• Bulletin of the Korean Chemical Society
• /
• 제23권10호
• /
• pp.1439-1444
• /
• 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.

• 한국임상약학회지
• /
• 제32권4호
• /
• pp.313-320
• /
• 2022

Background: Serotonin syndrome is a life-threatening disease if not appropriately treated. This study aimed to investigate the prescription status of contraindicated drug combinations that cause serotonin syndrome and identify the related factors. Methods: A cross-sectional study was conducted using nationwide claims data. Adult patients taking serotonergic drugs with Parkinson's disease or mental disorders were selected. Based on international medical databases (MDBs) and the Korean Drug Utilization Review (DUR), the status of prescribing contraindicated drug combinations that induce serotonin syndrome, the related factors, and the difference between international MDBs and the Korean DUR were analyzed. Results: Of the 49,773 study subjects, 163 (0.3%) were prescribed contraindicated serotonergic drug combinations based on international MDBs, and among them, only 105 (64.4%) were contraindicated by the Korean DUR. Positive influencing factors for prescribing contraindicated drug combinations include patient age between 65 and 74 and physician's specialties (neurologists, and orthopedists). Negative influencing factors were physician's specialty (internists) and medical institution (primary institutions). Conclusion: Despite the implementation of DUR, 3 out of 1,000 study subjects received contraindicated drug combinations that caused serotonin syndrome. Hence, it is necessary to comply with the DUR and improve it in accordance with international MDBs.

• 생물정신의학
• /
• 제5권2호
• /
• pp.162-165
• /
• 1998

The serotonin reuptake inhibitors(SRIs) and the serotonin selective reuptake inhibitors(SSRIs) are considered the first choice agents for pharmacologic treatment of obsessive-compulsive disordr(OCD). However, many patients with OCD experience little or no improvement in their symptoms when treated with SRIs or SSRIs. Patients who have experienced a partial or no response to an SRI/SSRI at 10 to 12 weeks are often considered for augmentation strategies. Nearly every class of psychotropic medications has been tried in an open fashion, though augmentation strategies have been somewhat disappointing.

• Natural Product Sciences
• /
• 제4권2호
• /
• pp.91-94
• /
• 1998

In folklore medicine Drymaria cordata Willd (Family-Caryophyllaceae) is reported to have laxative and anti-febrile properties along with anti-inflammatory activities. Sikkimis used this plant to treat all these ailments. The anti-inflammatory effect of the methanol extract of D. cordata was investigated against carrageenin, histamine, serotonin, dextran and $PGE_1$ induced rat hind paw oedema. It exhibited significant anti-inflammatory activity against all these phlogestic agents except $PGE_1$ in the order of carrageenin > serotonin > histamine. All these effects were compared with standard drug phenylbutazone in both the acute and chronic experimental models in albino rats.

• 통합자연과학논문집
• /
• 제9권2호
• /
• pp.128-135
• /
• 2016

5-hydroxytryptamine (serotonin) receptor ($5-HT_7R$) 7 is one of G-Protein coupled receptors, which is activated by the neurotransmitter Serotonin. After activation by serotonin, $5-HT_7$ activates the production of the intracellular signaling molecule cyclic AMP. $5-HT_7$ receptor has been found to be involved in the pathophysiology of various disorders. It is reported that $5-HT_7$ receptor antagonists can be used as antidepressant agents. In this study, we report the important structural and chemical parameters for 2-methoxyphenylpiperazinylakanamides as $5-HT_7R$ inhibitors. A 3D QSAR study based on comparative molecular field analysis (CoMFA) was performed. The best predictions were obtained for the best CoMFA model with $q^2$ of 0.594 with 6 components, $r^2$ of 0.986, Fisher value as 60.607, and an estimated standard error of 0.043. The predictive ability of the test set was 0.602. Results obtained the CoMFA models suggest that the data are well fitted and have high predictive ability. The contour maps are generated and studied. The contour analyses may serve as tool in the future for designing of novel and more potent $5-HT_7R$ derivatives.

• 생물정신의학
• /
• 제3권1호
• /
• pp.22-29
• /
• 1996

The introduction of chlorpromazine in the 1950's revolutionized the treatment of schizophrenia and ultimately led to the development of selective $D_2$ antagonists such as haloperidol, a goal in keeping with the prevalent theories at that time. However, limitations in the efficacy of these agents, a growing awareness of their side effects, and theoretical shifts in our understanding of schizophrenia have encouraged ongoing efforts to develop better 'atypical' antipsychotics. Clozapine, and subsequently risperidone, represent examples of these novel compounds, both of which incorporate shared serotonin-dopamine antagonism(SDA). The next years will be dominated by further development of SDA compounds, although a number of other lines of investigation are also being pursued.

• The Korean Journal of Pain
• /
• 제33권4호
• /
• pp.318-325
• /
• 2020

Background: Chemotherapy-induced peripheral neuropathy (CIPN) is a major side effect of anti-cancer drugs. Neurotensin receptors (NTSRs) are widely distributed within the pain circuits in the central nervous system. The purpose of this study was to determine the role of NTSR1 by examining the effects of an NTSR1 agonist in rats with CIPN and investigate the contribution of spinal serotonin receptors to the antinociceptive effect. Methods: Sprague-Dawley rats (weight 150-180 g) were used in this study. CIPN was induced by injecting cisplatin (2 mg/kg) once a day for 4 days. Intrathecal catheters were placed into the subarachnoid space of the CIPN rats. The antiallodynic effects of intrathecally or intraperitoneally administered PD 149163, an NTSR1 agonist, were evaluated. Furthermore, the levels of serotonin in the spinal cord were measured by high-performance liquid chromatography. Results: Intrathecal or intraperitoneal PD 149163 increased the paw withdrawal threshold in CIPN rats. Intrathecal administration of the NTSR1 antagonist SR 48692 suppressed the antinociceptive effect of PD 149163 given via the intrathecal route, but not the antinociceptive effect of intraperitoneally administered PD 149163. Intrathecal administration of dihydroergocristine, a serotonin receptor antagonist, suppressed the antinociceptive effect of intrathecally administered, but not intraperitoneally administered, PD 149163. Injecting cisplatin diminished the serotonin level in the spinal cord, but intrathecal or intraperitoneal administration of PD 149163 did not affect this reduction. Conclusions: NTSR1 played a critical role in modulating CIPN-related pain. Therefore, NTSR1 agonists may be useful therapeutic agents to treat CIPN. In addition, spinal serotonin receptors may be indirectly involved in the effect of NTSR1 agonist.

• 동의생리병리학회지
• /
• 제36권2호
• /
• pp.54-58
• /
• 2022

This study aimed to investigate the anti-stress function of Aucklandiae Radix (AR) and Cyperi Rhizoma (CR). The essential oils used in the experiment were extracted from AR and CR using Steam Distillation Extraction and Super critical CO₂ extraction. To observe the effects of sample administration, we measured feed intake, leukocytes, red blood cells, hemoglobin, platelets, serum serotonin content, immobility time, climbing time, and swimming time in mice subjected to chronic restraint stress as behavioral changes. The average body weight of all experimental groups increased than the average body weight of the control group. The immobility and climbing times of experimental groups A and B administered with supercritical extraction samples were shorter than those of the other experimental groups and the control group, and the swimming time was longer. The serotonin content in the blood of all experimental groups decreased compared to the normal group, and the serotonin content of the control group was increased. The authors suggest that Korean herbal medicines AR and CR may be utilized as anti-stress flavoring agents based on the above results.

• 생물정신의학
• /
• 제23권1호
• /
• pp.1-11
• /
• 2016

Development of various antidepressants such as monoamine oxidase inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitors, and noradrenergic and specific serotonergic antidepressant has led to a tremendous progression of pharmaceutical treatment for depression, but still there are some limitations of current antidepressants, such as treatment-resistant depression and delayed onset of antidepressants. The pathogenesis of depression is unclear because depression is a heterogeneous disease state, and the mechanisms of antidepressants remain uncertain as well. Nevertheless, in an attempt to develop novel antidepressants, some trials have been conducted based on the potential biological mechanism discovered in the numerous research results. This review will provide information about the potential novel antidepressants and the current states of clinical studies using them. In particular, some potential novel antidepressants anti-inflammatory agents, antioxidants, anticholinergics, modulators of Hypothalamic Pituitary Adrenal Axis, glutamate, and opioid systems, as well as some neuropeptides such as susbstance P, neuropeptide Y, and galanin will be discussed.

• Biomolecules & Therapeutics
• /
• 제6권3호
• /
• pp.303-311
• /
• 1998

The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.