From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies

Jonas Nii Nortey Eildal; Jacob Andersen; Anders Skov Kristensen; Anne Marie Jørgensen; Benny Bang-Andersen; Morten Jørgensen; Kristian Strømgaard

doi:10.1021/jm701602g

From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies

Jonas Nii Nortey Eildal, Jacob Andersen, Anders Skov Kristensen, Anne Marie Jørgensen, Benny Bang-Andersen, Morten Jørgensen, Kristian Strømgaard

50 Citationer (Scopus)

Abstract

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.

Originalsprog	Engelsk
Tidsskrift	Journal of Medicinal Chemistry
Vol/bind	51
Udgave nummer	10
Sider (fra-til)	3045-3048
ISSN	0022-2623
DOI	https://doi.org/10.1021/jm701602g
Status	Udgivet - 2008

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Eildal, J. N. N., Andersen, J., Kristensen, A. S., Jørgensen, A. M., Bang-Andersen, B., Jørgensen, M., & Strømgaard, K. (2008). From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies. Journal of Medicinal Chemistry, 51(10), 3045-3048. https://doi.org/10.1021/jm701602g

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 et al.

I: Journal of Medicinal Chemistry, Bind 51, Nr. 10, 2008, s. 3045-3048.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

Eildal, JNN, Andersen, J, Kristensen, AS, Jørgensen, AM, Bang-Andersen, B, Jørgensen, M & Strømgaard, K 2008, 'From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies', Journal of Medicinal Chemistry, bind 51, nr. 10, s. 3045-3048. https://doi.org/10.1021/jm701602g

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abstract = "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.",

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note = "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",

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AU - Jørgensen, Anne Marie

AU - Bang-Andersen, Benny

AU - Jørgensen, Morten

AU - Strømgaard, Kristian

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From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: Synthesis and structure-activity relationship studies

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