| Description | Fezolamine is a novel orally available non-tricyclic compound with antidepressant activity. It is three to two times more selective in blocking synaptosomal uptake of [3H]norepinephrine than uptake of [4H]3-hydroxytryptamine or [3H]dopamine in vitro. It blocked the inhibitory effects of rifampicin and tetraphenyl in classical behavioral tests using monoamine-depleted animals. |
| In vivo | 采用Fezolamine（100-450 mg/天；口服；6周；42名患者）治疗后，相对于治疗前状态，从第2周开始在患者及医师评分量表上观察到了显著改善。55%的患者的Hamilton抑郁症评分量表(HAM-D)分数提高了超过50%。与临床显著反应相关的中位剂量为245 mg/天。6名退出研究的患者中有5名是因为胃肠道不良反应。最常见的不良反应包括恶心（36%）、头痛（29%）、便秘（26%）和口干（24%）。[1] |
| molecular weight | 305.42 |
| Molecular formula | C20H23N3 |
| CAS | 80410-36-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (180.08 mM) |
| References | 1. Zisook S, et al. Efficacy and safety of fezolamine in depressed patients. Neuropsychobiology. 1987;17(3):133-138. 2. McCoy L, et al. Determination of fezolamine and its desmethyl metabolite in human plasma and urine by high-performance liquid chromatography. Intravenous pharmacokinetics in the beagle hound. J Chromatogr. 1985;344:211-220. 3. Baizman ER, et al. Pharmacologic profile of fezolamine fumarate: a nontricyclic antidepressant in animal models. J Pharmacol Exp Ther. 1987;243(1):40-54. |