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DOV-21,947
Systematic (IUPAC) name
(5S)-5-(3,4-dichlorocyclohexa-2,4-dien-1-yl)bicyclo[3.1.0]hexane
Identifiers
ATC code  ?
Chemical data
Formula  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status

DOV 21,947 is an antidepressant drug being developed by Merck & Co. which is currently in clinical trials.[1] It is a so-called triple re/uptake inhibitor (TUI) aka SNDRI or scari.[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]

It is closely related to DOV 102,677 and DOV 216,303.

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

DOV 21947 reduces the duration of immobility in the forced swim test in rats with an oral minimum effective dose (MED) of 5mg/kg. This anti-depressant-like effect manifests in the absence of significant increases in motor activity at doses of up to 20 mg/kg. DOV 21947 also produces a dose-dependent reduction in immobilty in the tail suspension test, with an oral MED of 5mg/kg.

References

  1. ^ a b c Skolnick, P; Popik, P; Janowsky, A; Beer, B; Lippa, AS (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







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