Amitifadine hydrochloride

• CAT Number: I003492
• CAS Number: 410074-74-7
• Molecular Formula: C11H12Cl3N
• Molecular Weight: 264.58
• Purity: ≥95%
• Target: Serotonin Transporter
• Solubility: 10 mM in DMSO
• Storage: -20°C
• IC50: 12/23/96 nM, 99/262/213 nM (Ki, for SERT/NET/ DAT) [1]

Amitifadine hydrochloride is a triple reuptake inhibitor (TRI) or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). Ki values for SERT/NET/ DAT are 99/262/213 nM. The IC50 values for serotonin, norepinephrine and dopamine reuptake are 12/23/96 nM.IC50 value: 12/23/96 nM, 99/262/213 nM (Ki, for SERT/NET/ DAT) [1]Target: Serotonin /Norepinephrine /Dopaminein vitro: Amitifadine is an antidepressant drug. Ki values for SERT, NET, and DAT are 99 nM, 262 nM, and 213 nM. The IC50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively. [1]In vivo: Amitifadine was active with minimal effective doses of 5 mg/kg in the rat forced swim test and mouse tail suspension antidepressant models. Consistent with triple re-uptake blockade, amitifadine inhibited ex vivo binding to dopamine, norepinephrine and serotonin transporters and robustly increased these transmitters in prefrontal cortex and dopamine in the striatum of rats. Recently, amitifadine was found in humans to have robust antidepressant activity and be well tolerated.[3]

Reference

[1]. Amitifadine
[2]. Skolnick P1, et al. Antidepressant-like actions of DOV 21,947: a /triple/ reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104.
[3]. Levin ED, et al. Amitifadine, a triple monoamine re-uptake inhibitor, reduces nicotine self-administration in female rats. Eur J Pharmacol. 2015 Jun 20;764:30-37.