410074-74-7
410074-74-7 structure
- Name: Amitifadine (hydrochloride)
- Chemical Name: (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane,hydrochloride
- CAS Number: 410074-74-7
- Molecular Formula: C11H12Cl3N
- Molecular Weight: 264.57900
- Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
- Create Date: 2017-06-13 07:22:19
- Modify Date: 2024-01-03 21:53:55
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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.
| Name | (1R,5S)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane,hydrochloride |
|---|---|
| Synonyms |
DOV 21,947
AMITIFADINE HYDROCHLORIDE UNII-R01R720TVG EB-1010 Amitifadine hydrochloride (USAN) Amitifadine HCl Amitifadine (hydrochloride) |
| 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 |
| Molecular Formula | C11H12Cl3N |
|---|---|
| Molecular Weight | 264.57900 |
| Exact Mass | 263.00400 |
| PSA | 12.03000 |
| LogP | 3.98510 |
| Storage condition | 2-8℃ |