144010-85-5Relevant articles and documents
Design, synthesis, and biological evaluation of a series of bifunctional ligands of opioids/SSRIs
Mehr-Un-Nisa,Munawar, Munawar A.,Lee, Yeon Sun,Rankin, David,Munir, Jawaria,Lai, Josephine,Khan, Misbahul A.,Hruby, Victor J.
, p. 1251 - 1259 (2015)
A series of opioid and serotonin re-uptake inhibitors (SSRIs) bifunctional ligands have been designed, synthesized, and tested for their activities and efficacies at μ-, δ- and κ opioid receptors and SSRIs receptors. Most of the compounds showed high affinities for μ- and δ-opioid receptors and lower affinities for SSRIs and κ opioid receptors. A docking study on the μ-opioid receptor binding pocket has been carried out for ligands 3-11. The ligands 7 and 11 have displayed the highest binding profiles for the μ-opioid receptor binding site with ΔGbind (-12.14 kcal/mol) and Ki value (1.0 nM), and ΔGbind (-12.41 kcal/mol) and Ki value (0.4 nM), respectively. Ligand 3 was shown to have the potential of dual acting serotonin/norepinephrine re-uptake inhibitor (SNRI) antidepressant activity in addition to opioid activities, and thus could be used for the design of multifunctional ligands in the area of a novel approach for the treatment of pain and depression.
Preparation method of escitalopram oxalate demethylation impurity
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Paragraph 0017, (2017/08/29)
The invention provides a brand-new preparation method of 1-(4- fluorophenyl)-1-(3-(fluorophenyl)propyl)-1,3-dihydroisobenzofiaran-5-formonitrile as an escitalopram oxalate process impurity. The brand-new preparation method provides a reference for qualitatively and quantitatively analyzing impurity conditions in a finished product of escitalopram oxalate, has an important effect on quality control of the escitalopram oxalate, and can promote safe medication of depressed patients.
Novel and high affinity fluorescent ligands for the serotonin transporter based on (S)-citalopram
Kumar, Vivek,Rahbek-Clemmensen, Troels,Billesb?lle, Christian B.,Jorgensen, Trine Nygaard,Gether, Ulrik,Newman, Amy Hauck
, p. 696 - 699 (2014/07/07)
Novel rhodamine-labeled ligands, based on (S)-citalopram, were synthesized and evaluated for uptake inhibition at the human serotonin, dopamine, and norepinephrine transporters (hSERT, hDAT, and hNET, respectively) and for binding at SERT, in transiently