Terbinafine是念珠菌属的角鲨烯环氧化酶有效的非竞争性抑制剂，Ki值为 30 nM。它具有抗真菌感染活性。

Terbinafine is a synthetic allylamine derivative with antifungal activity. Terbinafine exerts its effect through inhibition of squalene epoxidase, thereby blocking the biosynthesis of ergosterol, an important component of fungal cell membranes. As a result, this agent disrupts fungal cell membrane synthesis and inhibits fungal growth.

Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. [1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). [2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. [3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs<1 mg/L. [4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. [5]

Terbinafine is not only active after topical application but is extremely effective in experimental dermatophytoses following oral administration. In fungi infected guinea-pigs, the skin temperature dropps dramatically after the fourth treatment of terbinafine[6].

91161-71-6

C21H25N

291.438

TDT 067;Terbinex;SF 86-327;特比萘芬;Lamisil

H2O:<1 mgml
DMSO:58 mg/mL (199.01 mM)
Ethanol:58 mg/mL (199.01 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years