From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies
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From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram : Synthesis and structure-activity relationship studies. / Eildal, Jonas Nii Nortey; Andersen, Jacob; Kristensen, Anders Skov; Jørgensen, Anne Marie; Bang-Andersen, Benny; Jørgensen, Morten; Strømgaard, Kristian.
In: Journal of Medicinal Chemistry, Vol. 51, No. 10, 2008, p. 3045-3048.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram
T2 - Synthesis and structure-activity relationship studies
AU - Eildal, Jonas Nii Nortey
AU - Andersen, Jacob
AU - Kristensen, Anders Skov
AU - Jørgensen, Anne Marie
AU - Bang-Andersen, Benny
AU - Jørgensen, Morten
AU - Strømgaard, Kristian
N1 - Keywords: Animals; Benzofurans; Blood Platelets; Brain; Cell Line; Citalopram; Humans; Norepinephrine Plasma Membrane Transport Proteins; Propylamines; Rats; Recombinant Proteins; Serotonin Plasma Membrane Transport Proteins; Serotonin Uptake Inhibitors; Structure-Activity Relationship; Synaptosomes
PY - 2008
Y1 - 2008
N2 - Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity.
AB - Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1021/jm701602g
DO - 10.1021/jm701602g
M3 - Journal article
C2 - 18429609
VL - 51
SP - 3045
EP - 3048
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 10
ER -
ID: 8378305