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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $112 | In Stock | |
5 mg | $260 | In Stock | |
10 mg | $390 | In Stock | |
25 mg | $653 | In Stock | |
50 mg | $928 | In Stock | |
100 mg | $1,260 | In Stock | |
500 mg | $2,530 | In Stock |
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 | Fezolamine (100-450 mg/day; oral; 6 weeks; 42 patients) significant improvement relative to the patient's prestudy state was observed after 2 weeks in both patient and physician-rating scales. Fifty-five percent of patients improved their Hamilton Psychiatric Rating Scale for Depression (HAM-D) scores by more than 50%. The median dose associated with a clinically significant response was 245 mg/day. Five of the 6 patients who dropped out did so because of gastrointestinal adverse effects. The most common adverse effects were nausea (36%), headache (29%), constipation (26%), and dry mouth (24%).[1] |
Molecular Weight | 305.42 |
Formula | C20H23N3 |
Cas No. | 80410-36-2 |
Smiles | C(CCN(C)C)N1C=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3 |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (180.08 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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