The application of percutaneous retrograde pubic screw implantation assisted by hollow pedicle opener in treatment of pubic branch fracture / 中国修复重建外科杂志

Objective: To evaluate the effectiveness of percutaneous retrograde pubic screw implantation assisted by hollow pedicle opener in pubic branch fractures. Methods: The clinical data of 42 patients with pubic branch fractures treated by hollow screw fixation between March 2008 and March 2019 were analyzed retrospectively. According to the operation method, they were divided into the traditional operation group (20 cases in group A, fixed with traditional retrograde pubic screws) and the modified operation group (22 cases in group B, fixed with percutaneous retrograde pubic screws assisted by hollow pedicle opener). There was no significant difference ( P>0.05) between the two groups in terms of gender, age, cause of injury, fracture classification, comorbidity, and time from injury to operation. The operation time, blood loss, incision length, screw length, and complications were recorded and compared between the two groups. The fracture reduction was evaluated according to Matta standard on the next day after operation, and the function was evaluated by Majeed score at 12 months after operation. Results: The operation was successfully completed in both groups. The operation time, blood loss, and incision length of group B were significantly less than those of group A ( P0.05). Conclusion: Percutaneous retrograde pubic screw implantation assisted by hollow pedicle opener is effect for the pubic branch fractures with the advantage of smaller incision, shorter operation time, and less bleeding compared with traditional methods.

Association between Alcoholism Family History and Alcohol Screening Scores among Alcohol-dependent Patients

OBJECTIVE: Several tests can be used to screen for alcohol dependence (AD), a prevalent disease with a heterogeneous etiology. As some patients with AD have a strong familial tendency in this regard, a family history of alcohol use disorders can affect the outcomes of screening tests and diagnostic evaluations for AD. In this study, we evaluated associations between a family history of alcohol use disorders and evaluations using the Cut down, Annoyed, Guilty, Eye-opener (CAGE) test, Alcohol Use Disorder Identification Test (AUDIT), and Diagnostic and Statistical Manual of Mental Disorders-fourth edition (DSM-IV) diagnostic criteria among patients with AD. METHODS: We recruited 487 male patients with AD from eight hospitals in Korea. Patients were evaluated using the CAGE, AUDIT, and DSM-IV diagnostic criteria. Patients with and without family histories were compared in terms of these assessment tools. RESULTS: Drinking initiation, uncontrollable drinking, and problem drinking occurred earlier and CAGE "annoyed" scores were higher in patients with a family history. Alcohol problems before the age of 25 years, frequency of spontaneous or compulsive alcohol-seeking behavior, and frequencies of psychological dependence and guilt related to alcohol use were also higher. CONCLUSION: Earlier drinking problems, higher scores on specific items of the CAGE, and AUDIT, and meeting more diagnostic criteria indicate more dependent, harmful drinking by patients with AD who have a family history of this condition. Clinicians should consider patients' family history of alcohol use disorders when screening for AD to identify the correct diagnosis and develop appropriate treatment plans for these patients.

Effects of iptakalim on the functions of endothelin system in human pulmonary artery endothelial cells / 中国药理学通报

Aim To investigate the effects of iptakalim(IPT),a novel K_(ATP) opener,on the functions of endothelin system in human pulmonary artery endothelial cells.Methods Primary cultured human pulmonary artery endothelial cells were incubated with different concentrations iptakalim for 24 h.The levels of ET-1 in medium were observed by radioimmunoassay.Reverse transcription polymerase chain reaction(RT-PCR)was performed to analyze the expression of ET-1 and ECE.Results When endothelial cells were incubated with IPT at concentrations above 10 μmol·L~(-1),the levels of ET-1 release in medium and the levels of ET-1 mRNA were significantly inhibited.When endothelial cells were incubated with IPT at concentrations above 1 μmol·L~(-1),the levels of ECE mRNA were significantly inhibited.Conclusions IPT can inhibit the expression of ET-1 and ECE mRNA from human pulmonary artery endothelial cells, thus it inhibits the secretion of ET-1 from endothelial cells. Iptakalim may serve as a promising candidate drug to treat pulmonary hypertension.

Protective effect of hyperpolarized preservation solution combining sodium-hydrogen exchange inhibitor and potassium channel opener on donor heart / 第二军医大学学报

Objective: To study whether sodium-hydrogen exchange inhibitor(NHEI) can enhance the protective effect of hyperpolarized preservation solution containing potassium channel opener (PCO), and the effect was compared with that of Celsior solution. Methods: After equilibrated on a crystalloid-perfused Langendorff model for 30 min, rabbit hearts were divided into four groups: (1) Cel group: receiving another 30 min of equilibration, 8 h cold storage with Celsior solution and 1 h reperfusion; (2) Pin group: arrested and stored with pinacidil (a type of PCO) hyperpolarizing cardioplegia; (3) Cel+Car group: receiving the same treatment as Cel group except that 10 μmol/L cariporide (a type of NHEI) was administered during the second equilibration period and reperfusion; and (4) Pin+Car group: receiving cariporide treatment and hyperpolarized arrest and storage. Results: Recovery rate of systolic function in the Pin+Car group was significantly higher than that in the Pin group ([87.4±11.9]% vs [69.0±7.2]%, P0.05). No significant differences were found in any parameters between Cel group and Cel+Car group. There were no differences in coronary flow among all groups. Conclusion: NHEI can greatly enhance the protective effect of PCO hperpolarized preservation solution on the donor heart, and the combination of them has a comparable protective effect to Celsior solution.

Qualidade de semeadura na implantação da cultura do milho por três semeadoras-adubadoras de plantio direto / Sowing quality in implantation of maize crop by three no-tillage seeder-fertilizers

Com o objetivo de se avaliar três semeadoras para plantio direto de milho, montou-se um experimento em área do Departamento de Engenharia da UFLA, sob Latossolo Vermelho Distroférrico argiloso (LVdf), utilizando-se as seguintes semeadoras: S1 - Semeato SHM 11/13; S2 e S3 - John Deere RT 907, com diferentes sistemas de abertura de sulcos para deposição de adubo, deslocando-se a três velocidades (5,0; 6,5; 8,0 km h-1). As variáveis quantificadas foram: estande de plantas m-1, índice de velocidade de emergência de plantas; uniformidade de semeadura (duplos, aceitáveis, falhas), profundidade de semeadura, danos mecânicos e germinação das sementes. Adotou-se o delineamento estatístico de blocos casualizados, com os tratamentos dispostos em parcelas subdivididas. A uniformidade de semeadura para as semeadoras S1 e S3 (sistemas análogos para corte de palha e abertura dos sulcos de fertilizantes) foi semelhante, não sendo observadas diferenças significativas entre elas; o sistema pneumático não apresentou vantagem econômica (considerando o alto investimento) em relação ao sistema mecânico de discos horizontais, na implantação da cultura do milho; o aumento da velocidade reduziu a uniformidade de semeadura (duplos, aceitáveis e falhas) e aumentou a danificação mecânica das sementes.

An experiment was carried out at UFLA Agricultural Department, in order to technically evaluate three no-tillage seeder-fertilizers on clayey typical Dystroferric Red Latosol (LVdf). Seeders S1 - Semeato SHM 11/13, S2 and S3 - John Deere RT 907 with different furrow opening systems were utilized at three different speeds (5,0; 6,5; 8,0 km-1). Quantified variables were: stand plants m-1; plant emergence speed; sowing uniformity (double, acceptable, failure); sowing depth; mechanical damages, and seed germination. A randomized block design in shared fragments was employed. Sowing uniformity to S1 and S2 (analogous systems to straw cutting and fertilizer opening) showed no significant differences. Pneumatic system showed no economical benefits, considering the high investment, when compared to the mechanical system with horizontal disks in corn culture. Speed increase reduced sowing uniformity (double, acceptable, failure), besides increasing mechanical seed damage.

The Effect of Nicorandil on the Pharmacodynamics of Rocuronium / 대한마취과학회지

BACKGROUND: Some investigators have shown that nicorandil, a K(ATP) channel opener, depresses the neuromuscular transmission contraction of the skeletal muscle. However, others have reported that it improves the recovery of vecuronium relaxation and the myotonic activity of muscle. This study investigated the effect of nicorandil on rocuronium relaxation. METHODS: Hemidiaphragm-phrenic nerve preparations were obtained from male Sprague-Dawley rats (150-250 g). The preparations were bathed in Krebs' solution containing in (mM): NaCl 118, KCl 5, CaCl2 2.5, NaHCO3 30, KH2PO4 1, MgCl2 1 and glucose 11. The preparations were, then maintained at 32 degrees C and aerated with a mixture of 95% O2 and 5% CO2. Isometric forces that were generated in response to 0.1 Hz, and, 50 Hz for 1.9 seconds with supramaximal electrical stimulation (0.2 msec, rectangular) to the phrenic nerve were measured using a force transducer. The single twitch tension (ST) and peak tetanic tension (PTT) were calculated as % inhibition of the control, and the tetanic fade (TF), as % increase in the PTT. Each preparation was exposed to one of the 6 nicorandil concentrations (0.0, 0.625, 1.25, 2.5, 5, 10 micrometer), and the adequate volume of the rocuronium solution was cumulatively added to the tissue bath for a desired rocuronium concentration until there was an 80-90% decrease in the ST. The effect of rocuronium at each concentration was allowed to reach a steady state before the tension parameters were measured. The EC5, EC25, EC50, EC75, and EC95 of rocuronium for the ST, PTT and TF were calculated using a probit model. The differences between the EC50 of rocuronium according to the nicorandil concentrations were tested using a t-test and a Bonferroni's correction. RESULTS: 1.25 and 2.5 micrometer nicorandil shifted the cumulative concentration-response curves for the TF of rocuronium to the right. 5 and 10 micrometer nicorandil shifted the cumulative concentration-response curves for the ST of rocuronium to the left. CONCLUSIONS: Lower concentration of nicorandil may help maintain the tetanic contraction during rocuronium relaxation.

Effects of K+ Channel Opener WAY120491 on Renal Function in Rabbits / 대한신장학회잡지

BACKGROUND: K+ channel opener has been considered as a vasorelaxing agent working through hyperpolarization of vascular smooth muscle cells. Renal tubules-proximal, thick ascending limb of Henle and cortical collecting duct-are the site of the diversity of the K+ channel. ATP-sensitive K+ channel has been observed in the apical membranes of the thick ascending limb of Henle and collecting duct, and basolateral membrane of the proximal tubule. It was also shown that K+ channel opener increased renal hemodynamics and elicited diuretic and natriuretic effects. METHODS: To clarify the renal effects of WAY120491, a K+ channel opener, experiments were performed in unanesthetized normotensive and renal hypertensive rabbits allowing unilateral renal arterial infusion of agent. RESULTS: Intrarenal arterial infusion (0.13, 0.32 and 0.64 microgram/kg/min) of WAY120491 increaased CPAH, CCr, urine volume, UNaV, UKV and CH2O. Renal hemodynamic effects and increments of urine volume and free water clearance were completely blocked by glibenclamide (8.2 g/kg/min), while increments of UNaV and FENa were not significantly affected. Renal hemodynamic and tubular effects of WAY120491 were not significantly different in two-kidney one clip Goldblatt hypertensive rabbits from sham-operated rabbits. CONCLUSIONS: These results suggest that WAY120491 elicits renal effects through ATP-sensitive K+ channel in the renal vasculatures and renal tubules and the renal effects of WAT120491 may not be altered in the hypertension.

Effects of Pinacidil, Tetrathylammonium and Glibenclamide on Hypoxic Vasoconstriction in Isolated Perfused Rabbit Lungs / 대한마취과학회지

BACKGROUND: This study investigated the effects of the K+ channel opener, pinacidil on hypoxic pulmonary vasoconstriction in isolated perfused rabbit lungs. In order to evaluate the vasodilatation mechanism of K+ channel opener, we also studied the effects of two K+ channel blocker, tetraethylammonium (TEA), a Ca2+ activated K+ channel blocker and glibenclamide (GLB), an ATP-sensitive K+ channel blocker. METHODS: Isolated lungs from white rabbits were ventilated with a normoxic gas (21%O2-5%CO2-74%N2) and a hypoxic gas (3%O2- 5%CO2-92%N2) alternatively, and then perfused with blood-containing perfusate solution. After a hypoxic pressor response (HPR) had been obtained, various drugs were added to the perfusate reservoir to achieve the predetermined circulating concentration, and the influences of the drugs on HPR were then tested. RESULTS: Pinacidil (0.3-6.0 mcM) produced a dose-dependent pulmonary vasodilation on hypoxic ventilation challenge. TEA (1 mM) caused pulmonary vasoconstriction in normoxic ventilation and potentiated a hypoxic pressor response. When the hypoxic pressor response was potentiated by TEA, pinacidil (1.0, 3.0 mcM) reduced the contraction, but GLB did not cause pulmonary vasoconstriction under normoxic ventilation, potentiate a hypoxic pressor response. CONCLUSIONS: Piacidil is capable of opposing the pulmonary responses of acute hypoxia. Moreover the effects of TEA and GLB suggest that HPV might be mediated through Ca2+ activated K+ channels, not through ATP-sensitive K+ channels.

Effect of ATP sensitive potassium channel opener on neuronal apoptosis and the expression of caspase-8 in rats following cerebral ischemia-reperfusion / 临床神经病学杂志

Objective To study the effect of ATP sensitive potassium channel(KATP)opener on neuronal apoptosis and the expression of caspase-8 mRNA and protein in rats following cerebral ischemia-reperfusion.Methods 200 male Wistar rats were randomly divided into sham-operated group,control group,KATP opener precondition group(KATP opener group)and KATP opener and blocker precondition group(KATP blocker group).The middle cerebral artery ischemia-reperfusion models were established by using the intraluminal suture occlusion method.Neuronal apoptosis were detected by TUNEL staining,the expression of caspase-8 mRNA and protein were detected by immunohistochemical staining and RT-PCR methods.Results(1)The numbers of apoptotic cells in KATP opener group at 12 h,24 h,48 h,72 h after cerebral ischemia-reperfusion were significantly less than those in control group and KATP blocker group(P

Effects of Pinacidil, a Potassium-Channel Opener, on Biodistribution of Thallium-201 in Tumor-Bearing Mice / 대한핵의학회잡지

PURPOSE: Thallium behaves similarly to potassium in vivo. Potassium channel opener (K-opener) opens ATP-sensitive K+/-channel located at cell membrane, resulting in potassium efflux from cytosol. We have previously reported that K-opener can alter biokinetics of Tl-201 in cultured cells and in vivo. Malignant tumor cells have high Na-K ATPase activity due to increased metabolic activities and dedifferentiation, and differential delineation of malignant tumor can be possible with Tl-201 imaging. K-opener may affect tumoral uptake of Tl-201 in vivo. To investigate the effects of pinacidil (one of the potent K-openers) on the localization of the tumor with Tl-201 chloride, we evaluated the changes in biodistribution of Tl-201 with pinacidil treatment in tumor-bearing mice. MATERAL AND METHODS: Balb/c mice received subcutaneous implantation of murine breast cancer cells in the thigh and were used for biodistribution study 3 weeks later. 100 microgram of pinacidil dissolved in 200 microliter DMSO/PBS solution was injected intravenously via tail vein at 10 min after 185 KBq (5 microcurie) Tl-201 injection. Percentage organ uptake and whole body retention ratio of Tl-201 were measured at various periods after injection, and values were compared between control and pinacidil-treated mice. RESULTS: Pinacidil treatment resulted in mild decrease in blood levels of Tl-201, but renal uptakes were markedly decreased at 30-min, 1- and 2-hour, compared to control group. Hepatic, intestinal and muscular uptake were not different. Absolute percentage uptake and tumor to blood ratios of Tl-201 were lower in pinacidil treated mice than in the control group at all time points measured. Whole body retention ratio of Tl-201 was lower in pinacidil treated mice (58+/-4%), than in the control group (67+/-3%) at 24 hours after with injection of 100 microgram pinacidil. CONCLUSION: K-opener did not enhance, but rather decreased absolute tumoral uptake and tumor-to-blood ratios of Tl-201. Decreased whole body retention ratio and renal uptake were observed with pinacidil treatment in tumor-bearing mice.

Effects of new ATP-sensitive potassium channel pener iptakalim on Parkinsonian symptoms induced by haloperidol in rats / 中国临床药理学与治疗学

AIM : To investigate the effects of the new K ATP channel opener, iptakalim (Ipt), on the Parkinsonian symptoms induced by haloperidol in rats. METHODS : Using L -DOPA as the positive drug, the influences of Ipt on latency time, walking time, rearing and grooming of the parkinsonian-like rats induced by haloperidol were observed. RESULTS : Ipt ameliorated hypolocomotion and assuaged catalepsy induced by haloperidol in rats. Moreover, the effects of Ipt ( 0.5 mg?kg -1) were better than those of L -DOPA (100 mg?kg -1). CONCLUSION : Opening of K ATP channels may play a key role in improving Parkinsonian symptoms induced by haloperidol in rats.

Pharmacological evidence that cromakalim inhibits Ca2+ release from intracellular stores in porcine coronary artery

In the present study, it was aimed to further identify the intracellular action mechanism of cromakalim and levcromakaliin in the porcine coronary artery. In intact porcine coronary arterial strips loaded with fura-2/AM, acetylcholine caused an increase in intracellular free Ca2+ ((Ca2+)-i) in association with a contraction in a concentration-dependent manner. Cromakalim (1 micrometer) caused a reduction in acetylcholine-induced increased (Ca2+)-i not only in the normal physiological salt solution (PSS) but also in Ca2+ -free PSS (containing 1mM EGTA). In the skinned strips prepared by exposure of tissue to 20 micrometer beta-escin, inositol 1,4,5-trisphosphate (IP-3) evoked an increase in (Ca2+)-i but it was without effect on the intact strips. The IP-3-induced increase in (Ca2+)-i was inhibited by cromakalim by 78% and levcromakalim by 59% (1 micrometer, each). Pretreatment with glibenclamide (a blocker of ATP-sensitive K+ channels, 10 micrometer and apamin (a blocker of small conductance Ca2+/-activated K+ channels, 1 micrometer strongly blocked the effect of cromakalim and levcromakalim. However, charybdotoxin (a blocker of large conductance Ca2+ -activated K+ channels, 1-micrometer) was without effect. In addition, cromakalim inhibited the GTP-gamma-S (100 micrometer, nonhydrolysable analogue of GTP)-induced increase in (Ca2+)-i. Based on these results, it is suggested that cromakalim and levcromakalim exert a potent vasorelaxation, in part, by acting on the K+ channels of the intracellular sites (e.g., sarcoplasmic reticulum membrane), thereby, resulting in decrease in release of Ca2+ from the intracellular storage site.

Activation of the Cardiac ATP-Sensitive K+Channel by KR-30816,Newly Synthesized Potassium Channel Opener

BACKGROUND: The effects of a newly synthesized potassium channel opener, KR-30816((-)(nitro-2-hydroxymethyl-2-methy-2H-1-benzopyran-4-y1)pyridine oxide) on the action potential of papillary muscles of guinea pigs and the ATP-sensitive potassium channel current(IKATP) of single ventricular muscle cells of rats were examined to make clear its action mechanism of the KATPchannel. METHODS: We used the conventional microelectrode and the excised inside-out patch configuration. RESULTS: KR-30816 caused a shortening of the action potential duration in dose-dependent manner, which was inhibited by glibenclamide(3microM). Before run-down of the K+channel, KR-30816 activated the cardiac ATP-sensitive K+ channel only in the presence of ATP and shifted the dose-response relation curve between [ATP]i and the channel activity to the right in parallel. After run-down of the KATP channel, KR-30816 did not after the channel opening either in the absence or in the presence of UDP. CONCLUSION: These results suggest that KR-30816 antagonizes the inhibitory effect of ATP on the KATPchannel in a competitive manner, thereby enhancing the channel openings.