Eight new cyclopyrrolone compounds were synthesized according to the structure activity relationship and action mechanism of Zopiclone, a cyclopyrrolone hypnotic. Their preliminary pharmacodynamics are under investig...Eight new cyclopyrrolone compounds were synthesized according to the structure activity relationship and action mechanism of Zopiclone, a cyclopyrrolone hypnotic. Their preliminary pharmacodynamics are under investigation.展开更多
AIM：To examine possible differences in clinical outcomes between sub-threshold micro-pulse diode laser photocoagulation（SDM） and traditional modified Early Treatment Diabetic Retinopathy Study（mETDRS）treatment pr...AIM：To examine possible differences in clinical outcomes between sub-threshold micro-pulse diode laser photocoagulation（SDM） and traditional modified Early Treatment Diabetic Retinopathy Study（mETDRS）treatment protocol in diabetic macuiar edema（DME）.METHODS：A comprehensive literature search using the Cochrane Collaboration methodology to identify RCTs comparing SDM with mETDRS for DME.The participants were type Ⅰ or type Ⅱ diabetes mellitus with clinically significant macuiar edema treated by SDM from previously reported randomized controlled trials（RCTs）.The primary outcome measures were the changes in the best corrected visual acuity（BCVA） and the central macuiar thickness（CMT） as measured by optical coherence tomography（OCT）.The secondary outcomes were the contrast sensitivity and the damages of the retina.RESULTS：Seven studies were identified and analyzed for comparing SDM（215 eyes） with mETDRS（210 eyes）for DME.There were no statistical differences in the BCVA after treatment between the SDM and mETDRS based on the follow-up：3mo（MD,-0.02;95% Cl,-0.12 to 0.09;P=0.77）,6mo（MD,-0.02;95% Cl,-0.12 to 0.09;P=0.75）,12mo（MD,-0.05;95% Cl,-0.17 to 0.07;P=0.40）.Likewise,there were no statistical differences in the CMT after treatment between the SDM and mETDRS in 3mo（MD,-9.92;95% Cl,-28.69 to 8.85;P=0.30）,6mo（MD,-11.37;95% Cl,-29.65 to 6.91;P=0.22）,12mo（MD,8.44;95% Cl,-29.89 to 46.77;P=0.67）.Three RCTs suggested that SDM laser results in good preservation of contrast sensitivity as mETDRS,in two different followup evaluations：3mo（MD,0.05;95% Cl,0 to 0.09;P=0.04） and 6mo（MD,0.02;95% Cl,-0.10 to 0.14;P=0.78）.Two RCTs showed that the SDM laser treatment did less retinal damage than that mETDRS did（OR,0.05;95% Cl,0.02 to 0.13;P〈0.01）.CONCLUSION：SDM laser photocoagulation shows an equally good effect on visual acuity,contrast sensitivity,and reduction of DME as compared to conventional mETDRS protocol with less retinal damage.展开更多
OBJECTIVE Licorice is used throughout the world as a traditional herbal remedy.According to Chinese traditional medicine licorice alone can be used to treat inflammation.Although there have been some studies investiga...OBJECTIVE Licorice is used throughout the world as a traditional herbal remedy.According to Chinese traditional medicine licorice alone can be used to treat inflammation.Although there have been some studies investigated the anti-inflammatory ingredients of licorice,but for the potency of flavonoid glycoside and their aglycones on inflammation are not evaluated.This study was designed to assess the contributions of licorice flavonoid glycosides and their aglycons to its anti-inflammatory and hypnotic effects.METHODS For the flavonoid aglycone's enrichment,the extract of licorice(EL)was fermented in submerged culture of the edible fungus Grifola frondosa HB0071 mycelia which can produce β-glucosidase and catalyze the flavonoid glycosides to aglycones.EL and fermented extract of licorice(FEL) were used in this study.The anti-inflammation test was carried out in arachidonic acid(AA)-induced ear edema model and the hypnotic test was performed by using electroencephalogram(EEG) analysis method in normal freely moving SD rats.The chemicals constituents were analyzed by HPLC.RESULTS During fermentation,the falvonoid glycosides of licorice were hydrolyzed by the time process.Along with fermentation time,the concentration of the major flavonoid glycosides,liquiritin and isoliquiritin were decreased obviously,and simultaneously their aglycons,liquiritigenin and isoliquiriti.genin were remarkably increased in FEL.Moreover,the content of another major constituent glycyrrhi.zic acid and glycyrrhetinic acid were not changed after the fermentation.In AA-induced mice ear ede.ma test,after topical application,FEL(effective dose range:5-20 μg·ear-1) showed more potent inhibito.ry activity than EL(effective dose range:25-100 μg·ear-1).On the other hand,oral administration of EL and FEL exhibited the same hypnotic potency and both enhanced the total sleep time including rapid eye movement(REM) sleep and non-REM sleep time.CONCLUSION These results suggested that the enrichment of flavonoid aglycons such as liquiritigenin and isoliquiritigenin enhanced the anti-inflam.matory potency of licorice extract,and this potentiation has nothing to do with glycyrrhizic acid or glycyr.rhetinic acid.In addition,enrichment of flavonoid aglycones did not alter the hypnotic effect of licorice.展开更多
On the basis of the Zaleplon structure, novel pyrazolo[l,5-a]pyrimidines were designed and prepared for studies on their hypnotic activity. This paper reported the synthesis of twelve new 5-methyl-7-substituted-pyrazo...On the basis of the Zaleplon structure, novel pyrazolo[l,5-a]pyrimidines were designed and prepared for studies on their hypnotic activity. This paper reported the synthesis of twelve new 5-methyl-7-substituted-pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives by using simple starting materials such as propane dinitrile and triethyl orthoformate. The structures of the derived target compounds were confirmed by their IR and 1H-NMR spectroscopic data. The preliminary pharmacological evaluations indicated that some compounds showed hypnotic activity, while derivative 1c was the most polent one.展开更多
With a small-dose remifentanil, some patients showed no reaction and did not remember it postoperatively. We, therefore, hypothesized that remifentanil may decrease the level of consciousness and/or exhibit amnesic ef...With a small-dose remifentanil, some patients showed no reaction and did not remember it postoperatively. We, therefore, hypothesized that remifentanil may decrease the level of consciousness and/or exhibit amnesic effect when stimulations are avoided. Thirty-patients were divided into two groups: non-stimulation group and stimulation group. Anesthesia was induced with 1 micro-g·kg?1·min?1 of remifentanil using no additional hypnotic agent. In the non-stimulation group, patients were left free from any stimulation except non-invasive blood pressure monitoring. In the stimulation group, patients were asked to follow verbal commands. The level of consciousness was evaluated with electroencephalogram and BIS-value derived from it. In the non-stimulation group, all patients reached the decreased level of consciousness in 5 minutes. In the stimulation group, however, 14 patients were judged to be still conscious. 10 patients could open their mouth at the 5th minute, but 9 of these 10 patients did not remember it postoperatively. In conclusion, remifentanil, with no additional anesthetics, exhibited hypnotic and amnesic effects when stimulations were kept minimal.展开更多
Digital circuits operating in the sub-threshold regime consume the least energy. The strict energy constraints are desired in the applications which work at the lowest possible supply voltage. On the other hand, the c...Digital circuits operating in the sub-threshold regime consume the least energy. The strict energy constraints are desired in the applications which work at the lowest possible supply voltage. On the other hand, the conventional design flow utilizes the technology library provided by the foundry with a fixed voltage boundary, which causes problems when the supply scales down to the sub-threshold regime. In this paper, we present a design methodology to characterize the existing cell library with Liberty NCX to facilitate the standard design flow. It is demonstrated in 0.13 μm complementary metal-oxide-semiconductor （CMOS） technology with the supply voltage of 300 mV.展开更多
Leakage power and propagation delay are two significant issues found in sub-micron technology-based Complementary Metal-Oxide-Semiconductor(CMOS)-based Very Large-Scale Integration(VLSI)circuit designs.Positive Channel...Leakage power and propagation delay are two significant issues found in sub-micron technology-based Complementary Metal-Oxide-Semiconductor(CMOS)-based Very Large-Scale Integration(VLSI)circuit designs.Positive Channel Metal Oxide Semiconductor(PMOS)has been replaced by Negative Channel Metal Oxide Semiconductor(NMOS)in recent years,with low dimen-sion-switching changes in order to shape the mirror of voltage comparator.NMOS is used to reduce stacking leakage as well as total exchange.Domino Logic Cir-cuit is a powerful and versatile digital programmer that gained popularity in recent years.In this study regarding Adaptive Sub Threshold Voltage Level Control Pro-blem,the researchers intend to solve the contention issues,reduce power dissipa-tion,and increase the noise immunity by proposing Adaptive Sub Threshold Voltage Level Control(ASVLC)-based domino circuit.The efficiency and effec-tiveness of the domino circuit are demonstrated through simulation results.The suggested system makes use of high-speed broad fan-gate circuits,occupies mini-mum space,and consumes meagre amount of power.The proposed circuit was validated in Cadence simulation tool at a supply voltage of 1V,frequency of 100 MHz,and an operating temperature of 27°C with 64 input OR gates.As per the simulation results,the suggested Domino Gate reduced the power dissipa-tion by 17.58 percent and improved the noise immunity by 1.21 times in compar-ison with standard domino logic circuits.展开更多
Aim. To statistic the usage of hypnotics and sedatives in outpatient and emergency clinics prescriptions in one day. Method. Check all prescriptions on April 29, 1987 and November 13, 1995 in order to know the quantit...Aim. To statistic the usage of hypnotics and sedatives in outpatient and emergency clinics prescriptions in one day. Method. Check all prescriptions on April 29, 1987 and November 13, 1995 in order to know the quantity, kind and distribution of hypnotics and sedatives in different outpatient departments. Result. There were 1 319 prescriptions on April 29, 1987. Among them, hypnotics and sedatives were 122(9. 24%); in comparing with 2 065 prescriptions on November 13, 1995, hypnotics and sedatives were 141 (6. 82%). Benzodiazepine used more than 80% in all prescriptions. Conclusion. The possibility of long-term low-dosage using benzodiazepine is present. It must strengthen the control and education to avoid the drug-abuse.展开更多
文摘Eight new cyclopyrrolone compounds were synthesized according to the structure activity relationship and action mechanism of Zopiclone, a cyclopyrrolone hypnotic. Their preliminary pharmacodynamics are under investigation.
文摘AIM：To examine possible differences in clinical outcomes between sub-threshold micro-pulse diode laser photocoagulation（SDM） and traditional modified Early Treatment Diabetic Retinopathy Study（mETDRS）treatment protocol in diabetic macuiar edema（DME）.METHODS：A comprehensive literature search using the Cochrane Collaboration methodology to identify RCTs comparing SDM with mETDRS for DME.The participants were type Ⅰ or type Ⅱ diabetes mellitus with clinically significant macuiar edema treated by SDM from previously reported randomized controlled trials（RCTs）.The primary outcome measures were the changes in the best corrected visual acuity（BCVA） and the central macuiar thickness（CMT） as measured by optical coherence tomography（OCT）.The secondary outcomes were the contrast sensitivity and the damages of the retina.RESULTS：Seven studies were identified and analyzed for comparing SDM（215 eyes） with mETDRS（210 eyes）for DME.There were no statistical differences in the BCVA after treatment between the SDM and mETDRS based on the follow-up：3mo（MD,-0.02;95% Cl,-0.12 to 0.09;P=0.77）,6mo（MD,-0.02;95% Cl,-0.12 to 0.09;P=0.75）,12mo（MD,-0.05;95% Cl,-0.17 to 0.07;P=0.40）.Likewise,there were no statistical differences in the CMT after treatment between the SDM and mETDRS in 3mo（MD,-9.92;95% Cl,-28.69 to 8.85;P=0.30）,6mo（MD,-11.37;95% Cl,-29.65 to 6.91;P=0.22）,12mo（MD,8.44;95% Cl,-29.89 to 46.77;P=0.67）.Three RCTs suggested that SDM laser results in good preservation of contrast sensitivity as mETDRS,in two different followup evaluations：3mo（MD,0.05;95% Cl,0 to 0.09;P=0.04） and 6mo（MD,0.02;95% Cl,-0.10 to 0.14;P=0.78）.Two RCTs showed that the SDM laser treatment did less retinal damage than that mETDRS did（OR,0.05;95% Cl,0.02 to 0.13;P〈0.01）.CONCLUSION：SDM laser photocoagulation shows an equally good effect on visual acuity,contrast sensitivity,and reduction of DME as compared to conventional mETDRS protocol with less retinal damage.
文摘OBJECTIVE Licorice is used throughout the world as a traditional herbal remedy.According to Chinese traditional medicine licorice alone can be used to treat inflammation.Although there have been some studies investigated the anti-inflammatory ingredients of licorice,but for the potency of flavonoid glycoside and their aglycones on inflammation are not evaluated.This study was designed to assess the contributions of licorice flavonoid glycosides and their aglycons to its anti-inflammatory and hypnotic effects.METHODS For the flavonoid aglycone's enrichment,the extract of licorice(EL)was fermented in submerged culture of the edible fungus Grifola frondosa HB0071 mycelia which can produce β-glucosidase and catalyze the flavonoid glycosides to aglycones.EL and fermented extract of licorice(FEL) were used in this study.The anti-inflammation test was carried out in arachidonic acid(AA)-induced ear edema model and the hypnotic test was performed by using electroencephalogram(EEG) analysis method in normal freely moving SD rats.The chemicals constituents were analyzed by HPLC.RESULTS During fermentation,the falvonoid glycosides of licorice were hydrolyzed by the time process.Along with fermentation time,the concentration of the major flavonoid glycosides,liquiritin and isoliquiritin were decreased obviously,and simultaneously their aglycons,liquiritigenin and isoliquiriti.genin were remarkably increased in FEL.Moreover,the content of another major constituent glycyrrhi.zic acid and glycyrrhetinic acid were not changed after the fermentation.In AA-induced mice ear ede.ma test,after topical application,FEL(effective dose range:5-20 μg·ear-1) showed more potent inhibito.ry activity than EL(effective dose range:25-100 μg·ear-1).On the other hand,oral administration of EL and FEL exhibited the same hypnotic potency and both enhanced the total sleep time including rapid eye movement(REM) sleep and non-REM sleep time.CONCLUSION These results suggested that the enrichment of flavonoid aglycons such as liquiritigenin and isoliquiritigenin enhanced the anti-inflam.matory potency of licorice extract,and this potentiation has nothing to do with glycyrrhizic acid or glycyr.rhetinic acid.In addition,enrichment of flavonoid aglycones did not alter the hypnotic effect of licorice.
文摘On the basis of the Zaleplon structure, novel pyrazolo[l,5-a]pyrimidines were designed and prepared for studies on their hypnotic activity. This paper reported the synthesis of twelve new 5-methyl-7-substituted-pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives by using simple starting materials such as propane dinitrile and triethyl orthoformate. The structures of the derived target compounds were confirmed by their IR and 1H-NMR spectroscopic data. The preliminary pharmacological evaluations indicated that some compounds showed hypnotic activity, while derivative 1c was the most polent one.
文摘With a small-dose remifentanil, some patients showed no reaction and did not remember it postoperatively. We, therefore, hypothesized that remifentanil may decrease the level of consciousness and/or exhibit amnesic effect when stimulations are avoided. Thirty-patients were divided into two groups: non-stimulation group and stimulation group. Anesthesia was induced with 1 micro-g·kg?1·min?1 of remifentanil using no additional hypnotic agent. In the non-stimulation group, patients were left free from any stimulation except non-invasive blood pressure monitoring. In the stimulation group, patients were asked to follow verbal commands. The level of consciousness was evaluated with electroencephalogram and BIS-value derived from it. In the non-stimulation group, all patients reached the decreased level of consciousness in 5 minutes. In the stimulation group, however, 14 patients were judged to be still conscious. 10 patients could open their mouth at the 5th minute, but 9 of these 10 patients did not remember it postoperatively. In conclusion, remifentanil, with no additional anesthetics, exhibited hypnotic and amnesic effects when stimulations were kept minimal.
基金supported by the Important National S&T Special Project of China under Grant No.2011ZX01034-002-001-2
文摘Digital circuits operating in the sub-threshold regime consume the least energy. The strict energy constraints are desired in the applications which work at the lowest possible supply voltage. On the other hand, the conventional design flow utilizes the technology library provided by the foundry with a fixed voltage boundary, which causes problems when the supply scales down to the sub-threshold regime. In this paper, we present a design methodology to characterize the existing cell library with Liberty NCX to facilitate the standard design flow. It is demonstrated in 0.13 μm complementary metal-oxide-semiconductor （CMOS） technology with the supply voltage of 300 mV.
文摘Leakage power and propagation delay are two significant issues found in sub-micron technology-based Complementary Metal-Oxide-Semiconductor(CMOS)-based Very Large-Scale Integration(VLSI)circuit designs.Positive Channel Metal Oxide Semiconductor(PMOS)has been replaced by Negative Channel Metal Oxide Semiconductor(NMOS)in recent years,with low dimen-sion-switching changes in order to shape the mirror of voltage comparator.NMOS is used to reduce stacking leakage as well as total exchange.Domino Logic Cir-cuit is a powerful and versatile digital programmer that gained popularity in recent years.In this study regarding Adaptive Sub Threshold Voltage Level Control Pro-blem,the researchers intend to solve the contention issues,reduce power dissipa-tion,and increase the noise immunity by proposing Adaptive Sub Threshold Voltage Level Control(ASVLC)-based domino circuit.The efficiency and effec-tiveness of the domino circuit are demonstrated through simulation results.The suggested system makes use of high-speed broad fan-gate circuits,occupies mini-mum space,and consumes meagre amount of power.The proposed circuit was validated in Cadence simulation tool at a supply voltage of 1V,frequency of 100 MHz,and an operating temperature of 27°C with 64 input OR gates.As per the simulation results,the suggested Domino Gate reduced the power dissipa-tion by 17.58 percent and improved the noise immunity by 1.21 times in compar-ison with standard domino logic circuits.
文摘Aim. To statistic the usage of hypnotics and sedatives in outpatient and emergency clinics prescriptions in one day. Method. Check all prescriptions on April 29, 1987 and November 13, 1995 in order to know the quantity, kind and distribution of hypnotics and sedatives in different outpatient departments. Result. There were 1 319 prescriptions on April 29, 1987. Among them, hypnotics and sedatives were 122(9. 24%); in comparing with 2 065 prescriptions on November 13, 1995, hypnotics and sedatives were 141 (6. 82%). Benzodiazepine used more than 80% in all prescriptions. Conclusion. The possibility of long-term low-dosage using benzodiazepine is present. It must strengthen the control and education to avoid the drug-abuse.
