DOV-102,677

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DOV-102,677
Legal status
Legal status
Identifiers
  • (1S,5R)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane
JSmol)
  • C1[C@@H]2[C@]1(CNC2)C3=CC(=C(C=C3)Cl)Cl
  • InChI=1S/C11H11Cl2N/c12-9-2-1-7(3-10(9)13)11-4-8(11)5-14-6-11/h1-3,8,14H,4-6H2/t8-,11+/m0/s1 ☒N
  • Key:BSMNRYCSBFHEMQ-GZMMTYOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

DOV-102,677 is a

serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[1] It is the (−)-enantiomer of DOV-216,303, and its (+)-enantiomer is DOV-21,947 (amitifadine
).

Instead of being developed for depression, DOV-102,677 is being developed for the treatment of alcoholism.[2]

IC50 values for the SERT, NET and DAT are 129 nM, 103 nM, and 133 nM.[1]

DOV stereochemistry
DOV stereochemistry
Compound Uptake Binding
5-HT NE DA SERT NET DAT
DOV-216,303 14 20 78 190 380 190
Amitifadine 12 23 96 100 260 210
DOV-102,677 130 100 130 740 1000 220

DOV-102,677 (20 mg/kg IP) increased extracellular levels of dopamine and serotonin in the prefrontal cortex to 320 and 280% above baseline 100 min after administration. Dopamine levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. Norepinephrine levels increased linearly to a maximum of 348% at 240 min post-dosing.[1]

References

  1. ^
    S2CID 34989472
    .
  2. PMID 17908267
    .


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