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Fezolamine

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Catalog No. T68070Cas No. 80410-36-2

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.

Fezolamine

Fezolamine

🥰Excellent
Purity: 99.85%
Catalog No. T68070Cas No. 80410-36-2
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 SizePriceAvailabilityQuantity
1 mg$112In Stock
5 mg$260In Stock
10 mg$390In Stock
25 mg$653In Stock
50 mg$928In Stock
100 mg$1,260In Stock
500 mg$2,530In Stock
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Purity:99.85%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight305.42
FormulaC20H23N3
Cas No.80410-36-2
SmilesC(CCN(C)C)N1C=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
Storage & Solubility Information
StorageShipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (180.08 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2742 mL16.3709 mL32.7418 mL163.7090 mL
5 mM0.6548 mL3.2742 mL6.5484 mL32.7418 mL
10 mM0.3274 mL1.6371 mL3.2742 mL16.3709 mL
20 mM0.1637 mL0.8185 mL1.6371 mL8.1854 mL
50 mM0.0655 mL0.3274 mL0.6548 mL3.2742 mL
100 mM0.0327 mL0.1637 mL0.3274 mL1.6371 mL

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