DOV-102,677

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DOV-102,677
DOV-102,677 structure.png
Systematic (IUPAC) name
(5R)-5-(3,4-dichlorophenyl)bicyclo[3.1.0]hexane
Clinical data
Identifiers
None
Chemical data
Formula C11H11Cl2N
228.118 g/mol
 YesY (what is this?)  (verify)

DOV 102,677 is a psychoactive drug being developed by Merck as an antidepressant and is currently in clinical trials.[1] It is a so-called triple (re)uptake inhibitor (TUI), or 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.svg
Compound Uptake Binding
5-HT NE DA SERT NET DAT
216,303 14 20 78 190 380 190
21,947 12 23 96 100 260 210
102,677 130 100 130 740 1000 220

"DOV 102,677 (20 mg/kg IP) increased extracellular levels of DA and 5-HT in the prefrontal cortex to 320 and 280% above baseline 100 min after administration. DA levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. NE levels increased linearly to a maximum of 348% at 240 min post-dosing."[1]

References[edit]

  1. ^ a b c d Popik, P.; Krawczyk, M.; Golembiowska, K.; Nowak, G.; Janowsky, A.; Skolnick, P.; Lippa, A.; Basile, A. (2006). "Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677". Cellular and molecular neurobiology 26 (4–6): 857–873. doi:10.1007/s10571-006-9012-5. PMID 16636898.  edit
  2. ^ Mcmillen, B.; Shank, J.; Jordan, K.; Williams, H.; Basile, A. (2007). "Effect of DOV 102,677 on the volitional consumption of ethanol by Myers' high ethanol-preferring rat". Alcoholism, clinical and experimental research 31 (11): 1866–1871. doi:10.1111/j.1530-0277.2007.00513.x. PMID 17908267.  edit