소 부신수질 Muscarine 수용체의 성질

이신웅,이해태 영남대학교 약품개발연구소 1995 영남대학교 약품개발연구소 연구업적집 Vol.5 No.-

The nature of the muscarinic receptors in bovine adrenal medulla was investigated in this study. [³H]Quinuclidinyl benzilate(QNB) specifically bound to a single class of muscarinic receptor with a Kp value of about 70 pM in bovine adrenal medullary. cardiac ventricular and ileal homogenates. Pirenzepine inhibition curves of [³H]QNB binding to cardiac ventricular and ileal homogenates were steep, indicating the presence of a single class of binding site for pirenzepine with a Ki value of 990 nM and 508 nM, respectively. However, pirenzepine/[³H]QNB competition binding curves in adrenal medulla suggested the presence of two binding sites (Hill coefficient=0.59) with a high(M₁) and a low(M₂) affinity. Respective Ki values for pirenzepine were 16 nM and 633 nM, with 44% of total sites having a high affinity(M₃). Gallamine, which is selective to cardiac M₂-receptor, inhibited [³H]QNB binding to adrenal medullary, cardiac ventricular and ileal homogenates with Ki values of 12 μM, 6 μM and 13 μM, respectively. Thus, the binding affinities of pirenzepine and gallamine for M₂-receptor in adrenal medulla were similar to those in ileum, which contains the M₃-receptor. These results indicate that the M_(-1) and M_(3-) muscarinic receptor subtypes coexist in the bovine adrenal medulla.

광주광역시 치매의 유병률과 위험인자의 도시-농촌 지역 비교

신일선,김재민,윤진상,김석재,양수진,김웅장,이승현,강순아,곽지영,이형영 大韓神經精神醫學會 2002 신경정신의학 Vol.41 No.6

연구목적 : 본 연구의 목적은 광주광역시의 도시 및 농촌 지역에 거주하는 노인에서 치매의 유병률과 위험인자를 조사하고자 하였다. 부가적으로 이 두 지역간에 치매의 유병률과 위험인자를 비교하고자 하였다. 방 법 : 광주광역시의 전형적인 도시와 농촌지역의 65세 이상의 노인(N=1,598)을 대상으로, 2단계의 역학연구를 수행하였다. 1차 선별 단계에서는 38명의 훈련된 연구보조원이 대상노인을 면담하여, 사회인구학적 특징을 조사하고 한국판 간이정신상태검사(Korean version of Mini-Mental State Examination ; MMSE-K)로 평가하였다. 2차 임상 진단 단계에서는 1차 단계에서 MMSE-K 점수가 24점 이하인 노인(N=431)을 대상으로, 전문연구팀의 임상적 평가를 통해 치매를 진단하고 원인질환별로 알쯔하이머병(Alzheimer's disease ; AD), 혈관성 치매(vascular dementia ; VaD) 및 기타 치매로 분류하였다. 대상노인에서 치매의 유병률을 측정한 후, 광주광역시 전체 노인의 연령보정 유병률을 산출하였다. 전체 대상에서 AD의 위험인자를 조사한 후, 도시와 농촌군으로 나누어 분석을 다시 시행하였다. 결 과 : 1차 및 2차 단계의 참가율은 각각 71.0%(N=1,134) 및 83.2%(N=410) 였다. 연구 참여 노인(N=1,134)에서 전체 치매, AD 및 VaD의 유병률은 최소 각각 9.7%, 5.2%, 1.8%였다. 광주광역시 전체 노인의 연령 보정 유병률은 각각 10.7%, 5.7%, 1.9%인 것으로 산출되었다. AD의 독립 위험인자는 고령, 여성, 무학이었다. 도시와 농촌에 따른 유병률의 차이는 파악되지 않았다. 그러나 AD의 위험인자는 지역에 따라 차이가 있었다. 도시 노인에게는 무학만이, 농촌 노인에게는 고령과 여성인 경우가 독립 위험인자였다. 결 론 : 광주광역시 노인에서 치매의 유병률은 높았고, 이는 국내 다른 지역에서 수행된 선행연구 결과와 유사하였다. 알쯔하이머형 치매의 위험인자는 도시와 농촌에 따라 다른 결과를 보였다. 본 연구 결과는 한국에서의 치매의 실태를 반영하며, 치매의 적절한 관리와 예방을 위해서는 지역성 특성이 고려되어야 함을 시사한다. Objectives : The purpose of this study was to investigate the prevalence rate and risk factors of dementia in an urban and a rural sample of older persons in the metropolitan Kwangju area, Republic of Korea. In addition, the prevalence rate and risk factors of dementia between the two samples were compared. Methods : A two-phase epidemiological study of residents aged 65 or over(N=1,598) was conducted in a highly developed, urban and a non-contiguous, poorly developed, rural area of metropolitan Kwangju. In the first(screening) phase, 38 trained research assistants collectively peformed in-home interviews for all participants. Detailed sociodemographic characteristics were gathered and the Korean version of Mini-Mental State Examination (MMSE-K) was administered. In the second (diagnosing) phase, diagnosis of dementia was established for those scoring 24 or less on the MMSE-K in the screening phase(N=431), and etiological types of dementia were classified to Alzheimer's disease(AD), vascular dementia(VaD) or miscellanous type by two teams of experts. Prevalence rate of dementia was determined in the participants, and age-standardized prevalence rate adjusted by age distribution in metropolitan Kwangju was estimated. For AD, the risk factors were investigated in all participants, and analyses were repeated for the urban and rural samples separately. Results : The participating rates in the first and second phases were 71.0%(N=1,134) and 83.2%(N=410), respectively. In the participants, the prevalence rates of dementia(all types), AD and VaD were 9.7%, 5.2% and 1.8%, respectively. The age-standardized prevalence rates were 10.7%, 5.7% and 1.9%, respectively. Aging, female gender and no education(complete lack of formal education) were identified as independent risk factors for AD. No difference between the urban and rural samples was observed in the prevalence rates of dementia(all types), AD and YaD. However, risk factors for AD differed between these areas. In the urban sample, no education was the only significant factor ; whereas, aging and female gender were identified as risk factors in the rural sample. Conclusion : A high prevalence rate of dementia was observed among old persons in metropolitan Kwangju, consistent with previous studies conducted in other Korean areas. The risk factor profi1es for AD differed between urban and rural settings. The results of this study reflect the current status of dementia in Korea and suggests that appropriate management and prevention strategies for dementia should be tailored toward the geographic settings.

항 히스타민제의 H₁ 수용체와 무스카린 수용체에 대한 상대적 역가

이신웅,박영주,이정수 영남대학교 약품개발연구소 1994 영남대학교 약품개발연구소 연구업적집 Vol.4 No.-

The muscarinic antagonist l-[benzilic-4, 4'-³H]quinuclidinyl benzilate([³H]QNB) bound to a single class of muscarinic receptor with high affinity in guinea pig ileal membranes. The K_(D) and B_(max) values for [³H]QNB calculated from analysis of saturation isotherms were 54 pM and 156 fmol/mg, respectively. H₁-blockers inhibited [³H]QNB binding to ileal membranes with K_(i) values ranged from 0.008 μM to 1.6 μM. The pseudo-Hill coefficients of H₁-blockers for inhibition of [³H]QNB binding to the ileal membranes were close to unit. The K_(i) values for H₁-blockers were similar to the K_(M) values calculated by Schild plot of functional data obtained from inhibition of the carbachol-induced contraction in guinea-pig ileum, suggesting that binding of H₁-blockers vs [³H]QNB in ileal membranes represents an interaction with a receptor of physiological relevance. The K_(H) values of H₁-blockers for H₁-receptor estimated from inhibition of the histamine-induced contraction were the range of 0.15 nM to 56.5 nM. The K_(M)/K_(H) ratio of H₁-blockers varied over a wide range of 3 to 2300. Thus, the antihistaminic potencies of H₁-blockers do not correlate with their antimuscarinic potencies, which suggest that antihistamines have different antimuscarinic potencies in therapeutic blood levels causing similar antiallergic effect. Among 13 traditional antihistaminics examined in this study, drug having the highest and the lowest K_(M)/K_(H) ratio is triprolidine and diphenidol, respectively. The present results demonstrate that the antimuscarinic property of antihistamines is not necessary for their antiallergic effect, and data on the affinity of antihistamines for muscarinic and H₁-receptors can be an important parameter in the selection and evaluation of these drugs.

쥐 大腦 Muscarinic Receptor에 미치는 카드뮴의 影響

李正秀,朴令珠,裵基哲,李神雄 嶺南大學校 環境問題硏究所 1991 環境硏究 Vol.10 No.2

The effect of cadmium ?? on the [³H] quinuclidinyl benzilate (QNB) binding of the muscarinic receptors in the cerebrum was examined. ?? Inhibited [³H]QNB binding in both dose-dependent and time-dependent manners and this inhibitory action was irreversible. The ?? Value of ?? to inhibit [³H]QNB binding in the presence of 100 pM [³H]QNB in the cerebral microsome pretreated with ?? at 37℃ for 15 min was about 50㎛. The inhibition of [³H]QNB binding by 50㎛ ?? followed biphasic kinetics ; there is a rapid inhibition phase during first 10 min incubation periods and a slow inhibition phase after a rapid phase. ?? decreased the binding site concentration for [³H]QNB binding without affecting the affinity of QNB. These results suggest that sulphydryl group plays an important role to maintain the muscarinic receptor conformation for [³H]QNB binding.

충남 금산 지역주민에서 B형간염 표면항체(HBsAb) 발현빈도에 관한 연구

신현성,서희숙,이민웅 대한임상병리사협회 1993 대한임상병리사회지 Vol.25 No.1

인삼 사포닌이 개 심실 형질막의 K+-의존성 포스파타제 활성에 미치는 영향

이신웅,이정수 영남대학교 약품개발연구소 1992 영남대학교 약품개발연구소 연구업적집 Vol.2 No.-

The effects of ginseng saponins, gypsophila saponin, sodium dodecyl sulfate(SDS), and Triton X-100 on membrane K^(+)-dependent phosphatase activity which is lipid dependent and represents dephosphorylation step of the complete Na^(+), K^(+)-ATPase reaction were investigated in this study to elucidate whether the effects of ginseng saponins are due to the detergent action, using sarcolemma enriched preparation isolated from dog ventricle. Na^(+), K^(+)-ATPase and K^(+)-dependent phosphatase activities of cardiac sarcolemma were about 143 μmol Pi/mg protein/hr and 34 μmol p-nitrophenol/mg protein/hr, respectively. While ginseng saponins (triol>total>diol) inhibited K^(+)-dependent phosphatase activity, gypsophila saponin, and low dose of SDS(0.4 μg/μg protein), and Triton X-100 (0.6 μg/μg protein) increased the enzyme activity, indicating disruptive effect of detergents on membrane barriers. The activating effect of low doses of Triton X-100 on membrane K^(+)-dependent phosphatase appeared at concentration decreasing light scattering. However, the inhibitory effect of ginseng saponin appeared before a decrease in light scattering. These results suggest that low concentrations of ginseng saponins inhibit the membrane K^(+)-dependent phosphatase by interacting directly with enzyme before membrane disruption.

항 Histamine와 Muscarinic Receptor 와의 상호작용 (Ⅱ) : 대뇌 Muscarinic M1 Receptor 에 대한 작용 Action on the cerebral muscarinic M₁ Receptor

이신웅,박영주,박인숙,이정수 영남대학교 약품개발연구소 1991 영남대학교 약품개발연구소 연구업적집 Vol.1 No.-

A single uniform population of specific, saturable, high affinity binding site of [³H] guinuclidinyl benzilate(QNB) was identified in the rat cerebral microsomes. The Kd value(37.2 pM) for [³H]QNB calculated from the kinetically derived rate constants was in agreement with the Kd value(48.9 pM) determined by analysis of saturation isotherms at various receptor concentrations. Dimenhydrinate(DMH), histamine H₁-blocker, increased Kd value for [³H] QNB without affecting the binding site concentrations and this effect resulted from the ability of DMH to slow [³H]QNB-receptor association. Pirenzepine inhibition curve of [³H]QNB binding was shallow(nH = 0.52) indicating the presence of two receptor subtypes with high (M₁-site) and low(M₂-site) affinity for pirenzepine. Analysis of these inhibition curves yielded that 68% of the total receptor populations were of the M₁-subtype and the remaining 32% of the M₂-subtype. Ki values for the M₁- and M₂-subtypes were 2.42 nM and 629.3 nM, respectively. Ki values for H₁-blockers that inhibited [³H]QNB binding varied with a wide range (0.02-2.5μM). The Pseudo-Hill coefficients for inhibition of [³H]QNB binding by most of H₁-blockers examined except for oxomemazine inhibition of [³H]QNB binding were close to one. The inhibition curve for oxomemazine in competition with [³H]QNB was shallow(nH = 0.74) indicating the presence of two receptor populations with different affinities for this drug. The proportion of high and low affinity was 33:67. The Ki values for oxomemazine were 0.045±0.016 μM for high affinity and 1.145±0.232 μM for low affinity sites. These data indicate that muscarinic receptor blocking potency of H₁-blockers varies widely between different drugs and that most of H₁-blockers examined are nonselective antagonist for the muscarinic receptor subtypes, whereas oxomemazine might be capable of distinguishing between subclasses of muscarinic receptor.

쥐 심실에서 Digitalis Receptor Desensitization에 관한 연구

이신웅,이정수,장태수 영남대학교 약품개발연구소 1995 영남대학교 약품개발연구소 연구업적집 Vol.5 No.-

[³H]Ouabain binding parameters (K_(v) and B_(max)) to control rat ventricular strips and Langendorff preparations which were not previously exposed to ouabain were compared with those to both preparations that had been first exposed to a complete ouabain dose range of dose-response curve (10^(-5) M to 10^(-4) M). In rat ventricular strips and Langendorff perfused heart preparations, cumulative dose-response curves of ouabain revealed biphasic positive inotropic effects. a "low-dose" effect and a "high-dose" effect with ED_(50) values of 0.5 μM and 35 μM ouabain, respectively. The "low-dose" effect in ventricular strip disappeared or was diminished significantly when the ouabain dose-response curve was repeated after the washout of the effects of the first dose-response curve, whereas there were no significant differences in the maximal "high-dose" effect in both exposures to oubain. However, both of the control and ouabain-preexposed Langendorff perfused hearts revealed the same low-dose effects. The K_(D) value for [³H]ouabain binding and the ouabain binding site concentration (B_(max)) estimated by [³H]ouabain displacement assay in control preparations were 230 nM and 2 p㏖/㎎ protein, respectively. [³H]Ouabain binding parameters were not changed by repeated exposure to high concentrations of ouabain. These results suggest that digitalis receptor desensitization in the rat ventricular strip may due to the change of post-receptor events induced by ouabain binding to a high affinity site (a₂ isoform).

人蔘이 닭의 血中葡萄糖 및 遊離脂肪酸濃度에 미치는 影響

李神雄,李載欣,黃炳斗,琴基昌 충남대학교 의과대학 지역사회의학연구소 1974 충남의대잡지 Vol.1 No.1

Effect of Panax Ginseng on the plasma glucose and free fatty acid levels of the normal chicken and experimentally induced-hyperglycemic chicken, and on the release of glucose and glycogen contents in the chicken liver slices was investigated. 1) Plasma glucose levels was not influenced, but plasma FFA level decreased significantly by intravenous administration of Panax Ginseng in the normal chicken. 2) Epinephrine-induced hyperglycemic and hyperlipemic response and hyperglycemia induced by pancreatic ligation were inhibited by Panax Ginseng, and in the glucose tolerance test, Ginseng shortened the recovery time to normal glucose level. 3) In the chicken liver slices, Panax Ginseng inhibited the release of glucose from the specimen, but did not affect glycogen contents of the tissue.

니켈-크롬 합금에 폭로된 치과기공사들에서 자매염색분체 교환 빈도

신민정,성재혁,김웅철,이세훈 가톨릭대학산업의학센타 산업의학연구소 2002 韓國의 産業醫學 Vol.41 No.2

Nonprecious metal alloys were used in dental laboratories, may contain nickel, chromium, cobalt, molybdenum, beryllium, and small amounts gallium, ruthenium, or aluminum. Nonprecious metal alloys tend to rapid increase in use due to the economical merit. Despite the widespread use of Nickel-Chromium alloys, claims for safety of these alloys have not yet been accepted universally. This study was performed to investigate cytogenetic toxicity of Nickel-Chromium alloy in human cultured lymphocytes by sister chromatid exchange(SCE) which is a sensitive indicator of carcinogen and mutagen. Total subjects was divided into the two groups, including 34 Nickel-Chromium alloy exposed dental technicians and 24 control group members. 1. The frequencies of SCE were high in older than 40 years, but these was no statistical significance in two groups. 2. The effect of smoking on SCE values as higher than non-smokers in two groups, but there was no statistical significance. 3. The work duration also affected SCE frequencies, but these values didn't show any statistical difference between two groups. 4. The significant difference of SCE frequencies was found between Nickel-Chromium alloy exposed group and control group. 5. The SCE frequencies of current smoking exposed group was the highest and that of non-smoking control group was the lowest. The present study has shown that occupational exposure to Nickel-Chromium alloy is associated with an increase in SCE frequency.