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Selectivity of Oxomemazine for the $M_1$ Muscarinic Receptors

  • Lee, Shin-Woong;Woo, Chang-Woo;Kim, Jeung-Gu
    • Archives of Pharmacal Research
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    • v.17 no.6
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    • pp.443-451
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    • 1994
  • The binding characteristics of pirenzepine and oxomemazine to muscarinic receptor were studied to evaluate the selectivity of oxomemazine for the muscarinic receptor subtypes in rat cerebral microsomes. Equililbrium dissociation constant $(K_D){\;}of{\;}(-)[^3H]$quinuclidinyl benzilate$([^3H)QNB)$ determined from saturation isotherms was 64-pM. Analysis of the pirenzepine inghibition curve of [$^3H$]QNB binding to cerebral microsome indicatd the presence of two receptor subtypes with high $(K_1 = 16 nM, M_1 receptor)$two receptor subypes with about 20-fold difference in the affinity for high $(k_1 = 84nM, {\;} O_H receptor){\;} and {\;}low{\;} (K_1{\;} ={\;} 1.65\muM, {\;} O_L receptor$) affinity sites. The percentage populations of $M_1{\;} and M_3$, /TEX> receptors to the total receptors were 61 : 39, and those of $O_H{\;} and{\;} O_L$ receptors 39 : 61, resepectively. Both pirenzepine and oxomemazine increaed the $K_D$ value for $[^3H]QNB$ without affecting the binding site concentrations and Hii coefficient for the $[^3H]QNB$ without affecting the binding site concentractions and Hill coefficient for the [$^{3}$H]QNB binding. Oxomemazine had a 10-fold higher affinity at $M_1$ receptors than at $M_3$ receptors, and pirenzepine a 8-fold higher affinity at $O_H$ receptors were of $O_H$ receptors and 71% of $M_3$ receptors. However, $M_3$for oxomemazine and $O_H$for pirenzepine were composed of a uniform population. These results suggest that oxomemazine could be classified as a selective drug for $M_1$ receptors and also demonstrate that rat cerebral microsomes contain three different subtypes of $M_1{\;} M_3$ and the other site which is different from $M_1, {\;} M_2$, /TEX> receptors.

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P- and S-wave seismic studies in the Ulsan fault zone near Nongso-Eup (농소읍 부근 울산단층대에서의 P파 및 S파 탄성파 조사 연구)

  • Lee, Chang-Min;Kim, Ki-Young
    • 한국지구물리탐사학회:학술대회논문집
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    • 2006.06a
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    • pp.95-100
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    • 2006
  • To reveal subsurface structures of the Ulsan fault, seismic data were recorded along a 750-m long line near Nongso-Eup in Ulsan. P and S waves were generated simultaneously by impacting a 5 kg sledgehammer on a tilted plate. The data were received by 16 10-Hz 3-component geophones at 3 m intervals. Refracted P waves were inverted using the tomography method. Dip moveout and migration were applied to reflection data processed following a general sequence. Four layers were identified based on P-wave velocities and P- and S-wave stacked image. From top to bottom, the P-wave velocity of each layer ranges in $300{\sim}1100\;m/s$, $1100{\sim}1700\;m/s$, $1700{\sim}2700\;m/s$, and greater than 2700 m/s. The corresponding thickness of the top three layers averages 3.9 m, 5.9 m, 4.4 m, respectively. The S-wave stack section is effective to define subsurface structures shallower than 10 m.

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Effect of Nitrogen on Eleutheroside production and Adventitious Root Growth in Eleutherococcus koreanum Nakai Bioreactor Cultures (생물반응기를 이용한 섬오갈피나무의 부정근 배양시 질소농도 및 NH4+와 NO3- 비율이 부정근의 생육과 eleutherosides 함량에 미치는 영향)

  • Ahn, Jin-Kwon;Lee, Wi-Young;Park, Eung-Jun
    • Journal of Korean Society of Forest Science
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    • v.98 no.4
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    • pp.363-369
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    • 2009
  • This study was carried out to investigate the effect of ${NO_3}^-$ and ${NH_4}^+$ on the adventitious root growth and eleuthroside synthesis of Eleutherococcus koreanum in 5 L-bioreactor culture. The change in the medium components was also measured during culture. The fresh weignt of adventitious root reached to the highest level of 30.8 g FW/L in the presence of both 50 mM ${NO_3}^-$ and 10 mM $NH_4^+$, representing 3.6-fold increase compared to the 60 mM ${NH_4}^+$ alone. However, as the increase of the portion of ${NH_4}^+$, the root growth was decreased. However, the maximum eleutheroside B, E and E1 contents were $57.3{\mu}g/g$ DW, $188.4{\mu}g/g$ DW and $47.3{\mu}g/g$ DW, with 30 mM, 60 mM and 15 mM total nitrogen source, respectively. Fresh weight of adventitious root increased up to 6.8-fold of inoculum size within 9 weeks. The amounts of ${NH_4}^+$, $K^+$, ${NO_3}^-$ and ${PO_4}^-$ were decreased during culture periods. Based on these results, we suggest that various further studies are required to increase the biomass and the useful secondary metabilites.

Development of a culvert design model (유역배율별 저수지의 하천유지유량 공급능력)

  • Noh, Jae-Kyoung;Lee, Jae-Nam
    • Proceedings of the Korea Water Resources Association Conference
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    • 2011.05a
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    • pp.446-446
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    • 2011
  • 유역면적을 수혜면적으로 나눈 값을 유역배율이라 하며, 관개저수지에서 적어도 3 이상 되어야 용수공급의 효율이 있다. 저수지 둑 높이기 사업의 113개 저수지를 분석하면 유역배율이 3 이하 37개소, 3-10은 58개소, 10이상 18개소에 이르며, 이 중에서 몇 개 저수지를 선정하여 유역배율별 저수지로부터 하천유지유량 공급능력을 분석하였다. 분석방법은 저수지 물수지 모형을 구축하여, 이수관리곡선에 의해 용수공급제한 운영의 경우와 정상운영의 결과로 구분하여 하천유지유량 공급능력을 분석하였다. 사전연구로 유효저수량 21,504 천$m^3$, 유역면적 $84.79\;km^2$, 수혜면적 2,975 ha인 백곡저수지에 1966년부터 2009년까지 수혜지역에 공급할 논 관개용수 수요량을 일별로 추정하였으며, 연 관개수량은 최소 1,000만 $m^3$, 최대 4,173만 $m^3$, 평균 3,319만 $m^3$에 이르렀다. 10월부터 4월까지 하천유지유량으로 공급하는 것으로 계산하였으며, 백곡지 저수량 자료를 이용하여 유입량 모형 매개변수를 결정하여 저수지 유입량을 일별로 모의하였고, 기존저수지와 2 m 증고저수지에 대해 이수관리곡선을 작성하였다. 방류제한 운영시 관개용수 공급량은 기존저수지에서 홍수제 한수위가 없는 경우 3,151만 $m^3$, 홍수제한수위가 있는 경우는 3,014~3,087만 $m^3$로 64~137만 $m^3$ 감소하였으며, 2 m 증고 저수지에서 홍수제한수위가 없는 경우 3,293만 $m^3$, 홍수제한수위가 있는 경우는 3,175~3,245만 $m^3$로 48~118만 $m^3$ 감소한 것으로 나타나 감소율은 각각 2.0~4.3 %, 1.5~3.6 %에 불과하였다.

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Different Mechanisms for $K^+-Induced$ Relaxation in Various Arteries

  • Suh, Suk-Hyo;Park, Sung-Jin;Choi, Jai-Young;Sim, Jae-Hoon;Kim, Young-Chul;Kim, Ki-Whan
    • The Korean Journal of Physiology and Pharmacology
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    • v.3 no.4
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    • pp.415-425
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    • 1999
  • $[K^+]_o$ can be increased under a variety of conditions including subarachnoid hemorrhage. The increase of $[K^+]_o$ in the range of $5{\sim}15$ mM may affect tensions of blood vessels and cause relaxation of agonist-induced precontracted vascular smooth muscle $(K^+-induced$ relaxation). In this study, effect of the increase in extracellular $K^+$ concentration on the agonist-induced contractions of various arteries including resistant arteries of rabbit was examined, using home-made Mulvany-type myograph. Extracellular $K^+$ was increased in three different ways; from initial 1 to 3 mM, from initial 3 to 6 mM, or from initial 6 to 12 mM. In superior mesenteric arteries, the relaxation induced by extracellular $K^+$ elevation from initial 6 to 12 mM was the most prominent among the relaxations induced by the elevations in three different ways. In cerebral arteries, the most prominent relaxation was produced by the elevation of extracellular $K^+$ from initial 1 to 3 mM and a slight relaxation was provoked by the elevation from initial 6 to 12 mM. In superior mesenteric arteries, $K^+-induced$ relaxation by the elevation from initial 6 to 12 mM was blocked by $Ba^{2+}\;(30\;{\mu}M)$ and the relaxation by the elevation from 1 to 3 mM or from 3 to 6 mM was not blocked by $Ba^{2+}.$ In cerebral arteries, however, $K^+-induced$ relaxation by the elevation from initial 3 to 6 mM was blocked by $Ba^{2+},$ whereas the relaxation by the elevation from 1 to 3 mM was not blocked by $Ba^{2+}.$ Ouabain inhibited all of the relaxations induced by the extracellular $K^+$ elevations in three different ways. In cerebral arteries, when extracellular $K^+$ was increased to 14 mM with 2 or 3 mM increments, almost complete relaxation was induced at 1 or 3 mM of initial $K^+$ concentration and slight relaxation occurred at 6 mM. TEA did not inhibit $Ba^{2+}-sensitive$ relaxation at all and NMMA or endothelial removal did not inhibit $K^+-induced$ relaxation. Most conduit arteries such as aorta, carotid artery, and renal artery were not relaxed by the elevation of extracellular $K^+.$ Among conduit arteries, trunk of superior mesenteric artery and basilar artery were relaxed by the elevations of $[K^+]_o.$ These data suggest that $K^+-induced$ relaxation has two independent components, $Ba^{2+}-sensitive$ and $Ba^{2+}-insensitive$ one and there are different mechanisms for $K^+-induced$ relaxation in various arteries.

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Effect of Ganglioside $G_{M3}$ on the Erythrocyte Glucose Transporter (GLUT1): Conformational Changes Measured by Steady-State and Time-Resolved Fluorescence Spectroscopy

  • Yoon, Hae-Jung;Lee, Min-Yung;Jhon, GiI-Ja
    • BMB Reports
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    • v.30 no.4
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    • pp.240-245
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    • 1997
  • Interactions between ganglioside $G_{M3}$ and glucose transporter, GLUT1 were studied by measuring the effect of $G_{M3}$ on steady-state and time-resolved fluorescence of purified GLUT1 in synthetic lipids and on the 3-O-methylglucose uptake by human erythrocytes. The intrinsic tryptophan fluorescence showed a GLUT 1 emission maximum of 335 nm, and increased in the presence of $G_{M3}$ by 12% without shifting the emission maximum, The fluorescence lifetimes of intrinsic tryptophan on GLUT1 consisted of a long component of 7.8 ns and a short component of 2,3 ns and $G_{M3}$ increased both lifetime components. Lifetime components were quenched by acrylamide and KI. Acrylarnide-mduced quenching of long-lifetime components was partly recovered by $G_{M3}$ However. KI-induccd quenching of short- and long-lifetime components was not rescued by $G_{M3}$. The anisotropy of 1.6-diphenyl-1.3.5-hexatriene (DPH)-probed dimyristoylphosphatidylcholine (DMPC) model membrane was also increased with $G_{M3}$ incorporation, The transport rate of 3-O-methylglucose increased by 20% with $G_{M3}$ incorporation on the erythrocytes, Therefore, $G_{M3}$ altered the environment of lipid membrane and induced the conformational change of GLUT1.

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Increasing Instream flow in Nonsancheon by Water Storage Securing Scenario of Upstream Reservoirs (상류 저수지군의 저수량 확보 시나리오에 의한 논산천의 유지유량 증가)

  • Noh, Jae-Kyoung
    • Korean Journal of Agricultural Science
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    • v.36 no.1
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    • pp.99-109
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    • 2009
  • This study was performed to evaluate the effect of increasing instream flow at Nonsancheon stream of Nonsan city by securing water storages in upstream reservoirs; Ge-ryong, Gyoung-cheon, Dae-dun, and Tab-jeong. The paralleled and cascaded upstream reservoir operations for 8 storage securing scenarios were considered to simulate daily streamflows at Nonsan station. Using Tab-jeong reservoir water storage, the DAWAST model's parameters were determined, and the verified result showed Nash-Schcliffe's coefficient of 0.666. Instream flows were analyzed to supply maximum $59.85Mm^3$ on an annually average from upstream reservoir storage securing scenarios. The storage securing set of 2 m heightened Ge-ryong, 5 m Dae-dun, and 1 m Tab-jeong showed that the additional secured water storages were $17.132Mm^3$ and instream flow at Nonsan station was increased to $2.183m^3/s$, 2 times of present condition.

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Analyses of Sustainability(TBL) of Marine Sport Events (해양스포츠이벤트의 지속가능성(TBL) 분석)

  • Cho, Woo-Jeong;Kang, Shin-Beum
    • Journal of Navigation and Port Research
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    • v.37 no.1
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    • pp.91-100
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    • 2013
  • The purpose of this study was to examine the levels of sustainability of marine sport events by types of events and thus to provide fundamental information that helps developing sustainable marine sport events. In order to accomplish such the purpose, this study employed survey methodology with a total of 285 visitors to marine sport events. Questionnaires were developed based on Tripple Bottom Line theory suggested by previous research and validated throughout a panel of experts to check out content validity. Data collected were analyzed using descriptive statistics and ANOVA with Scheffe post hoc tests. Accordingly following findings were derived from current study. First, among 12 positive sustainability variables, marine space improvement had the highest mean score(M=3.82) but creation of jobs had the lowest mean score(M=3.46). Among 11 negative sustainability variables, traffic jab had the highest mean score(M=3.16) but conflict between participants and residents had the lowest mean score(M=2.73). Second, a festival typed marine sport event had the significantly high mean scores in all positive sustainability index including economic sustainability(M=3.79), social sustainability(M=3.84) and environmental sustainability(M=3.80). Third, a business typed marine sport event had the relatively higher mean scores in all negative sustainability index including economic sustainability(M=3.22), social sustainability(M=3.26) and environmental sustainability(M=3.25). In conclusion, these findings suggest that marine sport event organizers concentrate on marine sport event with more sustainability potentials.

The Significance of Plasma Urokinase-type Plasminogen Activator and Type 1 Plasminogen Activator Inhibitor in Lung Cancer (폐암에서 혈장 Urokinase-Type Plasminogen Activator 및 Type 1 Plasminogen Activator Inhibitor의 의의)

  • Park, Kwang-Joo;Kim, Hyung-Jung;Ahn, Chul-Min;Lee, Doo-Yun;Chang, Joon;Kim, Sung-Kyu;Lee, Won-Young
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.3
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    • pp.516-524
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    • 1997
  • Background : Cancer invasion and metastasis require the dissolution of the extracellular matrix in which several proteolytic enzymes are involved. One of these enzymes is the urokinase-type plasminogen activator(u-PA), and plasminogen activator inhibitors(PAI-1, PAI-2) also have a possible role in cancer invasion and metastasis by protection of cancer itself from proteolysis by u-PA. It has been reported that the levels of u-PA and plasminogen activator inhibitors in various cancer tissues are significantly higher than those in normal tissues and have significant correlations with tumor size and lymph node involvement. Here, we measured the concentration of plasma u-PA and PAI-1 antigens in the patients with lung cancer and compared the concentration of them with histologic types and staging parameters. Methods : We measured the concentration of plasma u-PA and PAI-1 antigens using commercial ELISA kit in 37 lung cancer patients, 21 benign lung disease patients and 24 age-matched healthy controls, and we compared the concentration of them with histologic types and staging parameters in lung cancer patients. Results : The concentration of u-PA was $1.0{\pm}0.3ng/mL$ in controls, $1.0{\pm}0.3ng/mL$ in benign lung disease patients and $0.9{\pm}0.3ng/mL$ in lung cancer patients. The concentration of PAI-1 was $14.2{\pm}6.7ng/mL$ in controls, $14.9{\pm}6.3ng/mL$ in benign lung disease patients, and $22.1{\pm}9.8ng/mL$ in lung cancer patients. The concentration of PAI-1 in lung cancer patients was higher than those of benign lung disease patients and controls. The concentration of u-PA was $0.7{\pm}0.4ng/mL$ in squamous cell carcinoma, $0.8{\pm}0.3ng/mL$ in adenocarcinoma, 0.9ng/mL in large cell carcinoma, and $1.1{\pm}0.7ng/mL$ in small cell carcinoma. The concentration of PAI-1 was $22.3{\pm}7.2ng/mL$ in squamous cell carcinoma, $22.6{\pm}9.9ng/mL$ in adenocarcinoma, 42 ng/mL in large cell carcinoma, and $16.0{\pm}14.2ng/mL$ in small cell carcinoma. The concentration of u-PA was 0.74ng/mL in stage I, $1.2{\pm}0.6ng/mL$ in stage II, $0.7{\pm}0.4ng/mL$ in stage IIIA, $0.7{\pm}0.4ng/mL$ in stage IIIB, and $0.7{\pm}0.3ng/mL$ in stage IV. The concentration of PAI-1 was 21.8ng/mL in stage I, $22.7{\pm}8.7ng/mL$ in stage II, $18.4{\pm}4.9ng/mL$ in stage IIIA, $25.3{\pm}9.0ng/mL$ in stage IIIB, and $21.5{\pm}10.8ng/mL$ in stage IV. When we divided T stage into T1-3 and T4, the concentration of u-PA was $0.8{\pm}0.4ng/mL$ in T1-3 and $0.7{\pm}0.4ng/mL$ in T4, and the concentration of PAI-1 was $17.9{\pm}5.6ng/mL$ in T1-3 and $26.1{\pm}9.1ng/mL$ in T4. The concentration of PAI-1 in T4 was significantly higher than that in T1-3. The concentration of u-PA was $0.8{\pm}0.4ng/mL$ in M0 and $0.7{\pm}0.3ng/mL$ in M1, and the concentration of PAI-1 was $23.6{\pm}8.3ng/mL$ in M0 and $21.5{\pm}10.8ng/mL$ in M1. Conclusions : The plasma levels of PAI-1 in lung cancer were higher than benign lung disease and controls, and the plasma levels of PAI-1 in T4 were significantly higher than T1-3. These findings suggest involvement of PAI-1 with local invasion of lung cancer, but it should be confirmed by the data on comparison with pathological staging and tissue level in lung cancer.

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A study on the Degradation and By-products Formation of NDMA by the Photolysis with UV: Setup of Reaction Models and Assessment of Decomposition Characteristics by the Statistical Design of Experiment (DOE) based on the Box-Behnken Technique (UV 공정을 이용한 N-Nitrosodimethylamine (NDMA) 광분해 및 부산물 생성에 관한 연구: 박스-벤켄법 실험계획법을 이용한 통계학적 분해특성평가 및 반응모델 수립)

  • Chang, Soon-Woong;Lee, Si-Jin;Cho, Il-Hyoung
    • Journal of Korean Society of Environmental Engineers
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    • v.32 no.1
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    • pp.33-46
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    • 2010
  • We investigated and estimated at the characteristics of decomposition and by-products of N-Nitrosodimethylamine (NDMA) using a design of experiment (DOE) based on the Box-Behken design in an UV process, and also the main factors (variables) with UV intensity($X_2$) (range: $1.5{\sim}4.5\;mW/cm^2$), NDMA concentration ($X_2$) (range: 100~300 uM) and pH ($X_2$) (rang: 3~9) which consisted of 3 levels in each factor and 4 responses ($Y_1$ (% of NDMA removal), $Y_2$ (dimethylamine (DMA) reformation (uM)), $Y_3$ (dimethylformamide (DMF) reformation (uM), $Y_4$ ($NO_2$-N reformation (uM)) were set up to estimate the prediction model and the optimization conditions. The results of prediction model and optimization point using the canonical analysis in order to obtain the optimal operation conditions were $Y_1$ [% of NDMA removal] = $117+21X_1-0.3X_2-17.2X_3+{2.43X_1}^2+{0.001X_2}^2+{3.2X_3}^2-0.08X_1X_2-1.6X_1X_3-0.05X_2X_3$ ($R^2$= 96%, Adjusted $R^2$ = 88%) and 99.3% ($X_1:\;4.5\;mW/cm^2$, $X_2:\;190\;uM$, $X_3:\;3.2$), $Y_2$ [DMA conc] = $-101+18.5X_1+0.4X_2+21X_3-{3.3X_1}^2-{0.01X_2}^2-{1.5X_3}^2-0.01X_1X_2+0.07X_1X_3-0.01X_2X_3$ ($R^2$= 99.4%, 수정 $R^2$ = 95.7%) and 35.2 uM ($X_1$: 3 $mW/cm^2$, $X_2$: 220 uM, $X_3$: 6.3), $Y_3$ [DMF conc] = $-6.2+0.2X_1+0.02X_2+2X_3-0.26X_1^2-0.01X_2^2-0.2X_3^2-0.004X_1X_2+0.1X_1X_3-0.02X_2X_3$ ($R^2$= 98%, Adjusted $R^2$ = 94.4%) and 3.7 uM ($X_1:\;4.5\;$mW/cm^2$, $X_2:\;290\;uM$, $X_3:\;6.2$) and $Y_4$ [$NO_2$-N conc] = $-25+12.2X_1+0.15X_2+7.8X_3+{1.1X_1}^2+{0.001X_2}^2-{0.34X_3}^2+0.01X_1X_2+0.08X_1X_3-3.4X_2X_3$ ($R^2$= 98.5%, Adjusted $R^2$ = 95.7%) and 74.5 uM ($X_1:\;4.5\;mW/cm^2$, $X_2:\;220\;uM$, $X_3:\;3.1$). This study has demonstrated that the response surface methodology and the Box-Behnken statistical experiment design can provide statistically reliable results for decomposition and by-products of NDMA by the UV photolysis and also for determination of optimum conditions. Predictions obtained from the response functions were in good agreement with the experimental results indicating the reliability of the methodology used.