• Advances in Traditional Medicine
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• v.8 no.1
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• pp.73-80
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• 2008

The objective of the present study was to assess the antipsychotic and antidiarrhoeal activities of ethanolic extract of roots of Rubia cordifolia in mice and rats. The antipsychotic activity of ethanolic extract of roots of Rubia cordifolia (ERC) was evaluated by observing its effect on amphetamineinduced stereotyped behavior in mice. Effect of ERC was also studied on motor coordination and locomotion in mice. The antidiarrhoeal activity was evaluated using castor oil-induced diarrhoea and excretion of sodium and potassium ions in the intestinal secretion in rats and gastrointestinal transit in mice. The ERC inhibited amphetamine-induced stereotyped behaviour, diminished locomotion and impaired motor coordination. ERC inhibited castor oil-induced diarrhoea, decreased both sodium and potassium excretion in the intestine and decreased gastrointestinal transit. Thus the present study confirms the anti-diarrhoeal activity of Rubia cordifolia. Further studies are necessary to evaluate the potential of Rubia cordifolia as an antipsychotic.

• Bulletin of the Korean Chemical Society
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• v.30 no.7
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• pp.1445-1451
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• 2009

New benzotriazoles (5-8) or dibenzodiazepine derivatives (11-18) were synthesized starting from 3-[(2-amino- 4,5-disubstitutedphenyl)amino]-5,5-disubstitutedcyclohex-2-enones (1-4) through internal coupling of their diazonium salts or internal Mannich reaction in the presence of aromatic aldehydes. Pharmacological evaluation of benzotriazole and dibenzodiazepine derivatives for their clozapine-like properties revealed that dibenzodiazepine 11 bearing 4-bromophenyl group exhibited the same antipsychotic activity as the reference drug clozapine while the activity of benzotriazole 7 was 25% lesser than that of clozapine. Moreover, compounds 7 and 11 did not show significant CNS depressant activity as well as no or slight neurotoxicity on contrast to clozapine when tested in mice using forced swim, rotarod and horizontal screen tests.

• Korean Journal of Biological Psychiatry
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• v.4 no.1
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• pp.48-53
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• 1997

CV(bDAT) cell line, expressing dopamine transporter stably, has been established by transfection of CV-1 cells with bovine dopamine transporter cDNA. Using CV(bDAT) cells, the effects of various antipsychotic drugs on dopamine uptake activity were investigated. All of antipsychotic drugs tested, inhibited the [$^3H$]dopamine uptake into CV(bDAT) cells with $IC_{50}s$ in the low to mid micromolar range, implying that antipsychotic drugs may produce overflow of dopamine in the synaptic cleft of dopaminergic neuron.

• Research in Community and Public Health Nursing
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• v.29 no.1
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• pp.76-86
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• 2018

Purpose: The purpose of study was to examine the relationship between obesity and its associated factors (psychiatric symptom, duration of illness, type of medication, physical activity, dietary habits, depressive symptom, and stress) in patients with chronic mental illness registered to community mental health welfare centers. Methods: This was a cross-sectional correlation study using a convenience sampling. A total of 392 participants were recruited from community mental health welfare centers. The obtained data were analyzed using binary and multinomial logistic regression. Results: Atypical antipsychotic medication, duration of illness, dietary habits (overeating, and drinking instant coffee) were significantly contributed variables into body mass index (BMI) obesity. Atypical antipsychotic medication and instant coffee were significantly related to abdominal obesity. Conclusion: These results emphasized the needs of tailored obesity-preventive management for the community-dwelling patients with chronic mental illness, topically focusing on the administration of atypical antipsychotic medication, duration of illness, and dietary habits.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.17 no.1
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• pp.152-158
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• 2016

Glutamate is one of the major excitatory neurotransmitters in the central nervous system of vertebrates. Human GDH (hGDH) is the enzyme that regulates the glutamate metabolism and its expression is higher in the brains of schizophrenia patients than in normal subjects. This study examined the changes in the hGDH enzymatic activity caused by antipsychotic drugs (haloperidol, risperidone, (${\pm}$)-sulpride, chlopromazine hydrochloride, melperone, (${\pm}$)butaclamol, domperidone, clozapine) related to schizophrenia. First of all, hGDH isozymes (hGDH1, hGDH2) were synthesized by genetic recombination. As a result of the enzyme assay, haloperidol, (${\pm}$)-sulpride, melperone and clozapine had an inhibitory effect on the hGDH isozymes. In addition, haloperidol showed a non-competitive inhibition against the substrate, 2-oxoglutarate. In contrast, it showed an uncompetitive inhibition against another substrate, NADH. The inhibitory effect of haloperidol on hGDH2 was abolished by the presence of L-leucine, an allosteric effector of hGDH, but by not other antipsychotic drugs. These results revealed the inhibition of enzyme activity by psychotropic drugs in hGDH isoenzymes (hGDH1 and hGDH2) and the possibility that haloperidol may be used to regulate the GDH activity and glutamate concentration in the central nervous system.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1019-1022
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• 2005

Risperidone has been reported to have neuroleptic activity. In this study, risperidone was synthesized using a new method involving a stille reaction, in which 2-methyl-3-vinyl-6,7,8,9-tet­rahydropyrido[1 ,2-a]pyrimidin-4-one was synthesized (5). The chemical synthesis process was found to be simple and produced risperidone in a high yield. In addition, can be easily scaled up for large scale synthesis.

• The Korean Journal of Pharmacology
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• v.30 no.3
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• pp.343-349
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• 1994

A number of neurological syndromes(e.g. tardive dyskinesia) are developed as a consequence of chronic treatment with neuroleptics or antipsychotic agents. Despite the long and succesful use of phenothiazine derivatives and related agents in the treatment of certain states of mental disease, the mechanisms of these drugs are still poorly understood. One current hypothesis from extensive reviews is that these compounds might significantly interfere with the cyclic nucleotide system in brain (Levin and Weiss, 1977; Nowicki et al., 1991; Haley et al., 1992). Nitric oxide (NO), one of an interesting messenger molecule and aberrant transmitter, is believed to play a important role in biological functions of cyclic nucleotides in nervous system. It has been reported that calcium-dependent NO synthesis in endothelial cytosol is mediated by calmodulin which is supposed to be tightly related to pharmacological actions of antipsychotic agents. In the present study, the effect of several antipsychotic agents on the activity of NO synthesis and formation of cyclic GMP were investigated. These agents inhibited both the formation of $[^3H]L-citrulline$ and that of $[^3H]cyclic$ GMP by concentration-dependent manner, and their inhibiting patterns are so similar to that of calmodulin antagonist.

• Korean Journal of Biological Psychiatry
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• v.5 no.1
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• pp.138-141
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• 1998

Neuroleptic malignant syndrome (NMS) is an uncommon but potentially fatal idiosyncratic reaction to neuroleptics, characterized by muscular rigidity, fever, autonomic dysfunction, and altered consciousness. The major theories to explain NMS is central dopaminergic blockade, but it is unclear. Risperidone is a new antipsychotic drug, a benzisoxazole derivative that blocks dopamine $D_2$ receptor and serotonin type 2 receptor. The comparatively greater serotonin-blocking activity is believed to give risperidone the specific property of not causing any more extrapyramidal side effects than conventional antipsychotics at the optimal dose of 4-8mg/day. It is postulated that risperidone is unlikely to cause NMS. Here, we report a case of risperidone induced neuroleptic malignant syndrome.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.13 no.5
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• pp.2125-2132
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• 2012

Fluoxetine and tianeptine are commonly used as antidepressants (AD), and haloperidol and risperidone are widely used as antipsychotic drugs (APD), and it modulates various ion channels. TREK2 channel subfamily is very similar to physiological properties of TREK1 channel which can play important roles in the pathophysiology of mental disorders such as depression and schizophrenia, therefore, the pharmacological effect of psychiatric and depression drug on TREK2 channel may be similar to those of TREK1. Using the excised inside-out patch-clamp technique, we have examined the effects of APD and AD on cloned TREK2 channel expressed CHO cells. Fluoxetine (selective serotonin release inhibitor, SSRI) inhibited the TREK2 channel in a concentration-dependent manner ($IC_{50}$ $13{\mu}M$), whereas selective serotonin reuptake enhancer (SSRE) tianeptine increased without reducing the TREK2 channel activity. Haloperidol also inhibited the TREK2 channel in a concentration-dependent manner ($IC_{50}$ $44{\mu}M$), whereas even higher concentration ($100{\mu}M$) of risperidone did not completely inhibit on the activity. This study showed that TREK2 channel was preferentially blocked by fluoxetine rather than tianeptine, and inhibited by haloperidol rather than risperidone, suggesting differential effect of TREK2 channels by APD and AD may contribute to some mechanism of adverse side effects.

• Journal of muscle and joint health
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• v.22 no.2
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• pp.57-66
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• 2015

Purpose: The purpose of this study was to evaluate the incidence of postoperative delirium in elderly patients with osteoarthritis surgery and identify risk factors for its development. Methods: This study enrolled 288 patients who underwent osteoarthritis surgery in a hospital between May and November 2014. Data were collected prospectively. The Nursing Delirium Screening Scale was used to detect delirium. Multivariable logistic regression analysis was used to identify independent risk factors for postoperative delirium. Patients were also followed for outcome. Results: Postoperative delirium developed in 42 patients (14.6%). Logistic regression analysis identified old age, low physical activity, antipsychotic agents, number of catheters, and intensive care unit admission as risk factors. Worse outcomes, including increased hospital mortality, reoperation, and discharge at care facilities, occurred in subjects who developed delirium. Conclusion: Osteoarthritis surgery in elderly patients was associated with a high incidence of postoperative delirium. The results of the this study regarding patient populations vulnerable to delirium should be taken into account so that such patients could be identified preoperatively or in the immediate postoperative period.