• Bulletin of the Korean Chemical Society
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• v.23 no.10
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• pp.1439-1444
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• 2002

6-Nitroquipazine has higher binding affinity for SERT than other selective serotonin reuptake inhibitors. We have prepared 6-nitroquipazine based rhenium complexes which would lead to the development of potential SPECT imaging agents with $^{99m}Tc$ for 5-HT transporter.

• Korean Journal of Biological Psychiatry
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• v.4 no.2
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• pp.188-193
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• 1997

Along with psychosocial factors of suicide, biological backgrounds of suicide are explored by extensive works mostly on biological markers, neurobiological models, genetic bases, and relationships with aggression and violence. The biology of suicide confers on neurotransmitters in central nervous system exploring metabolites, receptor binding affinities, neuroendocrine challenge tests in brain, cerebrospinal fluid, blood and etc. The major concerns with suicide are focused mainly on serotonin system : low CSF 5-HIAA concentration, higher $5-HT_2$ receptor binding, and blunt prolactin response to fenfluramine. Postmortem study, in vivo study, genetic contributions, and some other issues such as suicidal methods, serum cholesterol, alcohol, and selective serotonin reuptake inhibitors are reviewed and discussed.

• Biomolecules & Therapeutics
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• v.20 no.6
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• pp.506-512
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• 2012

Although pruritus is the critical symptom of atopic dermatitis that profoundly affect the patients' quality of life, controlling and management of prurirtus still remains as unmet needs mainly due to the distinctive multifactorial pathogenesis of pruritus in atopic dermatitis. Based on the distinct feature of atopic dermatitis that psychological state of patients substantially influence on the intensity of pruritus, various psychotropic drugs have been used in clinic to relieve pruritus of atopic dermatitis patients. Only several psychotropic drugs were reported to show real antipruritic effects in atopic dermatitis patients including naltrexone, doxepin, trimipramine, bupropion, tandospirone, paroxetine and fluvoxamine. However, the precise mechanisms of antipruritic effect of these psychotropic drugs are still unclear. In human skin, serotonin receptors and serotonin transporter protein are expressed on skin cells such as keratinocytes, melanocytes, dermal fibroblasts, mast cells, T cells, natural killer cells, langerhans cells, and sensory nerve endings. It is noteworthy that serotonergic drugs, as well as serotonin itself, showed immune-modulating effect. Fenfluramine, fluoxetine and 2, 5-dimethoxy-4-iodoamphetamine significantly decreased lymphocyte proliferation. It is still questionable whether these serotonergic drugs exert the immunosuppressive effects via serotonin receptor or serotonin transporter. All these clinical and experimental reports suggest the possibility that antipruritic effects of selective serotonin reuptake inhibitors in atopic dermatitis patients might be at least partly due to their suppressive effect on T cells. Further studies should be conducted to elucidate the precise mechanism of neuroimmunological interaction in pruritus of atopic dermatitis.

• Korean Journal of Biological Psychiatry
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• v.4 no.2
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• pp.237-245
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• 1997

The study was designed to evaluate the significant roles of SSRI in rat of depression model. Chronic exposure to mild unpredictable stress has been found to depress the consumption of sweet 1% sucrose solutions in the Sprague-Dawley rats. We applied the variety of 11 types of stress regimens and identified depressive behaviours(developed by Willner) in 70 Sprague-Dawley rats. Rats in experiments were stratified into 6 groups, ie ; 3 kinds of SSRI(paroxetine, fluoxetine, sertraline), clomipramine, choline and saline control. Memory function was evaluated by passive avoidance learning and retention test. The authors determined how long memory retention would remain improved with 24 hour, 1 week, 2 weeks, 3 weeks, and 4 weeks at training-testing interval in depressive states of the Sprague-Dawley rats. The results were as follows ; 1) There were no significant differences between the 6 groups at the 24 hour training-testing interval. 2) The paroxetine treated group showed significant differences from the control group at the 1 week and 2 weeks training-testing interval. 3) The paroxetine and the fluoxetine treated groups showed singificant differences from the control group at 3 week training-testing interval. 4) The paroxetine and the choline treated groups showed significant differences from the control group at 4 week training-testing interval. In summary, paroxetine had an effect on long term memory processing from 1st week to 4th week. Also, fluoxetine(at 3rd week) and choline(at 4th week) had effect on long term memory processing. Sertraline, clomipramine were ineffective on memory processing during 4 weeks observation. Possible explanations why paroxetine had early effect on memory processing than the other selective serotonin reuptake inhibitors are rapid bioavailability, which is the characteristics of pharmacokinetics of paroxetine. In clinical situation, author carefully suggest that SSRI would be beneficial to improve the memory function caused by depressive neurochemical changes.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.3
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• pp.257-263
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• 2009

This study aimed to investigate whether selective serotonin reuptake inhibitors (SSRIs) attenuate brain injury and facilitate recovery following photothrombotic cortical ischemia in mice. Male ICR mice were anesthetized and systemically administered Rose Bengal. Permanent focal ischemia was induced in the medial frontal and somatosensory cortices by irradiating the skull with cold light laser. The animals were treated with fluoxetine or sertraline once a day for 14 d starting 1 h after ischemic insult. Treatment with fluoxetine and sertraline significantly reduced the infarct size. The Evans blue extravasation indices of the fluoxetine- and sertraline-treated groups were significantly lower than that of the vehicle group. Treatment with fluoxetine and sertraline shifted the lower limit of the mean arterial blood pressure for cerebral blood flow autoregulation toward normal, and significantly increased the expression of heme oxygenase-1 (HO-1) and hypoxia-inducible factor-1 ${\alpha}$ (HIF-1 ${\alpha}$) proteins in the ischemic region. These results suggest that SSRIs, such as fluoxetine and sertraline, facilitate recovery following photothrombotic cortical ischemia via enhancement of HO-1 and HIF-1 ${\alpha}$ proteins expression, thereby providing a benefit in therapy of cerebral ischemia.

• Bulletin of the Korean Chemical Society
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• v.25 no.6
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• pp.895-899
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• 2004

We have designed a new family of radioligands, 3-(amino- and hydroxymethyl)-4-(5-iodopyridin-2-ylthio)indoles, combining characteristically distinct moieties proven to impart successful binding ability in a variety of structurally diverse selective serotonin reuptake inhibitors recently published. Described in this article are the syntheses of 3-substituted 4-(5-iodopyridin-2-ylthio)-indoles, featuring successful adaptation of the modified Leimgruber-Batcho indole synthesis onto the key intermediate 1-(5-iodopyridin-2-ylthio)-2-methyl-3-nitrobenzene (6) prepared from the nucleophilic aromatic substitution of chloropyridine 7 with thiophenol 8.

• Korean Journal of Biological Psychiatry
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• v.8 no.1
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• pp.167-174
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• 2001

A 54-year old male patient who was suffering from bipolar I disorder for 19 years and was admitted to the National Bugok Mental Hospital due to a depressive episode, was referred to the Kosin University Gospel Hospital. On arrival at the emergency room, he had confused mentality with disorientation, memory impairment, hypomania, marked anxiety and hyperirritability. The change of neuromuscular activity such as ataxia, gait disturbance, tremor, shivering, myoclonus and epileptic seizures was also shown. In addition, the symptoms and signs of autonomic instability including diaphoresis, tachycardia, hypotension, fever and facial flushing were noticed. The above symptoms developed after the administration of sertraline successive to the discontinuation of fluoxetine without any washout period. The degree of severity seemed to be severe because he had epileptic seizures, fever and hypotension. He was recovered from the severe serotonin syndrome by the supportive symptomatic treatment with sodium valproate, clonazepam, lorazepam and cyproheptadine after cessation of the selective serotonin reuptake inhibitors during hospitalization. Therefore, this rare case of severe serotonin syndrome was reported and related literatures were also reviewed.

• The Korean Journal of Physiology and Pharmacology
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• v.16 no.5
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• pp.327-332
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• 2012

Sertraline is a commonly used antidepressant of the selective serotonin reuptake inhibitors (SSRIs) class. In these experiments, we have used the whole cell patch clamp technique to examine the effects of sertraline on the major cardiac ion channels expressed in HEK293 cells and the native voltage-gated $Ca^{2+}$ channels in rat ventricular myocytes. According to the results, sertraline is a potent blocker of cardiac $K^+$ channels, such as hERG, $I_{Ks}$ and $I_{K1}$. The rank order of inhibitory potency was hERG > $I_{K1}$ > $I_{Ks}$ with $IC_{50}$ values of 0.7, 10.5, and 15.2 ${\mu}M$, respectively. In addition to $K^+$ channels, sertraline also inhibited $I_{Na}$ and $I_{Ca}$, and the $IC_{50}$ values are 6.1 and 2.6 ${\mu}M$, respectively. Modification of these ion channels by sertraline could induce changes of the cardiac action potential duration and QT interval, and might result in cardiac arrhythmia.

• Korean Journal of Clinical Pharmacy
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• v.33 no.1
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• pp.62-69
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• 2023

Objective: Adherence is an important component in the treatment of various diseases, and poor adherence to antidepressants in patients with major depressive disorder is common. Non-adherence can be more prevalent in elderly patients with multiple morbidity and polypharmacy, resulting in negative treatment outcomes. The purpose of this study was to analyze adherence to antidepressants in Korean elderly patients with major depressive disorder. Method: A retrospective study was conducted using the Korean National Health Insurance claims database, and the subjects of this study were patients aged 65 or older who received at least one prescription of antidepressant monotherapy for the treatment of major depressive disorder between January 1, 2020 and June 30, 2020. Adherence was measured using the proportion of days covered at 6 months after the initial antidepressant prescription date. Logistic regression analysis was used to identify factors associated with adherence. Results: A total of 416,766 patients were finally included in the study. Over half of patients were non-adherent (52.67%) to antidepressants. According to the multivariate logistic regression analysis, national health insurance or medical aid, taking selective serotonin reuptake inhibitors or selective norepinephrine reuptake inhibitors, and having comorbidities were significantly associated with greater rates of adherence in the study subjects. The highest adherence rate was observed in patients taking vortioxetine. Conclusion: There was a considerable rate of non-adherence in Korean elderly patients with major depressive disorder. Health care professionals should try to improve adherence in elderly patients with major depressive disorder.

• Journal of the Korean Academy of Child and Adolescent Psychiatry
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• v.28 no.1
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• pp.14-19
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• 2017

Children exposed to potentially traumatic events are at risk of developing posttraumatic stress disorder (PTSD). However, the subsequent developmental course of posttraumatic stress symptoms appears to vary considerably. In this regard, some PTSD symptoms resolve without significant interventions, while for many children and adolescents, they persist until the patient receives appropriate treatment specifically designed to address PTSD and other trauma related symptoms. Evidence-based psychotherapies represent the standard of care for children with PTSD and, while psychopharmacologic interventions are utilized for many youth with posttraumatic stress symptoms and PTSD, there is little data available to guide the use of these medications in this population. However, given the structural challenges involved in disseminating and delivering evidence-based psychotherapies in all settings, prescribing clinicians should be aware of the medications whose use in children with pediatric PTSD has been studied. Herein, we review the PTSD assessment modalities, as well as the use of pharmacologic interventions in PTSD, including antiadrenergic agents, selective serotonin reuptake inhibitors and other medications.