1449371-87-2
Chemical Structure
TAS-303
- CAS No.: 1449371-87-2
- Formula:C22H20D7NO3
- Molecular Weight:360.50
IUPAC Name: piperidin-4-yl 2,2-diphenyl-2-(propoxy-d7)acetate
InChIKey: FMRVAGKPRZLTRG-KORWVGAPSA-N
SMILES: C(C(OC1CCNCC1)=O)(OC(C(C([2H])([2H])[2H])([2H])[2H])([2H])[2H])(C2=CC=CC=C2)C3=CC=CC=C3
Biological Activity:
TAS-303 is an orally effective selective norepinephrine transporter (NET) inhibitor. TAS-303 inhibits human NET ligand binding with a Ki of 50.9 nM, and suppresses NET-mediated norepinephrine uptake with an IC50 of 38.9 nM. TAS-303 enhances norepinephrine-induced contraction in isolated rat urethral tissues, elevates plasma norepinephrine levels in rats, and increases urethral baseline pressure and leak point pressure. TAS-303 is applicable for research related to stress urinary incontinence, norepinephrine reuptake, and lower urinary tract function[1][2].
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TAS-303 | TAS-303 is an orally effective selective norepinephrine transporter (NET) inhibitor. TAS-303 inhibits human NET ligand binding with a Ki of 50.9 nM, and suppresses NET-mediated norepinephrine uptake with an IC50 of 38.9 nM. TAS-303 enhances norepinephrine-induced contraction in isolated rat urethral tissues, elevates plasma norepinephrine levels in rats, and increases urethral baseline pressure and leak point pressure. TAS-303 is applicable for research related to stress urinary incontinence, norepinephrine reuptake, and lower urinary tract function. |
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References
- [1]. Mizutani H, et al. TAS-303, a Novel Selective Norepinephrine Reuptake Inhibitor that Increases Urethral Pressure in Rats, Indicating Its Potential as a Therapeutic Agent for Stress Urinary Incontinence. J Pharmacol Exp Ther. 2018 Aug;366(2):322-331.
- [2]. Kumagai Y, et al. A Drug-Drug Interaction Study to Evaluate the Effect of TAS-303 on CYP3A Activity in the Small Intestine and Liver. Journal of clinical pharmacology. 2020 Jun;60(6):702-710.
