2.Competitiveα-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid receptor antagonists:research advances
Dian XIAO ; Lingxiao WANG ; Xinbo ZHOU ; Song LI
Journal of International Pharmaceutical Research 2014;(4):407-412
α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropic glutamate receptors widely distributed in the central nervous system, mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases, such as epilepsy, amyotrophic lateral scelerosis,Parkinson′s dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor′s function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.
4. Competitive α-amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid receptor antagonists: Research advances
Journal of International Pharmaceutical Research 2014;41(4):407-412
α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropie glutamate receptors widely distributed in the central nervous system,mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases,such as epilepsy, amyotrophic lateral scelerosis, Parkinson's dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor's function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.
5.Role of heat shock protein 47 on experimental diabetic nephropathy of rats.
Dian-ge LIU ; Qing-juan ZHANG ; Zhuang GONG ; Xiao-chun WU ; Yu-feng LÜ
Chinese Journal of Pathology 2007;36(9):627-628
Actins
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metabolism
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Animals
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Collagen Type III
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metabolism
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Collagen Type IV
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metabolism
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Desmin
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metabolism
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Diabetes Mellitus, Experimental
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complications
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Diabetic Nephropathies
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metabolism
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pathology
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HSP47 Heat-Shock Proteins
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metabolism
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Kidney Glomerulus
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metabolism
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pathology
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Male
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Random Allocation
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Rats
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Rats, Sprague-Dawley
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Vimentin
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metabolism
6.Observation on effect of danxiaoling in supplementary treatment of intrahepatic cholestasis in pregnancy.
Dian-yun SHI ; Hua CHEN ; Mei XIAO
Chinese Journal of Integrated Traditional and Western Medicine 2002;22(2):116-118
OBJECTIVETo evaluate the curative effect of Danxiaoling Pill (DXLP), a Chinese herbal preparation, in treating intrahepatic cholestasis in pregnancy (ICP).
METHODSFifty-eight cases of ICP were divided randomly into two groups and treated by DXLP and Composite Yiganling as control respectively with the other identical conventional treatment. The changes of clinical symptoms, related laboratory parameters after treatment and the condition of labor were observed.
RESULTSThe total effective rate in both groups was 100%, but the markedly effective rate in the DXLP treated group was higher than that in control group (P < 0.01). Levels of blood cholyglycine acid (CGA), alanine transaminase (ALT), aspartate transaminase (AST), total bilirubin, total cholesterol and low density lipoprotein were all decreased in both groups after treatment, but DXL showed a better efficacy in decreasing CGA, ALT and AST than that of Yiganling. Moreover, the amniotic fluid meconium contaminated rate, premature delivery occurrence in the DXLP group were lower than those in the control group, while the weight of newborn baby was higher in the former than in the latter.
CONCLUSIONDXLP could effectively lower the serum bile acid and improve liver function in treating ICP.
Adult ; Alanine Transaminase ; blood ; Aspartate Aminotransferases ; blood ; Cholestasis, Intrahepatic ; blood ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Glycocholic Acid ; blood ; Humans ; Phytotherapy ; Pregnancy ; Pregnancy Complications ; blood ; drug therapy
7.Study on effect of pH on rectum permeability of active ingredients in Reduning suppositories in vitro.
Ming YAN ; Ying-chun WEI ; Jin MENG ; Dian-hong XU ; Yun WU ; Wei XIAO
China Journal of Chinese Materia Medica 2015;40(8):1493-1496
OBJECTIVETo investigate the effect of different pH on rectum permeability of chlorogenic acid and geniposide.
METHODFour kinds of Reduning suppositories of different pH were separated and put into the rectum to study the suppositories in vitro and the content of chlorogenic acid and geniposide samples was determined by HPLC to calculate the permeation in 24 hours.
RESULTWith increase of pH within 2.5-7.4, the steady state flux of chlorogenic acid was increased, but the steady state flux of geniposidesamples was steady.
CONCLUSIONAdjusted the pH can increase the rectum permeability of active ingredients in Reduning auppositories.
Animals ; Chlorogenic Acid ; pharmacokinetics ; Drugs, Chinese Herbal ; pharmacokinetics ; Hydrogen-Ion Concentration ; Iridoids ; pharmacokinetics ; Male ; Permeability ; Rats ; Rats, Sprague-Dawley ; Rectum ; metabolism ; Suppositories ; pharmacokinetics
8.A continuous-monitoring procedure of alkaline phosphatase activity with p-acetylphenylphosphace as substrate
Ling WANG ; Zhong-Xin LI ; Dian-Jun WEI ; Xiao-Qin DING ; Zong-Hua HU ; Hui JIN ;
Chinese Journal of Laboratory Medicine 2001;0(03):-
Objective To establish a new determination method for the measuring of alkaline phosphatase activity (ALP) with p-acetyl phenyl phosphace (PAP-PNa_2) as substrate.Methods With the help of Vital semiautomatic analyzer,researched a continuous-monitoring procedure and set up experimental parameters.Results When using this assay,the wavelength of PAP's absorption was 325 nm and the Km of ALP was 0.376 mmol/L.The molecular extinction coefficient of PAP at 340 nm was 23 390 L?mol~(-1)? cm~(-1) and the concentration of citrate buffer was 0.438 mol/L.During the process,we found that the optimum pH of enzyme was 10.4,and the concentration of substrate was 5.0 mmol/L.The time of linear reaction was 900 seconds,and the linear range was 0-1 110 U/L.Serum total ALP were 63.1-118.3 U/ L(male) and 52.5-89.0 U/L(female),based on results from 60 heath adults.Conclusions The method is practical in its repetition and convenience,saves time and is not liable to be affected by bilirubin in serum.It is especially suited to the use of automatic analyzers.
9. AMPA receptor positive modulator, ampakines: research progress
Journal of International Pharmaceutical Research 2019;46(5):325-331
Ampakines are a class of pharmacological agents acting as positive modulators of AMPA receptors. Currently, clinical indications studied for ampakines involve many diseases including the respiratory depression and psychoneurosis, etc. The studies using CX516 and CX546 as tool compounds have shown that ampakines could be classified into "high impact ampakines"and "low impact ampakines". The two subclasses of ampakines differ in the chemical structures, influences on receptor dynamics, receptor-ligand bindings, synaptic transmissions, neurotrophin regulations and side effects. According to the available literature, the low impact ampakines have better clinical application prospects than high impact ampakines because of their high safety and good tolerance. The above different characteristics of the two subclasses of ampakines are reviewed in this paper.
10.Observation of Ex - press miniature implantation with deep sclerectomy surgery for refractory glaucoma
Yu, DI ; Qing-Zhu, NIE ; Dian-Wen, GAO ; Xiao-Long, CHEN
International Eye Science 2016;16(6):1150-1152
?AIM: To evaluate the effect for refractory glaucoma by using Ex - Press miniature implantation with deep sclerectomy.?METHODS: Thirty eyes in 24 patients with refractory glaucoma were treated by Ex- Press miniature ( P50 ) implantation with deep sclerectomy. The patients’ symptom, intraocular pressure ( IOP ) , visual acuity and complications were analyzed in a 12mo follow-up period.?RESULTS: During the follow-up period, all patients’ ocular pain was reduced. The mean IOP before operation and at the last follow-up time were 51. 15 ± 2. 60mmHg (1kPa=7. 5mmHg) and 15. 11 ± 2. 51mmHg, respectively, there was significant difference (P<0. 05). Postoperative visual acuity was improved in 8 eyes, had no significant change in 22 eyes. After operation, hyphema of anterior chamber appeared in 2 eye ( 7%) , which were obsorbed after 1wk.? CONCLUSION: Ex - Press miniature implantation combined with deep sclerectomy surgery is a relatively effective and safe treatment for the patients with refractory glaucoma. This method can significantly degrade the IOP, lessen ocular pain and reduce the complications risk.