• Title/Summary/Keyword: DAT1

Search Result 253, Processing Time 0.027 seconds

Structural Requirements for Modulating 4-Benzylpiperidine Carboxamides from Serotonin/Norepinephrine Reuptake Inhibitors to Triple Reuptake Inhibitors

  • Paudel, Suresh;Kim, Eunae;Zhu, Anlin;Acharya, Srijan;Min, Xiao;Cheon, Seung Hoon;Kim, Kyeong-Man
    • Biomolecules & Therapeutics
    • /
    • v.29 no.4
    • /
    • pp.392-398
    • /
    • 2021
  • In this study, we determined the effect of 24 different synthetic 4-benzylpiperidine carboxamides on the reuptake of serotonin, norepinephrine, and dopamine (DA), and characterized their structure-activity relationship. The compounds with a two-carbon linker inhibited DA reuptake with much higher potency than those with a three-carbon linker. Among the aromatic ring substituents, biphenyl and diphenyl groups played a critical role in determining the selectivity of the 4-benzylpiperidine carboxamides toward the serotonin transporter (SERT) and dopamine transporter (DAT), respectively. Compounds with a 2-naphthyl ring were found to exhibit a higher degree of inhibition on the norepinephrine transporter (NET) and SERT than those with a 1-naphthyl ring. A docking simulation using a triple reuptake inhibitor 8k and a serotonin/norepinephrine reuptake inhibitor 7j showed that the regions spanning transmembrane domain (TM)1, TM3, and TM6 form the ligand binding pocket. The compound 8k bound tightly to the binding pocket of all three monoamine reuptake transporters; however, 7j showed poor docking with DAT. Co-expression of DAT with the dopamine D2 receptor (D2R) significantly inhibited DA-induced endocytosis of D2R probably by reuptaking DA into the cells. Pretreatment of the cells with 8f, which is one of the compounds with good inhibitory activity on DAT, blocked DAT-induced inhibition of D2R endocytosis. In summary, this study identified critical structural features contributing to the selectivity of a molecule for each of the monoamine transporters, critical residues on the compounds that bound to the transporters, and the functional role of a DA reuptake inhibitor in regulating D2R function.

Study on Control and Tuberization Inhibition of Eleocharis kuroguwai Ohwi (올방개의 괴경형성(塊莖形成) 억제(抑制) 및 방제(防除)에 관(關)한 연구(硏究))

  • Im, I.B.;Park, S.H.;Guh, J.O.
    • Korean Journal of Weed Science
    • /
    • v.11 no.1
    • /
    • pp.60-67
    • /
    • 1991
  • The experiment was conducted to evaluate weeding effect and to inhibit tuberization of Eleocharis kuroguwai authority by single or systematic applications of several herbicides. E. kuroguwai was controlled above 90 percentage by pretilachlor and butachlor+bensulfuron application at 5-10 DAT(Days after transplanting) followed by bentazon at 50 DAT and weeded 88 percentage by mefenacet+bensulfuron application at 15 DAT. Tuberization inhibition rate of E. kuroguwai was higher at the application of butachlor+bensulfuron at 5 DAT followed by bentazon at 50 DAT than any other applications. The weight variation of E. kuroguwai tubers formed at 15-20cm soil stratum was larger than that at 10-15cm. Tuber of E. kuroguwai was hardly formed at top soil stratum (0-5cm) and deep soil (15-20cm) by the systematic application of bentazon at 50 DAT. Grain yield of rice from systematic application with bentazon at 50 DAT and mefenacet+bensulfuron at 10-15 DAT was similar to that of hand weeded plot.

  • PDF

Susceptibility of Pine Sawyer, Monochamus saltuarius Adults (Coleoptera: Cerambycidae) to Commercially Registered Insecticides (북방수염하늘소의 살충제 감수성)

  • Han, Ju-Hwan;You, Jong-Hyun;Kim, Eun-Hee;Yang, Jeong-Oh;Noh, Doo-Jin;Yoon, Chang-Mann;Kim, Gil-Hah
    • The Korean Journal of Pesticide Science
    • /
    • v.12 no.3
    • /
    • pp.262-269
    • /
    • 2008
  • This study was performed to investigate the toxicity of 39 registered insecticides to the susceptibility, systemic effect, and residual effect and control effect against Pine sawyer beetle, Monochamus saltuarius. Eleven kinds of chemicals such as fenitrothion, fenthion, phenthoate, phosphamidon, dinotefuran, actamiprid, clothianidin, thiacloprid, thiamethoxam, esfenvalerate+fenitrothion, and fipronil were showed 100% insecticidal activity both in body spray and twig dipping bioassay. Among these chemicals, fenitrothion and fenthion were showed 100% insecticidal activity when sprayed at 4000 times diluted solutions, and phenthoate, thiacloprid, thiamethoxam and fipronil were showed 100% insecticidal activity when sprayed at 2000 times diluted solution. Root systemic effect was showed 100% mortality in phosphamidon, clothianidin, thiamethoxam, and 77.7% in thiacloprid. In residual effect, fenitrothion and thiamethoxam were showed 80% mortality fifteen days after treatment (DAT), and fenthion, phosphamidon, clothianidin were showed 80% mortality ten DAT, fenitrothion, thiamethoxam, fipronil showed 100% mortality in seven DAT, thiacloprid was showed 100% mortality in three DAT. Fenthion and phenthoate were showed 100% mortality one DAT. In the control effect, 6 kinds of chemicals were showed 100% mortality one DAT and all chemicals showed 100% mortality three DAT.

Evaluation of Acute and Residual Toxicity of Insecticides Registered on Strawberry against Honeybee (Apis mellifera) (딸기에 등록된 살충제의 꿀벌에 대한 급성 및 엽상잔류독성)

  • Ahn, Ki-Su;Yoon, Changmann;Kim, Ki-Hyun;Nam, Sang-Young;Oh, Man-Gyun;Kim, Gil-Hah
    • The Korean Journal of Pesticide Science
    • /
    • v.17 no.3
    • /
    • pp.185-192
    • /
    • 2013
  • This study was performed to evaluate the spray toxicity and leaf residual toxicity of 52 kinds of insecticides registered for strawberry against adult honeybee Apis mellifera. According to the IOBC standard, the acute toxicity by spraying showed below 30% was classified as non-toxic. Among tested insecticides, 32 insecticides (flonicamid, lufenuron, novaluron, three kinds of acetamiprid, thiacloprid, milbemectin, acequinocyl, TBI-1, two kinds of chlorfenapyr, chlorfluazuron, cyenopyrafen, cyfumetofen, etoxazole, fenpyroximate, flubendiamide, flufenoxuron, hexythiazox, metaflumizone, two kinds of methoxyfenozide, DBB-2032, pyridalyl, spiromesifen, tebufenpyrad, teflubenzuron, acetamiprid + methoxyfenozide, acrinathrin + spiromesifen, bifenazate + spiromesifen, cyenopyrafen + flufenoxuron) did not show any toxic effect, it is thought to be safe. And the others (20 insecticides) showed higher toxicity to honeybee. Insecticides which showed acute toxicity higher than 90% was selected and tested the residual toxicity. All insecticides except emamectin benzoate EC, and indoxacarb SC showed 100% mortality at one day after treatment (DAT). However, the toxicities of emamectin benzoate, indoxacarb SC, and abamectin did not show until 3, 7, 14 DAT, respectively. Nine insecticides such as indoxacarb WP, thiamethoxam WG, abamectin + chlorantraniliprole SC, acetamiprid + etofenprox WP, acetamiprid + indoxacarb WP, bifenthrin + clothianidin SC, bifenthrin + imidacloprid WP, bifenazate + pyridaben SC, chlorfenapyr + clothianidin SC showed over 90% residual toxicity until 31 Day. In pouring treatment, thiamethoxam WG showed 76.9% mortality at 28 DAT and 50.0% mortality at 31 DAT. After 35 days, thiamethoxam WG showed no effect to honeybee. Bifenthrin + clothianidin SC and tefluthrin + thiamethoxam GR showed 57.1 and 80.0% mortality at 24 DAT, respectively. In spraying treatment, thiamethoxam WG and bifenthrin+clothianidin SC showed very high residual toxicity with 100% mortality in thirty-five DAT. After spraying treatment with thiamethoxam WG, bifenthrin+clothianidin SC, bifenthrin + imidacloprid WP, thiamethoxam WG showed 100% residual toxicity until 21 DAT and there was no activity after 28 DAT. Bifenthrin+clothianidin SC and bifenthrin+imidacloprid WP showed very high residual toxicity until 49 DAT.

Relationship among Pain, Depression and Activities of Daily Living in Nursing Home Residents (노인요양시설 입소 노인의 통증, 우울 및 일상생활활동과의 관련성)

  • Lee, Young-Mi
    • Journal of the Korea Academia-Industrial cooperation Society
    • /
    • v.15 no.11
    • /
    • pp.6728-6738
    • /
    • 2014
  • This study investigated the relationship among pain, depression and activities of daily living in nursing home residents. Data was collected through a structured questionnaire survey of residents at 4 nursing homes in S city. The measures were the Numeric Rating Scale (NRS) and Discomfort Scale-Dementia of the Alzheimer Type (DS-DAT) for self-reported and observational pain, Geriatric Depression Scale Short Form-Korea Version (GDSSF-K) for depression, Barthel Activities of Daily Living (BADL) scale for ADL. The data were analyzed using the Pearson's correlation coefficient and hierarchical multiple regression using the SPSS/PC 20.0 program. The analysis results of the relationship of pain, depression and activities of daily living, both DS-DAT and NRS showed a significant negative correlation with the activities of daily living and a positive correlation with depression. Finally, gender, arthritis, depression, and activities of daily living explained 28.1% of the variance in pain using NRS, whereas depression and activities of daily living explained 21.5% of the variance in pain using DS-DAT. The results highlight the need to develop a pain management program that reduces the depression and promotes the activities of daily living in nursing home residents; hence, a differentiated approach as non-pharmacological interventions is required.

Residual Activity and Effect of Soil-applied Herbicides on Succeeding Crops in Vegetable Fields;4. Residual Amount of Herbicides Nitralin and Napropamide (주요채소용제초제(主要菜蔬用除草劑)의 토양중(土壤中) 잔효와 후작물(後作物)에 미치는 영향(影響);제(第)4보(報) : 제초제(除草劑) Nitralin과 Napropamide의 잔류량조사(殘留量調査))

  • Ryang, H.S.;Moon, Y.H.;Choi, E.S.;Jang, M.S.;Lee, J.H.;Chang, Y.N.
    • Korean Journal of Environmental Agriculture
    • /
    • v.10 no.2
    • /
    • pp.113-118
    • /
    • 1991
  • The soil residual amount of herbicides nitralin and napropamide was determined in 6 winter crops field using a chemical assay method. Chemical analysis on soil residue revealed that a relatively high amount of nitralin was detected between 150 and 200 days after treament(DAT). However, regardless of soil types the residue at 220 DAT ranged from 0.053 to 0.141ppm and from 0.134 to 0.308ppm, at the rate of 75 and 150 g a.i./10a, respectively. The residue of napropamide applied at the rate of 75 g a.i./l0a ranged from 0.006 to 0.072ppm at 150 DAT, but not detectable at 220 DAT. When application rate increased to 150 g a.i./10a, napropamide residue was between 0.005 and 0.16ppm at 150 DAT and less than 0.004ppm at 200 DAT, and was not detected at 220 DAT, irrespective of soil types. The results of chemical analysis for the two herbicides showed a similar trend to those obtained from the experiments in agar medium and fields.

  • PDF

Investigation into the Possible Genetic Role of Serotonin and Dopamine Transporters in Psychological Resilience

  • Cho, Sang Hyun;Chung, Jae Kyung;Bang, Yang Weon;Joo, Eun-Jeong
    • Korean Journal of Biological Psychiatry
    • /
    • v.25 no.1
    • /
    • pp.16-20
    • /
    • 2018
  • Objectives Psychological resilience is the ability to cope with stress. The genetic background behind psychological resilience is not much known. The serotonin transporter and dopamine transporter are implicated in stress related psychology and emotional processing. The aim of this study is to investigate a possible genetic role of functional polymorphisms of serotonin and dopamine transporters for psychological resilience. Methods A total of 951 healthy adult subjects were included. Psychological resilience was measured using Connor-Davidson Resilience Scale (CD-RISC). Genotyping was performed for serotonin transporter gene(SERT) promoter variable number tandem repeat (VNTR) and dopamine transporter gene(DAT1) 3'-untranslated region (UTR) VNTR. Genetic association analysis was conducted between genotypes and the CD-RISC score. Results No genetic association was observed for SERT promoter VNTR or DAT1 3'-UTR VNTR with CD-RISC score. No genetic interaction between SERT promoter VNTR and DAT1 3'-UTR VNTR with CD-RISC score was detected. Conclusions Either serotonin or dopamine transporter did not seem to play a significant role for psychological resilience in this sample.

  • PDF

A Study of Jowiseungchungtang in patients with mild Dementia of Alzheimer type (조위승청탕(調胃升淸湯)이 초기 Dementia of Alzheimer type 환자의 인지기능 변화에 미치는 효과)

  • Cho, Seung-Hun;Kim, Jong-Woo;Kim, Hyun-Taek;Chung, Kyung-Chun;Whang, Wei-Wan
    • Journal of Oriental Neuropsychiatry
    • /
    • v.14 no.1
    • /
    • pp.17-26
    • /
    • 2003
  • Objective : The clinical efficacy of Jowiseungchungtang(oriental herbal medication) over 6-month on the cognitive function in patients with mild Dementia of Alzheimer type(DAT) was investigated in this study. Method : The subjects for this study consisted of dementia patients who visited to the outpatient dementia department of Oriental Neuropsychiatry of the Kyunghee Oriental hospital. Patients were required to have at entry: a dignosis of mild DAT; Biochemical test, CBC, Urine analysis, Chest X -ray, EKG, Brain- MRI, Mini-Mental States-Korea(MMSE-K), Korean-Dementia Rating Scale(K-DRS), Samsung Dementia Questionaire(SDQ;to their caregiver). Patients(n=31) were assigned to treatment with Jowiseungchungtang (fourth/day for 6-month). The primary outcome measure was K-DRS. Result : 1. Patients' mean age was $71.4{\pm}6.6$ years(range 59 to 86 years). 2. Patients' mean education was $6.1{\pm}4.9$ years. K-DRS scores at baseline was $110.5{\pm}12.2$. K-DRS scores at 6-month was $109.0{\pm}17.0$. K-DRS scores at 6-month was not significantly different with K-DRS scores at baseline(t=.791 r=.435 p<.05). Conclusion : Treatment with Jowiseungchungtang for 6-month protected the cognitive function decline in patients with mild DAT.

  • PDF

Effect of Biodegradable Film Mulching on Soil Environment and Onion Growth and Yield (생분해성 멀칭필름이 토양환경과 양파 생육 및 수량에 미치는 영향)

  • Ji-Sik Jung;Do-Won Park;Hyun-Sug Choi
    • KOREAN JOURNAL OF CROP SCIENCE
    • /
    • v.68 no.3
    • /
    • pp.207-215
    • /
    • 2023
  • This study was compared the soil environment and growth and yield of onion (Allium cepa L.) treated with non-mulching (NM) and mulching polyethylene film (PEF) and two biodegradable films (BFI and BFII) commonly used in farmhouses. Visual observation confirmed the degradation of BFI and BFII films after 150 days after tansplanting (DAT). BFII increased light penetration into the films and reduced the weight maintenace after 180 DAT, with a high decompostion at 30 days after soil tilling. Soil moisture contents much fluctuated between -14 kP and - 0 kPa in NM plots, increasing the minimum soil temperature of BFI plots. Mulching treatments decreased soil organic matter contents but did not subtantially increase soil mineral nutrients, soil bulk density, and number of bacteria compared to those of NM plots. Onion root growth was increased by PEF and BFI treatments at an early growth stage, 60 DAT, with the most remarkable stem extension observed for PEF and BFI treatments after 150 DAT. PEF and BFI treatments increased the bulb's diameter, length, weight, and lodging at 180 DAT. BFI treatments exhibited a high portion of the "very large" category producing with 55.3 tons ha-1 based on the classification into bulb size, followed by PE (49.3 tons), NM (9.4 tons), and BFII treatments (2.7 tons) at 230 DAT.

Evaluation of Toxicity of Plant Extract Made by Neem and Matrine against Main Pests and Natural Enemies (멀구슬과 고삼을 원료로 한 식물추출물의 주요해충과 천적에 대한 독성평가)

  • Hwang, In-Cheon;Kim, Jin;Kim, Hyeong-Min;Kim, Do-Ik;Kim, Sun-Gon;Kim, Sang-Su;Jang, Cheol
    • Korean journal of applied entomology
    • /
    • v.48 no.1
    • /
    • pp.87-94
    • /
    • 2009
  • KNI3126 which is the eco-friendly material made by plant extracts - neem and matrine - have been evaluated for efficacies against 6 main pests and toxicity on natural enemies. Insecticidal efficacies of KNI3126 against plant hopper were above 95% at 5 days after treatment (DAT), whereas pesticidal effects against the cotton aphid were above 95% at 3 DAT and slightly decreased at 5 DAT. Insecticidal efficacy against the palm thrips resulted in lower control value as 68.1% than that of chemical insecticides. KNI3126 showed more than 95% control value against diamond back moth, suggesting that it could suppress the population of pest hard to control as eco-friendly material. Mortalities against two-spotted spider mite were about 80% at 1 DAT and over 90% at 5 DAT, respectively. For evaluation of the toxicity on natural enemies, effect against predatory natural enemy was classified as moderate selective toxicity based on the criterion of International Organization of Bio-Control (IOBC), whereas against parasitic natural enemies was found to be relatively safe. Repellent effect was weak against plant hopper, but strong against two-spotted spider mite. In the toxicity test for safety, KNI3126 was classified as the lowest level at acute oral, acute dermal and fish toxicity test and did not induce the irritancy at skin irritation test and eye irritation test.