HY-18060B Related Classifications
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