Cephaeline dihydrochloride is a naturally occurring alkaloid that is a selective CYP2D6 inhibitor with an IC50=121 μM. It has an affinity for and oral activity at the 5-HT4 receptor and is capable of inducing vomiting.

CYP2D6:121 μM, CYP3A4:1000 μM

在人体肝微粒体系统中，Cephaeline dihydrochloride 对主要的细胞色素 P450 酶系表现出较弱的抑制活性。研究表明，其对 CYP2D6 的半数抑制浓度（IC₅₀）为 121 μM，抑制常数（Ki）为 54 μM，属竞争性抑制；而对 CYP3A4 的 IC₅₀ 为 1000 μM，Ki 为 355 μM，为非竞争性抑制[1]。