Bradanicline tosylate  (Synonyms: TC-5619 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^[1].

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.

Bradanicline tosylate (3-100 mg/kg; p.o.; 60 min prior to induction) dose-dependently inhibits citric acid-induced cough in male Hartley guinea pigs^[1].
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.

533.64

C₂₉H₃₁N₃O₅S

1111942-11-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Canning BJ, et al. Evidence for Alpha₇ Nicotinic Receptor Activation During the Cough Suppressing Effects Induced by Nicotine and Identification of ATA-101 as a Potential Novel Therapy for the Treatment of Chronic Cough. J Pharmacol Exp Ther. 2022;380(2):94-103.  [Content Brief]