Amitifadine
Systematic (IUPAC) name
[(1R,5S) -1-(3,4-dichlorophenyl)-3-

azabicyclo[3.1.0] hexane hydrochloride]
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
ATC code  ?
PubChem CID 11658655
ChemSpider 9833390 YesY
ChEMBL CHEMBL592374 YesY
Chemical data
Formula C11H11Cl2N.HCl
Mol. mass 264.58
SMILES eMolecules & PubChem
 YesY (what is this?)  (verify)

Amitifadine, also known as DOV 21,947 or EB-1010, is an antidepressant drug being developed by Euthymics Bioscience Inc. which is currently in clinical trials.[1] It is a so-called triple re/uptake inhibitor (TUI) or SNDRI.[1]

It is the (+)-enantiomer of DOV 216,303. IC50 values for SERT, NET, and DAT are Ki 99 nM, 262 nM, and 213 nM.[1]. The IC50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively


DOV.gif
Com Uptake Binding
5-HT NE DA SERT NET DAT
216303 14 20 78 190 380 190
21947 12 23 96 100 260 210
102677 130 100 130 740 1000 220

Amitifadine reduces the duration of immobility in the forced swim test in rats with an oral minimum effective dose (MED) of 5 mg/kg. This anti-depressant-like effect manifests in the absence of significant increases in motor activity at doses of up to 20 mg/kg. Amitifadine also produces a dose-dependent reduction in immobility in the tail suspension test, with an oral MED of 5 mg/kg. In microdialysis studies, amitifadine increased extracellular levels of serotonin, norepinephrine and dopamine in brain regions and did not induce hyperactivity in rats.[2] Results in a small clinical trial indicated that amitifadine had statistically significant antidepressant depressant and was well tolerated.[3]

References [link]

  1. ^ a b c Skolnick, P.; Popik, P.; Janowsky, A.; Beer, B.; Lippa, A. S. (2003). "Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor". European Journal of Pharmacology 461 (2–3): 99–104. DOI:10.1016/S0014-2999(03)01310-4. PMID 12586204.  edit
  2. ^ Golembiowska, K.; Kowalska, M.; Bymaster, F. P. (2012). "Effects of the triple reuptake inhibitor amitifadine on extracellular levels of monoamines in rat brain regions and on locomotor activity". Synapse 66 (5): 435–444. DOI:10.1002/syn.21531. PMID 22213370.  edit
  3. ^ Tran, P.; Skolnick, P.; Czobor, P.; Huang, N. Y.; Bradshaw, M.; McKinney, A.; Fava, M. (2012). "Efficacy and tolerability of the novel triple reuptake inhibitor amitifadine in the treatment of patients with major depressive disorder: A randomized, double-blind, placebo-controlled trial". Journal of Psychiatric Research 46 (1): 64–71. DOI:10.1016/j.jpsychires.2011.09.003. PMID 21925682.  edit
GABAA PAMs
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α2δ VDCC Blockers
5-HT1A Agonists
H1 Antagonists
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
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M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)


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