2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Bradanicline tosylate

Bradanicline (TC-5619) tosylate 是一种口服有效、具有中等血脑屏障穿透性的 α7 nAChR 的激动剂。Bradanicline tosylate 对人源 α7 nAChR 表现出高亲和力及亚型选择性。Bradanicline tosylate 具有镇咳活性，依赖于持续的受体结合与激活。Bradanicline tosylate 需通过全身给药来剂量依赖性地抑制由柠檬酸、缓激肽及吸入尼古丁诱发的咳嗽。Bradanicline tosylate 在临床前研究中耐受性良好，被广泛应用于慢性难治性咳嗽的相关研究。

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Bradanicline tosylate

Bradanicline tosylate Chemical Structure

CAS No. : 1111942-11-0

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Bradanicline tosylate 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Bradanicline tosylate 可在体外强效且选择性地激活人源 α7 nAChRs，其 EC50 为 17 nM[1]。
Bradanicline tosylate 不会在体外诱导 α7 nAChRs 脱敏[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Bradanicline tosylate 相关抗体:
体内研究
(In Vivo)

Bradanicline tosylate (3-100 mg/kg；口服；诱发前 60 分钟) 可剂量依赖性地抑制雄性 Hartley 豚鼠中柠檬酸诱发的咳嗽，在 10、30 和 100 mg/kg 剂量下观察到具有统计学意义的效应[1]。
Bradanicline tosylate (30 mg/kg；腹腔注射；激发前 30 分钟) 可抑制雄性 Hartley 豚鼠中柠檬酸诱发的咳嗽，但以 3 mg/mL 浓度通过气溶胶直接递送气道时 (与柠檬酸激发同用) 则无此作用[1]。
Bradanicline tosylate (30 mg/kg；腹腔注射；单次给药；攻击前 30 分钟) 可抑制雄性 Hartley 豚鼠中缓激肽诱发的咳嗽[1]。
Bradanicline tosylate (30 mg/kg；腹腔注射；单次给药；攻击前 30 分钟) 可抑制雄性 Hartley 豚鼠中尼古丁诱发的咳嗽[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hartley Guinea pigs (male, 200-400 g)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose; 60 minutes pre-challenge
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.
分子量

533.64

Formula

C29H31N3O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Bradanicline tosylate 相关分类

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Keywords:

Bradanicline1111942-11-0TC-5619TC5619TC 5619nAChRNicotinic acetylcholine receptorsmale Hartley guinea pigsbradykininCNScitric acidchronic refractory coughα7 nAChRnicotinic acetylcholine receptornicotineInhibitorinhibitorinhibit

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