Clickable photoaffinity ligands for the human serotonin transporter based on the selective serotonin reuptake inhibitor (S)-citalopram
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چکیده
منابع مشابه
Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram
Three photoaffinity ligands (PALs) for the human serotonin transporter (hSERT) were synthesized based on the selective serotonin reuptake inhibitor (SSRI), (S)-citalopram (1). The classic 4-azido-3-iodo-phenyl group was appended to either the C-1 or C-5 position of the parent molecule, with variable-length linkers, to generate ligands 15, 22, and 26. These ligands retained high to moderate affi...
متن کاملSelective Serotonin Reuptake Inhibitor Citalopram
Background and Purpose The aim of the study was to investigate the efficacy and safety of the selective serotonin reuptake inhibitor citalopram in treating poststroke depression, since available treatments are usually poorly tolerated. Methods A 6-week double-blind, placebo-controlled trial was undertaken. Diagnosis and outcome were determined using the Hamilton Depression Scale, and unwanted e...
متن کاملThe selective serotonin reuptake inhibitor citalopram induces the storage of serotonin in catecholaminergic terminals.
We investigated whether selective inhibition of serotonin (5-hydroxytryptamine; 5-HT) transporter with citalopram leads to accumulation of 5-HT in catecholaminergic neurons. In the rabbit olfactory tubercle, citalopram (1-10 microM) inhibited [(3)H]5-HT uptake; however, the maximal degree of inhibition achieved was 70%. Addition of nomifensine (1-10 microM) was required for complete inhibition ...
متن کاملSerotonin syndrome: fentanyl and selective serotonin reuptake inhibitor interactions.
Serotonin syndrome is a rare but potentially fatal adverse drug reaction associated with increased serotonergic activity in the central nervous system. It is characterized by a triad of symptoms, which include altered mental status, neuromuscular hyperactivity, and autonomic instability or hyperactivity. Due to the potential of rapid onset, it is important for clinicians to recognize the signs ...
متن کاملSelective Serotonin Reuptake Inhibitors
It has long been postulated that a deficiency in CNS serotonergic activity is the cause of, or a predisposing factor for, depression. [1] However, the evidence for this association is largely circumstantial and it certainly does not represent an adequate and full model for depression, probably due to there being multiple aetiological factors. [2] Some pharmacological trial data also cast doubt ...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2018
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2018.09.029