The Sound of Evolution
Theophylline
茶鹼
Mechanism of action:
Theophylline 是一種甲基黃嘌呤類（methylxanthine）化合物。Theophylline 可抑制細胞內磷酸二酯酶（phosphodiesterase）（尤其是 PDE3/PDE4）的活性，減少 cAMP 的分解，使其濃度上升。cAMP 增加後會活化蛋白激酶 A（protein kinase A），讓支氣管平滑肌放鬆。Theophylline 也會拮抗腺苷受體（adenosine receptor）A₁ 與 A₂A 受體，減少支氣管收縮，增強呼吸中樞興奮性。
Reference(s):
1. Nantwi KD et al. (2003). Adenosine A1 receptor mRNA expression and the effects of systemic theophylline administration on respiratory function 4 months after C2 hemisection. J Spinal Cord Med.
2. Daly JW et al. (1987). Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res.
3. Abdelrahman A et al. (2020). Substituted 4-phenylthiazoles: Development of potent and selective A(1), A(3) and dual A(1)/A(3) adenosine receptor antagonists. Eur J Med Chem.