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
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]
Referencesedit
^ abcdPopik P, Krawczyk M, Golembiowska K, Nowak G, Janowsky A, Skolnick P, et al. (2006). "Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677". Cellular and Molecular Neurobiology. 26 (4–6): 857–73. doi:10.1007/s10571-006-9012-5. PMID 16636898. S2CID 34989472.
^McMillen BA, Shank JE, Jordan KB, Williams HL, Basile AS (November 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): 1866–71. doi:10.1111/j.1530-0277.2007.00513.x. PMID 17908267.
This psychoactive drug-related article is a stub. You can help Wikipedia by expanding it.
psychoactive, drug, being, developed, merck, currently, clinical, trials, triple, reuptake, inhibitor, serotonin, norepinephrine, dopamine, reuptake, inhibitor, sndri, enantiomer, enantiomer, amitifadine, legal, statuslegal, statusus, investigational, drugiden. DOV 102 677 is a psychoactive drug being developed by Merck and is currently in clinical trials 1 It is a triple reuptake inhibitor TRI or serotonin norepinephrine dopamine reuptake inhibitor SNDRI 1 It is the enantiomer of DOV 216 303 and its enantiomer is DOV 21 947 amitifadine DOV 102 677Legal statusLegal statusUS Investigational New DrugIdentifiersIUPAC name 1S 5R 1 3 4 dichlorophenyl 3 azabicyclo 3 1 0 hexaneCAS Number410074 75 8 YPubChem CID11637190ChemSpider9811932 NUNIINS8NWQ6NF4ChEMBLChEMBL488638 NCompTox Dashboard EPA DTXSID50469820Chemical and physical dataFormulaC 11H 11Cl 2NMolar mass228 12 g mol 13D model JSmol Interactive imageSMILES C1 C H 2 C 1 CNC2 C3 CC C C C3 Cl ClInChI 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 NKey BSMNRYCSBFHEMQ GZMMTYOYSA N N N Y what is this verify 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 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 edit a b c d Popik P Krawczyk M Golembiowska K Nowak G Janowsky A Skolnick P et al 2006 Pharmacological profile of the triple monoamine neurotransmitter uptake inhibitor DOV 102 677 Cellular and Molecular Neurobiology 26 4 6 857 73 doi 10 1007 s10571 006 9012 5 PMID 16636898 S2CID 34989472 McMillen BA Shank JE Jordan KB Williams HL Basile AS November 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 71 doi 10 1111 j 1530 0277 2007 00513 x PMID 17908267 nbsp This psychoactive drug related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title DOV 102 677 amp oldid 1196047003, wikipedia, wiki, book, books, library,
