• The Korean Journal of Malacology
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• v.25 no.1
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• pp.15-22
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• 2009

Because it is known that bivalve hearts contain various modulatory systems activated by neuroendocrine substances, it was examined whether different classes of endogenous and synthetic drugs of neuroendocrinological importance can influence cardiac functions of the Pacific oyster Crassostrea gigas. Cholinergically active agents acetylcholine and carbachol increased heart rates while diminishing cardiac contractility. Adrenergically active substances norepinephrine (NE) and epinephrine (Epi) also induced heart rate increase and contractility decrease. An $\alpha_1$-adrenergic receptor-selective agonist phenyephrine (PE) failed to modulate either parameter. The Epi-induced heart rate increase and contractile depression were both blocked significantly by non-selective $\beta_1/\beta_2$-adrenergic antagonist propranolol. A $\beta_1$-selective antagonist atenolol prevented Epi-induced heart rate decrease but not the contractile depression, suggesting possible $\beta_2$ receptors for Epi-induced contractile depression. The three autacoids examined exerted discrete responses: histamine increased heart rate and depressed contraction; $\gamma$-amino-butyric acid increased both parameters; serotonin failed to change either parameter. The 5 piscine anesthetic agents examined, MS-222, benzocaine, quinaldine, urethane, pantocaine and pentobarbital, all failed to influence the cardiac function of oysters. Collectively, activities of neuroendocrinologically acting agents in mammals showed unexpected and distinct activities from those in mammalian cardiovascular systems. These results obtained from substances of different physiological functions can serve as a basis for understanding neuroendocrine control of the heart function in Pacific oyster.

• The Korean Journal of Pain
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• v.33 no.2
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• pp.108-120
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• 2020

From the perspective of the definition of pain, pain can be divided into emotional and sensory components, which originate from potential and actual tissue damage, respectively. The pharmacologic treatment of the emotional pain component includes antianxiety drugs, antidepressants, and antipsychotics. The anti-anxiety drugs have anti-anxious, sedative, and somnolent effects. The antipsychotics are effective in patients with positive symptoms of psychosis. On the other hand, the sensory pain component can be divided into nociceptive and neuropathic pain. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioids are usually applied for somatic and visceral nociceptive pain, respectively; anticonvulsants and antidepressants are administered for the treatment of neuropathic pain with positive and negative symptoms, respectively. The NSAIDs, which inhibit the cyclo-oxygenase pathway, exhibit anti-inflammatory, antipyretic, and analgesic effects; however, they have a therapeutic ceiling. The adverse reactions (ADRs) of the NSAIDs include gastrointestinal problems, generalized edema, and increased bleeding tendency. The opioids, which bind to the opioid receptors, present an analgesic effect only, without anti-inflammatory, antipyretic, or ceiling effects. The ADRs of the opioids start from itching and nausea/vomiting to cardiovascular and respiratory depression, as well as constipation. The anticonvulsants include carbamazepine, related to sodium channel blockade, and gabapentin and pregabalin, related to calcium blockade. The antidepressants show their analgesic actions mainly through inhibiting the reuptake of serotonin or norepinephrine. Most drugs, except NSAIDs, need an updose titration period. The principle of polypharmacy for analgesia in case of mixed components of pain is increasing therapeutic effects while reducing ADRs, based on the origin of the pain.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.20 no.2 s.33
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• pp.142-150
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• 2007

Objectives : This study was carried out to investigate the latest study tendency in mouse model of skin pruritus published since 2005 and to arrange various experimental methods. Methods : We examined the journal(such as Experimental dermatology and British journal of dermatology) and in Pubmed since 2005, regarded pruritus and scratching behavior model as key words. Results and Conclusion : 1. BALB/c, hairless, NC/Nga and ICR mice were the most used in scratching behavior model. According to scratching-induced agents. we need to select experimental mice. 2. There are various methods inducing skin pruritus; by cohabitation with NC/Nga mice having severe skin lesions, by injection intradermally(or subcutaneously) with agent inducing inflammation, by inducing contact dermatitis with TNCB, TNFB, destruction of skin barrier and by transgenic mice. 3. Injection intradermally(or subcutaneously) with agent inducing inflammation is the most used out of methods inducing skin pruritus. Compound 48/80, histamine, substance P and others(chloroquine, serotonin, carrageenin, TPA etc.) were included in agents inducing inflammation and pruritus in skin pruritus model. 4. Video camera, SCLABA system, MicroAct and acoustic evaluation system were included in evaluation methods of scratching behavior mouse model.

• Korean Journal of Biological Psychiatry
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• v.11 no.1
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• pp.14-25
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• 2004

The current understanding of the mechanisms of pharmacotherapy for depression is characterized by an emphasis on increasing synaptic availability of serotonin, noradrenaline, and possibly dopamine, while minimizing side effects. The acute effects of current available effective antidepressants include blocking selective serotonin or noradrenaline reuptake, alpha2 autoreceptors or monoamine oxidase. Although efficacious, current treatments often produce partial or limited symptomatic improvement rather than remission. While current pharmacotherapies target monoaminergic systems, distinct neurobiological underpinnings and other systems are likely involved in the pathogenesis of depression. Recently, several promising hypotheses of depression and antidepressant action have been formulated. These hypotheses are largely based on dsyregulation of neural plasticity, CREB, BDNF, corticotropin-releasing factor, glucocorticoid, hypothalamic-pituitary adrenal axis and cytokines. Based on these new theories and hypotheses of depression, a number of new and novel agents, including corticotropin-releasing factor antagonists, antiglucocorticoids, and substance P antagonists show a considerable promise for refining treatment options for depression. In this article, the current available pharmacotherapies, current understanding of neurobiology and pathogenesis of depression and new and promising directions in pharmacological research on depression will be discussed.

• Natural Product Sciences
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• v.19 no.4
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• pp.337-341
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• 2013

The effects of gypenosides (GPS) on electric footshock (EF)-induced acute stress in mice were investigated. Mice were treated orally with GPS (30-400 mg/kg) once a day for 5 days. After 2 days of GPS treatment, mice were exposed to EF stimuli (intensity, 2 mA; interval, 10 s; duration, 3 min) for acute stress for 3 days. Spontaneous locomotor activity was increased by acute EF stress, which was decreased by treatment with GPS (100 and 400 mg/kg). In addition, the increased levels of dopamine and serotonin by acute EF stress in the brain were reduced by treatment with GPS (100 and 400 mg/kg). The serum levels of corticosterone increased by acute EF stress were also reduced by GPS (100 and 400 mg/kg). These results suggest that GPS shows the ameliorating effects on acute EF stress by modulating the activity of dopaminergic and serotonergic neurons, and the serum levels of corticosterone. Clinical trials of GPS need to be conducted further so as to develop promising anti-stress agents.

• The Journal of Korean Medicine
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• v.28 no.3 s.71
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• pp.165-172
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• 2007

Objectives : To find antipruritic herbal medicines, we screened the water extracts of four herbal medicines which have been frequently prescribed to treat dermatologic diseases in oriental medicine. Methods : Water extracts of Bupleuri Radix, Scutellariae Radix, Cimicifugae Rhizoma and Puerariae Radix were administered at a dose of 300 mg/kg to male ICR mice. 1 hour later, serotonin hydrochloride dissolved in physiologic saline at a concentration of 100 nmol / 50${\mu}{\ell}$ was administered intradermally to the nape of the neck at a dose of 50${\mu}{\ell}$. Then the scratching behavior was observed. Dry skin pruritus was induced with cutaneous application of acetone / ether (1:1) mixture and water (AEW) to the rostral back of male ICR mice, twice a day for 5 days. 14 hours after the last application, the most effective material in the first experiment was administered perorally at doses of 75, 150, 300, 600 and 1200 mg/kg. 1 hour later, the scratching behavior was observed. Results : Water extracts of Puerariae Radix significantly inhibited the serotonin-induced scratching behavior and the mean of scratching bouts was reduced by half compared with the control group. Bupleuri Radix group also showed a 29% decrease in the mean of scratching bouts, but there was no statistical significance. Water extracts of Puerariae Radix also inhibited the AEW-induced scratching behavior, in a dose-dependent manner. The dose of 150 mg/kg showed the highest and statistically significant antipruritic effect. Conclusions : These results suggest that Puerariae Radix and its constituents have antipruritic effect, and are new candidates as antipruritic agents.

• Journal of Ginseng Research
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• v.10 no.2
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• pp.123-132
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• 1986

The pepsinogen secretion was stimulated by the cholecystokinin, caerulein, isoproterenol, and carbachol, respectively. But it was increased slightly and returned to control level by the combiantions of total saponin with each above the agents. Even though the atropine had the inhibition effect, the pepsinogen secretion was recovered to normal level from depressed condition by the combination of the atropine with total saponin. Propranolol showed the same pattern as atropine, too. On the other hand, the pepsinogen secretion was stimulated by the DBcAMP alone, but decreased to control level by the combination with the total saponin. In the case of DBcGMP, the pepsinogen secretion was decreased by itself, but stimulated the above control level by the combination with total saponin. Histamine alone had little effect on the pepsinogen secretion, but when combinated with total saponin, the pepsinogen secretion was increased. Serotonin alone and with total saponin, had no effect respectively, From the above results, the total saponin may have the normalization action stimulating or decreasing the pepsinogen secretion to the control level.

• Journal of Medicine and Life Science
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• v.18 no.3
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• pp.49-55
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• 2021

Atypical antipsychotics are more effective than typical antipsychotics and have fewer side effects such as tardive dyskinesia and extrapyramidal symptoms; therefore, prescriptions of atypical antipsychotics are increasing. However, recently, it has been reported that atypical antipsychotics have a higher incidence of diabetes, hyperglycemia, and obesity than typical antipsychotics. Atypical antipsychotics induce obesity-inhibiting appetite-related receptors such as serotonin and dopamine. Decreased exercise due to improving psychotic symptoms, and genetic characterictics can also cause weight gain. Hyperglycemia and hypoglycemia were another metabolic problem related to treatment with atypical antipsychotics. The mechanisms of hyperglycemia were mainly related obesity, decreased anorexigenic hormones, and increased insulin resistance in multiple organs. There are also reports that genes related to diabetes have an effect on the incidence of diabetes mellitus treated with atypical antipsychotics. On the other hand, although it is not clear why hypoglycemia occurs, it documented in case reports all over the world. There are more reports of atypical antipsychotics than typical antipsychotics and these are frequently reported in Asians. Further research on the mechanism of hypoglycemia related to atypical antipsychotics is strongly recommended.

• 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.

• Biomolecules & Therapeutics
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• v.30 no.2
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• pp.191-202
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• 2022

Tetrazoles were designed and synthesized as potential inhibitors of triple monoamine neurotransmitters (dopamine, norepinephrine, serotonin) reuptake based on the functional and docking simulation of compound 6 which were performed in a previous study. The compound structure consisted of a tetrazole-linker (n)-piperidine/piperazine-spacer (m)-phenyl ring, with tetrazole attached to two phenyl rings (R1 and R2). Altering the carbon number in the linker (n) from 3 to 4 and in the spacer (m) from 0 to 1 increased the potency of serotonin reuptake inhibition. Depending on the nature of piperidine/piperazine, the substituents at R1 and R2 exerted various effects in determining their inhibitory effects on monoamine reuptake. Docking study showed that the selectivity of tetrazole for different transporters was determined based on multiple interactions with various residues on transporters, including hydrophobic residues on transmembrane domains 1, 3, 6, and 8. Co-expression of dopamine transporter, which lowers dopamine concentration in the biophase by uptaking dopamine into the cells, inhibited the dopamine-induced endoctytosis of dopamine D₂ receptor. When tested for compound 40 and 56, compound 40 which has more potent inhibitory activity on dopamine reuptake more strongly disinhibited the inhibitory activity of dopamine transporter on the endocytosis of dopamine D₂ receptor. Overall, we identified candidate inhibitors of triple monoamine neurotransmitter reuptake and provided a theoretical background for identifying such neurotransmitter modifiers for developing novel therapeutic agents of various neuropsychiatric disorders.