Terbinafine hydrochloride 具有抗真菌感染活性。它是念珠菌属的角鲨烯环氧化酶的非竞争性抑制剂，Ki值为 30 nM。它还对某些革兰氏阳性和革兰氏阴性细菌具有抗菌活性。

Terbinafine Hydrochloride is a synthetic allylamine derivative structurally related to naftifine. Terbinafine is active against dermatophytes.

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 also very effective in experimental dermatophytoses following oral administration. In fungi-infected guinea pigs, the skin temperature dropps dramatically after the fourth treatment of terbinafine[6].

78628-80-5

C21H26ClN

327.9

TDT 067 hydrochloride;Terbinafine HCl;KWD 2019;盐酸特比萘芬

DMSO:32.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years