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1.
Experimental Neurobiology ; : 529-536, 2019.
Article in English | WPRIM | ID: wpr-763775

ABSTRACT

Stress can induce a serious epileptic encephalopathy that occurs during early infancy. Recent studies have revealed that prenatal stress exposure is a risk factor for the development of infantile spasms. Our previous work demonstrates that prenatal stress with betamethasone-induced alterations to the expression of the K⁺/Cl⁻ co-transporter (KCC2) in gamma-aminobutyric acid (GABA) interneurons lowers the seizure threshold in exposed animals. Here, we further investigated the mechanisms involved in this KCC2 dysfunction and explored possible treatment options. We stressed Sprague-Dawley rats prenatally and further treated dams with betamethasone on gestational day 15, which increases seizure susceptibility and NMDA (N-Methyl-D-aspartate)-triggered spasms on postnatal day 15. In this animal model, first, we evaluated baseline calpain activity. Second, we examined the cleavage and dephosphorylation of KCC2. Finally, we checked the effect of a calpain inhibitor on seizure occurrence. The phosphorylated-N-methyl-D-aspartate Receptor 2B (NR2B):non-phosphorylated NR2B ratio was found to be higher in the cortex of the prenatally stressed beta-methasone model. We further found that the betamethasone model exhibited increased phosphorylation of calpain-2 and decreased phosphorylation of KCC2 and Glutamic acid decarboxylase 67 (GAD67). After using a calpain inhibitor in prenatal-stress rats, the seizure frequency decreased, while latency increased. GABAergic depolarization was further normalized in prenatal-stress rats treated with the calpain inhibitor. Our study suggests that calpain-dependent cleavage and dephosphorylation of KCC2 decreased the seizure threshold of rats under prenatal stress. Calpain-2 functions might, thus, be targeted in the future for the development of treatments for epileptic spasms.


Subject(s)
Animals , Humans , Infant , Infant, Newborn , Rats , Betamethasone , Brain Diseases , Calpain , Epilepsy , gamma-Aminobutyric Acid , Glutamate Decarboxylase , Interneurons , Models, Animal , N-Methylaspartate , Phosphorylation , Rats, Sprague-Dawley , Risk Factors , Seizures , Spasm , Spasms, Infantile
2.
An. acad. bras. ciênc ; 89(3,supl): 2505-2513, 2017. tab, graf
Article in English | LILACS | ID: biblio-886805

ABSTRACT

ABSTRACT Sodium chloride is traditionally used as a food additive in food processing. However, because of its high sodium content, NaCl has been associated with chronic diseases. Margarine is a popular product that is used in several preparations, but it includes high sodium content; therefore, it is among the products whose sodium content should be reduced. Thus, the objective of this study was to produce margarines with reduced sodium content prepared using a salt mixture. The following 4 margarine formulations were prepared: Formulation A (control - 0% sodium reduction), Formulation B (20.8% less sodium), Formulation C (33.0% less sodium) and Formulation D (47.4% less sodium). The low sodium formulations were produced using a salt mixture consisting of NaCl, KCl, and monosodium glutamate at different concentrations. The margarines were evaluated using an acceptance test and descriptive tests: time-intensity and temporal dominance of sensations. The mixture used is a good alternative for preparing low sodium margarine because the low sodium formulations feature equal salinity and do not produce a strange or bad taste. Furthermore, it may be possible to prepare margarines with up to 47.4% less sodium and that are acceptable to consumers.


Subject(s)
Sensation , Taste , Sodium Chloride, Dietary/administration & dosage , Food Handling/methods , Margarine/analysis , Time Factors
3.
Chinese Pharmacological Bulletin ; (12): 74-83, 2017.
Article in Chinese | WPRIM | ID: wpr-509258

ABSTRACT

Aim To explore the effects of hypertension on the contractibility of rat basilar artery and its inter-actions with the sodium pump activity.Methods The basilar artery was respectively isolated from Wistar and SHR rats,and the isometric tension of arterial rings was measured by Multi Myograph System-610M.The cont-ractibilities of arterial rings induced by KCl or 5-HT were compared between the basilar arteries of the two groups of rats to analyze the effect of hypertension on the cerebral vascular tension and the activity of sodium pump.Results In SHR rats,the concentration-re-sponse curves of the contraction of isolated basilar ar-tery rings induced by KCl and 5-HT were significantly shifted to right,and the relaxation of vascular tone in-duced by K+which was reintroduced from the external was attenuated compared with those in the WR.These results suggested that hypertension could significantly decrease the activity of the sodium pump and the con-tractile responses of KCl and 5-HT.OUA could con-tract the basilar artery in a concentration-dependent manner,and its concentration-response curve was opti-mally fitted by a two-site binding model:Kd was 1.7 ×10 -8 and 1.6 ×10 -5 mol·L-1,respectively.The results indicated that the two different function sodium pumps existed in the rat basilar artery:one with the high OUA affinity and the other with the low OUA af-finity.If the high and low affinity sodium pumps were inhibited by 5 ×10 -7 and 10 -4 mol · L-1 OUA,re-spectively,the concentration-response curves of KCl and 5-HT would shift to left in SHR rats but not in WR rats.It suggested that OUA could enhance the contrac-tion induced by KCl and 5-HT significantly,and a concentration-dependent effect was observed in the SHR vascular contraction induced by 5-HT (r =0.9393 ,P<0.05 ).When the two concentrations of OUA were applied,there was no significant difference in the shift left of the concentration-response curves in-duced by KCl in the SHR cerebral vessels.However, the marked difference was shown in the shift left in-duced by 5-HT.The results implied that only the high affinity sodium pump was involved in the contractile re-sponse of SHR cerebral vascular to KCl,whereas,the contractile response of SHR cerebral vascular to 5-HT was induced by both high and low affinity sodium pumps.Conclusion Hypertension could lower the contractile response of the basilar artery to vasocon-strictors,and the mechanism might relate to the de-creased sensitivity of the sodium pump induced by hy-pertension or the increased sensibility of the sodium pump to OUA.

4.
Chinese Pharmacological Bulletin ; (12): 1703-1706, 2017.
Article in Chinese | WPRIM | ID: wpr-667973

ABSTRACT

Aim To investigate the protective effects of S-adenosylmethionine (SAM)on KCl-stimulated pri-mary cultured neurons and the potential mechanism. Methods The primary cultured cortical neurons were randomly divided into three groups:normal (Con) group,KCl group and SAM-KCl group. The changes of cell morphology were observed by microscope,and the mRNA and protein expression levels of caveolin-1 (Cav-1)in each group were detected by qPCR and Western blot. Results After treated with 0. 05 mol· L - 1 KCl for 12 hours,the primary cultured neurons showed morphological injury,shortening of neurites, reduction of soma mass and accumulation of cells. While neurons pretreated with 0. 02 mol·L-1 SAM for 6 hours could significantly reduce the damage induced by KCl. qPCR and Western blot analysis showed that SAM could reduce the neurons expression of Cav-1 mRNA and protein that induced by KCl. Conclusion SAM can protect neurons from the damage induced by KCl,and Cav-1 plays a critical role in this process.

5.
China Pharmacist ; (12): 1016-1019, 2017.
Article in Chinese | WPRIM | ID: wpr-619675

ABSTRACT

Objective: To study the influence of Xinmailong injection (XML) on the isolated thoracic aorta of rats in different states.Methods: A cumulative dosing method was utilized to evaluate the influence of XML on the isolated thoracic aorta of rats in resting state, and KCl or noradrenaline (NA) induced contracted state.Different tool drugs were used to analyze the mechanism of the effects.Results: Compared with the control group, a specific concentration range of XML could excite the isolated thoracic aorta in resting state, further increase the vascular tension after KCl action, while decrease the vascular tension after NA action.The vasodilative effect of XML on blood vessel after NA action was inhibited by propranolol and diclofenac, while showed no influence from Nω-Nitro-L-arginine.Conclusion: XML has different effects on the isolated thoracic aorta of rats in different states, and the mechanisms of the effects are related to calcium channel, β-receptor and prostaglandins.

6.
Chinese Journal of Emergency Medicine ; (12): 650-653, 2017.
Article in Chinese | WPRIM | ID: wpr-619369

ABSTRACT

Objective To study the effect of potassium chloride (KCl) before CPR on successful resuscitation of rats with ventricular fibrillation (VF).Methods Sprague-Dawley (SD) rats with VF induced by alternating electricity current were randomly (ramdam runmber) divided into KCl group and normal saline (NS) group.Rats of two groups were prepared with 0.8 mL/kg of 2.5% KCl in KCI group and equivalent volume of NS in NS group instead before CPR.The resuscitation was considered to be failure if ROSC was absent for 10 min.The comparisons of time required for ROSC,the average attempt of defibrillation,the average joule used for defibrillation,ROSC rate and 72 h survival rate were carried out between the two groups.Results The length of time required for ROSC in the KCl group (n =10) was shorter than that in NS group (n=10) [(283.89±152.44) svs.(404.38±164.27) s] (t=1.369,P =0.196).The average attempt of defibrillation in KCl group were fewer compared to the NS group [(1.50 ± 0.75) times vs.(2.66 ± 0.57) times,(t =2.701,P =0.022)],the average joule used for defibrillation in KCl group were less compared to NS group [(3.75 ± 2.86) J vs.(8.33 ± 2.88) J,(t =2.78,P =0.019)].The ROSC rate in the KCl group was higher than that in NS group (P =0.011).The 72 h survival rate in KCl group was higher than that in NS group (P =0.001).Conclusions Increasing plasma potassium level before CPR could increase the ROSC rate and survival rate in rats with VF.

7.
Journal of the Korean Ophthalmological Society ; : 724-733, 2016.
Article in Korean | WPRIM | ID: wpr-58328

ABSTRACT

PURPOSE: To evaluate the effect and prognostic factors of automated thermodynamic treatment (thermal compression therapy device [KCL 1100®]) for Meibomian gland dysfunction (MGD). METHODS: Patients (48 eyes of 24 subjects) with MGD were recruited for a prospective clinical trial. Patients received 15-minute treatments twice a day using the KCL 1100®. Severity of dry eye symptoms were evaluated using the Standard Patient Evaluation for Eye Dryness (SPEED) and Ocular Surface Disease Index (OSDI), and severity of Meibomian gland function was evaluated using the Meibomian gland expressibility (MGE), Meibomian gland secretion (MGS) score and lipid layer thickness measured by LipiView®. To evaluate ocular surface, we measured tear break-up time (BUT) and fluorescein corneal staining score (Oxford scale). Data were presented for baseline and at 2 weeks and 1 month post-treatment. RESULTS: Dry eye symptom (SPEED, OSDI), Meibomian gland function (MGE, MGS), and ocular surface index (BUT, Oxford scale) of patients were significantly improved from baseline to 2 weeks (p 0.05). There were no significant adverse events during the treatment. CONCLUSIONS: KCL 1100® automated thermodynamic treatment is an effective and safe treatment for MGD. Additionally, KCL 1100® is more effective in patients with moderate dry eye symptom and MGD.


Subject(s)
Humans , Fluorescein , Meibomian Glands , Prospective Studies , Tears , Thermodynamics
8.
Acta Laboratorium Animalis Scientia Sinica ; (6): 188-193, 2015.
Article in Chinese | WPRIM | ID: wpr-464725

ABSTRACT

Objective To investigate the potential of chronic myeloid leukemia ( CML) cell line KCL22 in indu-cing leukemia in NOD-SCID mice for setting up a basis for constructing a CML mouse transplantation tumor model. Methods 2 ×107 KCL22 cells in logarithmic growth phase were injected via the tail vein into experimental NOD-SCID mice whereas PBS was injected to the mice of control group.General condition of the mice of both groups was observed.Wright staining was used to observe the changes of blood and bone marrow smears.PCR was conducted to detect the transcription level of BCR-ABL, and histology with HE staining was used to evaluate the tumor cell invasion in the liver and spleen. Results Four weeks after the injection of KCL22 cells, the mice in experimental group showed physical signs of decreased reactivity, depression, swollen hindlimb muscles and petechia on the hindlimb femur.Peripheral white blood cells ( WBC) began to increase after 5 weeks, with a significantly increased quantity compared with the control group (P90 days) (P<0.05).Conclusions A NOD-SCID mouse model of CML transplantation tumor is successfully established with leukemia KCL22 cells.

9.
Medical Journal of Chinese People's Liberation Army ; (12): 616-621, 2015.
Article in Chinese | WPRIM | ID: wpr-850253

ABSTRACT

Objective To analyze the influence of SH3 domain mutant (ABL SH3-T79Y) in BCR-ABL protein of chronic myeloid leukemia (CML) in combination with imatinib (IM) on the proliferation of CML cells in vivo and vitro, and to discuss the mechanism thereof. Methods Recombinant ABL SH3-T79Y mutant adenovirus vectors which were successfully constructed in previous work was used with IM to treat K562/G01 cells, then the cell-colony forming ability of K562/G01 cells was determined by clone formation assay, and cell cycle was assessed by flow cytometry. KCL22 cells were treated by recombinant SH3-T79Y and IM to construct subcutaneous solid tumor model in Balb/c nude mice, then the formation rate of subcutaneous tumor was estimated, the pathological examination was conducted, and the proliferation ability of KCL22 cells was assayed. K562/G01 cells were treated by SH3-T79Y and IM in combination, and the expression levels of p-BCR-ABL, BCR-ABL, p-CrkL, CrkL and Cyclin-D1 protein were determined by Western blotting. Cells treated with PBS, null recombinant adenovirus vectors or IM alone served as control groups. Results Compared to the 3 control groups, clone forming rate of K562/G01 cells decreased significantly (P<0.05) and cell cycles were arrested at S phase after being combined SH3-T79Y and IM treatment. The subcutaneous solid tumor formation rate in KCL22- Balb/c nude mice was 16.7% after combined SH3-T79Y and IM treatment, and large number of tumor cells were observed in tumor pathology examination. Western blotting revealed that the expression levels of p-BCR-ABL, p-CrkL, BCR-ABL, CrkL and Cyclin-D1 were decreased in K562/G01 cells. Conclusion Combined treatment of SH3-T79Y and imatinib may inhibit the proliferation of CML cells in vivo and in vitro by decreasing BCR-ABL and CrkL phosphorylation as well as Cyclin-D1 protein.

10.
Journal of the Korean Ophthalmological Society ; : 1321-1326, 2013.
Article in Korean | WPRIM | ID: wpr-93350

ABSTRACT

PURPOSE: To evaluate the clinical usefulness of KCL 990(R) for the treatment of dry eye with meibomian gland dysfunction (MGD). METHODS: Patients (n = 54 eyes, 27 subjects) diagnosed with dry eye with MGD were recruited for a prospective, one-month clinical trial. Patients received a twice-a-day 15-minute treatment using the KCL 990(R). Effectiveness parameters included patient symptom scores using the Ocular Surface Disease Index (OSDI) questionnaires, tear osmolarity measured with TearLab(R) (TearLab Corporation, San Diego, CA, USA), classical tear break-up time (TBUT), and objective TBUT value using an Optical Quality Analysis System (OQAS(R), Visiometrics, Castelldefels, Spain). Data are presented for pre-treatment (baseline) and at 1 week and 1 month post-treatment. An objective TBUT value was estimated in each eye when the optical scattering index (OSI) started to increase consistently, and data were obtained at pretreatment (baseline) and at 1 month post-treatment. RESULTS: The symptom scores on OSDI questionnaires, tear osmolarity, and tear break-up time improved significantly from baseline to one week (p < 0.05). This improvement was maintained with no significant regression at 1 month (p < 0.05). The objective TBUT value decreased significantly at 1 month (p < 0.05). CONCLUSIONS: KCL 990(R) contributed to improve not only signs and symptoms of dry eye with MGD, but also the function of the tear film and ocular surface.


Subject(s)
Humans , Dry Eye Syndromes , Eye , Meibomian Glands , Osmolar Concentration , Prospective Studies , Surveys and Questionnaires , Tears
11.
Article in English | IMSEAR | ID: sea-161558

ABSTRACT

Sand matrix based KCl controlled release fertilizer is made and tested. The parameters of the study are initial fraction of KCl, fractional binder, Fractional inert, Diameter of the pellet and Particle size of the sand. The release of fertilizer from the pellet depended on the compositional parameters of the study. Based on Fick`s second law, a model was developed for the sand matrix fertilizers with napthalene coating. Simulated data from the model was agreeing well with experimental values. The developed equations are as follows:

12.
Journal of Veterinary Science ; : 141-146, 2009.
Article in English | WPRIM | ID: wpr-221143

ABSTRACT

The effect of NaCl plus 3% chitosan on the systolic blood pressure of spontaneously hypertensive rats (SHR) were evaluated and compared with NaCl plus KCl (NaCl, 49.36% + KCl 49.36%) and chitosan or NaCl treatment alone. In SHR, administration of NaCl plus chitosan (44 mM Na/day) for two months significantly decreased the systolic blood pressure greater than of NaCl plus KCl and NaCl alone. NaCl plus chitosan resulted, though not statistically significant, in decreased urinary Na+ excretion and decreased blood urea nitrogen levels. Urinary creatinine of NaCl plus chitosan was slightly decreased compared to 3 treated groups. Serum electrolytes levels, however, remained unchanged. The combination of NaCl and chitosan may be superior to the conventional use of NaCl plus KCl or NaCl alone in the prevention of hypertension. Even though these supplementary diets have demonstrated potential anti-hypertensive effects in the experimental animal model, further research is needed before any recommendations can be made.


Subject(s)
Animals , Male , Rats , Angiotensin I/blood , Angiotensin II/biosynthesis , Blood Pressure/drug effects , Blood Urea Nitrogen , Body Weight/drug effects , Chitosan/administration & dosage , Chlorides/blood , Creatinine/urine , Heart/physiology , Histocytochemistry , Hypertension/prevention & control , Kidney/physiology , Potassium/blood , Potassium Chloride/administration & dosage , Random Allocation , Rats, Inbred SHR , Sodium/blood , Sodium Chloride, Dietary/administration & dosage , Systole/drug effects
13.
Psychiatry Investigation ; : 94-101, 2008.
Article in English | WPRIM | ID: wpr-33387

ABSTRACT

OBJECTIVE: The interaction between MK-801, a model of psychosis and KCl-induced depolarization or electroconvulsive shock (ECS), a therapeutic model of electroconvulsive therapy (ECT), was investigated in SH-SY5Y cells and the rat frontal cortex. METHODS: SH-SY5Y cells were pretreated with 1 microM MK-801 for 15 min, followed by cotreatment with 100 mM KCl for 5 min. MK-801 was reintroduced after the KCl was washed out, and the samples were incubated before harvesting. For the experiments in rats, male Sprague-Dawley rats were treated with MK-801 followed by ECS. Immunoblot analyses of glycogen synthase kinase 3beta (GSK3beta) (Ser9), AKT (Ser473) and extracellular legulated kinase (ERK)1/2 in SH-SY5Y cells and the rat frontal cortex were performed. RESULTS: KCl-induced neuronal depolarization resulted in the transient dephosphorylation of AKT (Ser473) and GSK3beta (Ser9), followed by increased phosphorylation of the enzymes in SH-SY5Y cells. Cotreatment with MK-801 and KCl inhibited the initial dephosphorylation of AKT and GSK3beta produced by KCl-induced neuronal depolarization. Similarly, ECS resulted in the transient dephosphorylation of AKT (Ser473) and GSK3beta (Ser9), whereas cotreatment with MK-801 inhibited the initial dephosphorylation of AKT (Ser473) and GSK3beta (Ser9) produced by ECS in the rat frontal cortex. No significant interaction was observed between MK-801 and KCl in the dephosphorylation of ERK1/2. CONCLUSION: These results suggest that an antagonistic interplay between MK-801 and neuronal depolarization by KCl or ECS is involved the regulation of AKT (Ser473) and GSK3beta (Ser9) phosphorylation.


Subject(s)
Animals , Humans , Male , Rats , Dizocilpine Maleate , Electroconvulsive Therapy , Electroshock , Glycogen Synthase Kinases , Neurons , Phosphorylation , Phosphotransferases , Psychotic Disorders , Rats, Sprague-Dawley
14.
The Korean Journal of Nutrition ; : 500-508, 2007.
Article in Korean | WPRIM | ID: wpr-645358

ABSTRACT

The purpose of this study was to investigate the influence of mixed NaCl-KCl salt on sodium intake and urinary excretion of sodium and potassium. In this study, 3-day food records for pre-experimental diet and 24-hr urine collected for 2-days, 6-day experimental diet food and 24-hr urine were used to evaluate the relationship between Na metabolism. In the experimental diet food, mixed NaCl-KCl salt was added. During the pre-experimental diet period, intakes of Na and K were 178.2 mEq and 56.4 mEq, respectively. The urinary excretion of Na and K in 24-hr were 139.6 mEq, 27.7 mEq, respectively and urinary Na/K ratio was 6.6. During the experimental diet period, intakes of Na and K were 130.2 mEq and 120.4 mEq, respectively. The urinary excretion of Na and K in 24-hr were 100.2 mEq, 37.1 mEq, respectively and urinary Na/K ratio was 2.8. According to this study, it is concluded that mixed NaCl-KCl salt diet decreased the intake of Na, and increased the intake of K.


Subject(s)
Diet , Metabolism , Potassium , Sodium
15.
Journal of Medical Research ; (12)2006.
Article in Chinese | WPRIM | ID: wpr-560465

ABSTRACT

0.05)and could be induced significantly after 12 h (P

16.
Journal of Laboratory Medicine and Quality Assurance ; : 207-211, 2006.
Article in Korean | WPRIM | ID: wpr-98172

ABSTRACT

BACKGROUND: The KCl hypotonic treatment is important for swelling the cells and adequate spreading of chromosomes on the slide. Cytogenetic laboratory usually use 0.075M KCl solution. Sometimes, it is difficult to obtain enough and good quality of metaphase cells, because of inadequate hypotonic treatment. The purpose of this study was to evaluate the mitotic index and band resolution according to the different KCl concentration. METHODS: The group I included blood specimens obtained from 14 newborns (median age 1 day, range 1-8 days) and 4 cord blood. The group II included 16 persons whose median age was 28 years (1-37 years). The blood was cultured in RPMI 1640 medium with fetal calf serum and phytohemagglutinin for 72 hours. Mitosis was arrested by adding colcemid (100 ng/mL). The hypotonic treatment was done by adding different KCl concentration such as 0.075M, 0.068M and 0.057M for 30 minutes at 37 degrees C. The mitotic index was calculated as the number of metaphase cells per total 1,000 cells. The band resolution was evaluated by 2 persons independently. RESULTS: For group I, the mitotic index was not different according to the KCl concentration; 0.075M, 18.8 (5.5~31.5); 0.068M, 22.3 (11~32.5); 0.057M, 20.5 (2.5~29), (P=0.137). The proportion of cells with 400 or more band resolution was significantly higher in specimens treated with 0.068M KCl than those treated with 0.075M KCl; 0.075M, 67.8% (56~92.5); 0.068M, 73.6% (46.1~84.6); 0.057M, 71.6% (63~89.2), (P=0.027). For group II, the results were similar to those of group I. The mitotic index was as follows; 0.075M, 22.3 (5~28); 0.068M, 26 (4~34.5); 0.057M, 21.5 (2.5~36.5), (P=0.568). The proportion of cells with 400 or more band resolution was as follows; 0.075M, 66.6% (42.8~83.3); 0.068M, 69.7% (54.3~87.5); 0.057M, 68.2% (50~78.6) (P=0.04). CONCLUSIONS: For 0.068M or 0.057M KCl treatment, band resolution was improved, while the mitotic index was similar to that of 0.075M KCl. We suggest use of 0.068M or 0.057M KCl hypotonic treatment in addition to 0.075M KCl for chromosome preparation of peripheral blood.


Subject(s)
Humans , Infant, Newborn , Cytogenetics , Demecolcine , Fetal Blood , Metaphase , Mitosis , Mitotic Index
17.
Chinese Journal of Clinical Pharmacology and Therapeutics ; (12)2004.
Article in Chinese | WPRIM | ID: wpr-556902

ABSTRACT

AIM: To observed the effects of BWYJ (a naftopidil ramification) on intracellularlar free Ca~(2+)([Ca~(2+)]_i) in smooth cells (SMCs) in order to further explore its vasodilative mechanisms. METHODS: The [Ca~(2+)]_i was determined with the Fura-2/AM loaded SMCs in aorta of rabbit, and the effects of BWYJ on the elevation induced by NA, and high potassium and 5-HT were observe. RESULTS: In the Fura-2/AM loaded SMCs, BWYJ had no effect on the resting [Ca~(2+)]_i, but it reduced the increase of [Ca~(2+)]_i induced by NA and 5-HT, and there was no influence on the increase of [Ca~(2+)]_i induced by high potassium. CONCLUSION: The vasodilative mechanisms of BWYJ may be related to its inhibitive effects on the Ca~(2+)-influx and Ca~(2+)-release mediated by ?_1- and 5-HT_(2A) receptors. It inhibits the release of intracellular calcium, and the result is it decrease the [Ca~(2+)]_i in SMCs.

18.
Chinese Pharmacological Bulletin ; (12)2003.
Article in Chinese | WPRIM | ID: wpr-566620

ABSTRACT

Aim To investigate the effects of YMⅢ,a derivative of naftopidil, on the vascular contractive activities in rabbit aorta and to explore its vasodilative mechanisms.Methods The isotonic contractions of the thoracic aorta strips from rabbits were recorded, and the effects of YMⅢ on the concentration-response curves of noradrenaline(NA),high potassium and 5-hydroxytryptamine(5-HT)were observed.Intracellular free Ca2+([Ca2+]i)was investigated in the pressence of and the absence of YMⅢ in different conditions.Results YMⅢ(10-8,5?10-8,10-7 mol?L-1)shifted the concentration-response curve of NA with a parallel manner to right, the maximum response was unchanged and the pA2 value was 8.00; YMⅢ (10-5 mol?L-1)also shifted the concentration-response curve induced by high potassium to right but with non-parallel manner,the response was depressed and the pD′2 value was 4.26. However, YMⅢ(10-7,10-6,10-5 mol?L-1)had no statistical influence on the concentration-response curve induced by 5-HT, although it tended to depress the response of the curve at 10-5 mol?L-1.In Ca2+-free medium,YMⅢ (10-8,5?10-8 and 10-7mol?L-1) significantly inhibited the transient contraction induced by NA and the long-lasting one induced by addition of Ca2+ with a concentration-dependent manner.But even at 10-5 mol?L-1,it did not inhibit the contraction induced by caffeine.Conclusions YMⅢ may be ?-adrenergic receptor blocker.Its vasodilative mechanism may be related to:blocking ?-adrenergic receptor on cell membrane resulting in the inhibition on the influx of extracellular Ca2+ and the release of intracellular calcium.

19.
Chinese Pharmacological Bulletin ; (12): 267-271, 2002.
Article in Chinese | WPRIM | ID: wpr-857481

ABSTRACT

AIM: To study the effects of different kinds of chloride channel blockers on KCl and 5-HT-induced contractile responses in cerebrovascular smooth muscle. METHOD: The tension of rabbit basilar artery rings was measured. RESULTS: 1 DIDS, furosemide and NPPB inhibited the responses to KCl and 5-HT in a concentration- dependent manner. The effects of DIDS, furosemide and NPPB on the response to 5-HT were stronger than that to KCl. 2 When SK&F 96365 evoked a maximum inhibitory effect on 5-HT-induced response, subsequent additions of DIDS, furosemide and NPPB could further produced vascular relaxation. CONCLUSION: The chloride channel participates KCl and 5-HT-induced contractile responses in cerebral basilar artery.

20.
Chinese Journal of Clinical Pharmacology and Therapeutics ; (12)2000.
Article in Chinese | WPRIM | ID: wpr-677144

ABSTRACT

Aim The protective effect and mechanism of TPG on PC12 cells in calcium overloading injury models were studied. Methods Two injury models induced by KCl and NMDA were used to assay the action of TPG in cultured PC12 cells. Results The morphological examination revealed that TPG possessed obvious protective effects on PC12 cells in injury models. MTT and LDH measurement indicated that TPG increased the number of live cells and reduced the extent of cell injury significantly. TPG also lessened the concentration of calcium ion in cytoplasm. Conclusion TPG protected rat PC12 cells against two calcium overloading injuries effectively in vitro. Its actions may deal with anti oxidation, inhibition of NO production and blocking of both types of calcium channel.

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