Bradanicline hydrochloride  (Synonyms: TC-5619 hydrochloride)

Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough^[1].

EC₅₀: 17 nM (human α7 nAChR) K_i: 1.4 nM (human α7 nAChR)

Bradanicline hydrochloride potently and selectively activates human α7 nAChRs in vitro, with an EC₅₀ of 17 nM^[1].
Bradanicline hydrochloride 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 (3-100 mg/kg; p.o.; 60 min prior to induction) hydrochloride dose-dependently inhibits citric acid-induced cough in male Hartley guinea pigs, with statistically significant effects observed at doses of 10, 30 and 100 mg/kg^[1].
Bradanicline (30 mg/kg; i.p.; 30 min prior to challenge) hydrochloride 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 (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) hydrochloride inhibits bradykinin-induced cough in male Hartley guinea pigs^[1].
Bradanicline (30 mg/kg; i.p.; single administration; 30 minutes prior to challenge) hydrochloride 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.

397.90

C₂₂H₂₄ClN₃O₂

1111941-90-2

O=C(N[C@H]1[C@@H](N2CCC1CC2)CC3=CC=CN=C3)C4=CC5=CC=CC=C5O4.Cl

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]