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Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $98 | In Stock | |
5 mg | $229 | In Stock | |
10 mg | $343 | In Stock | |
25 mg | $586 | In Stock | |
50 mg | $838 | In Stock | |
100 mg | $1,160 | In Stock | |
1 mL x 10 mM (in DMSO) | $219 | In Stock |
Description | Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment. |
Targets&IC50 | [3H]-DAU 6215:0.3 microM |
In vitro | Litoxetine HCl (0.3-3 microM) antagonized the high- and low-potency phases of the 5-HT curve.[1] Litoxetine HCl (1 and 3 microM) responses to 5-MeOT were shifted to the right in a concentration-dependent manner.[1] |
In vivo | Litoxetine HCl (twice daily for 4 days), a novel specific serotonin reuptake inhibitor.[2] |
Alias | litoxetine HCL(86811-09-8 Free base) |
Molecular Weight | 277.79 |
Formula | C16H20ClNO |
Smiles | [H]Cl.C1(COC2CCNCC2)=CC3=C(C=CC=C3)C=C1 |
Relative Density. | no data available |
Storage | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 22.5 mg/mL (81 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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