Amitifadine (hydrochloride)

Modify Date: 2024-01-03 21:53:55

Amitifadine (hydrochloride) Structure
Amitifadine (hydrochloride) structure
Common Name Amitifadine (hydrochloride)
CAS Number 410074-74-7 Molecular Weight 264.57900
Density N/A Boiling Point N/A
Molecular Formula C11H12Cl3N Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Amitifadine (hydrochloride)


Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.

 Names

Name (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane,hydrochloride
Synonym More Synonyms

 Amitifadine (hydrochloride) Biological Activity

Description Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
Related Catalog
Target

IC50: 12 nM (serotonin), 23 nM (norepinephrine), 96 nM (dopamine)[1].

In Vitro Amitifadine (DOV 21,947) 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 The 30 mg/kg Amitifadine dose significantly reduces nicotine self-administration. The 5 and 10 mg/kg doses reduce nicotine self-administration during the first 15 min. of the session when the greatest amount of nicotine is self-administered. The 30 mg/kg Amitifadine dose, but not the lower doses cause a significant reduction in locomotor activity averaged over the 1-hour session and reduce food motivated responding. The 10 mg/kg dose causes hypoactivity at the beginning of the session, but 5 mg/kg does not cause any hypoactivity. The effect of chronic Amitifadine treatment (10 mg/kg) over the course of 15 sessions is also determined. Amitifadine causes a significant reduction in nicotine self-administration, which is not seen to diminish over two consecutive weeks of treatment and a week after enforced abstinence. Amitifadine significantly reduces nicotine self-administration. This prompts further research to determine if Amitifadine might be an effective treatment for smoking cessation[2].
References

[1]. 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.

[2]. 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.

 Chemical & Physical Properties

Molecular Formula C11H12Cl3N
Molecular Weight 264.57900
Exact Mass 263.00400
PSA 12.03000
LogP 3.98510
Storage condition 2-8℃

 Synonyms

DOV 21,947
AMITIFADINE HYDROCHLORIDE
UNII-R01R720TVG
EB-1010
Amitifadine hydrochloride (USAN)
Amitifadine HCl
Amitifadine (hydrochloride)
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