Proceedings of the Western Pharmacology Society最新文献_第2页

Treatment with LA-419 prevents monocrotaline-induced pulmonary hypertension and lung injury in the rat. 用LA-419治疗可预防大鼠单罂粟碱引起的肺动脉高压和肺损伤。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

M Mourelle, M T Martin, F Giménez

引用次数: 0

Relationship among changes in hematocrit, albumin and corticosteroid dose on the disposition of tacrolimus during the first six months following renal transplantation. 肾移植术后前6个月红细胞压积、白蛋白和皮质类固醇剂量变化与他克莫司处置的关系。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

A L Robles-Piedras, S Romano-Moreno, I Fuentes-Noriega, E Mancilla-Urrea, E H González-López, A Domínguez-Ramírez

{"title":"Relationship among changes in hematocrit, albumin and corticosteroid dose on the disposition of tacrolimus during the first six months following renal transplantation.","authors":"A L Robles-Piedras, S Romano-Moreno, I Fuentes-Noriega, E Mancilla-Urrea, E H González-López, A Domínguez-Ramírez","doi":"","DOIUrl":"","url":null,"abstract":"Tacrolimus is a macrolide immunosuppressant that is safe and effective for the prevention of rejection after kidney transplantation. The oral bioavailability of tacrolimus averages 20% to 25%; however, the inter-individual variability in this parameter is large. Because of the poor correlation of dose to blood concentration between patients, the variability in pharmacokinetics and a relatively narrow therapeutic window, therapeutic drug monitoring of tacrolimus trough whole blood concentrations must be a standard practice. The objective of this evaluation was to determine the relationship among changes in hematocrit, albumin, and corticosteroid dosing on the disposition of tacrolimus during 6 months of treatment in renal transplant recipients. Blood samples for the determination of trough tacrolimus concentrations were taken immediately prior to the morning dose, samples were collected according to the request of the attending physician. Clinical and dosage data were reviewed 6 months after transplantation. The analysis was conducted including 11 patients who were analyzed for hematocrit and albumin at the same time they are measured tacrolimus blood levels. The mean age was 25.3 years (range 17 to 41 years) 4 of the patients were female. Levels of tacrolimus, hematocrit and albumin over the first 24 weeks post-transplant were documented and the estimated relative clearance of tacrolimus were calculated. Statistical evaluation of the data indicates poor correlation between relative clearance and both hematocrit and albumin levels and the mean oral steroid dose. This observation is of clinical significance because dose adjustment may be required to maintain blood concentrations within thetherapeutic range in patients in whom hematocrit or albumin concentrations are changing.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pre-transplant mycophenolate mofetil pharmacokinetics in Mexican children. 墨西哥儿童移植前霉酚酸酯的药代动力学。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

M Villa, R González, P García-Roca, A M Hernández, L Ortiz, G Castañeda-Hernández, M Medeiros

{"title":"Pre-transplant mycophenolate mofetil pharmacokinetics in Mexican children.","authors":"M Villa, R González, P García-Roca, A M Hernández, L Ortiz, G Castañeda-Hernández, M Medeiros","doi":"","DOIUrl":"","url":null,"abstract":"Mycophenolate mofetil is an immunosuppressive pro-drug frequently used to prevent renal graft rejection. It is hydrolyzed by esterases to obtain the active drug mycophenolic acid (MPA). There is high inter-patient variation in mycophenolic acid pharmacokinetics. Area under the concentration versus time curve (AUC) is used for therapeutic drug monitoring and recommended levels are 30-60 microg x hr/L. The aim of this study was to determine mycophenolic acid pharmacokinetics in children awaiting renal allograft in order to predict mycophenolate mofetil dose requirements. Children with end-stage renal disease on the waiting list for renal allograft transplantation were invited to participate in the study. A nine-point pharmacokinetic profile was performed. All patients received a single dose (600 mg/m2, subcutaneously) of mycophenolate mofetil at time zero. Mycophenolic acid was measured by HPLC. The AUC0-12h was estimated by the trapezoidal rule. Ten children were included in the study. Mean age was 13.5 +/- 3.5 years. The median AUC0-12h was 20.3 microg x hr/L, median Cmax = 0.7 microg/mL. Two children (20%) had no detectable levels of mycophenolic acid after a single mycophenolate mofetil dose, other two patients had AUC > 60 microg x hr/L. One patient had abdominal pain 1 hr after the mycophenolate mofetil dose. Twenty percent of our patients had AUC0-12h higher than the recommended value after a single mycophenolate mofetil dose, those patients should receive lower mycophenolate mofetil dose since the beginning of the transplant to avoid adverse events, and another 20% of patients had no detectable mycophenolic acid levels after a single mycophenolate mofetil dose. UGT1A9 gene polymorphisms remain to be studied in our patients, since they could explain the differences in bioavailability.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507703","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Calmodulin antagonists inhibit sea urchin sperm hyperpolarization necessary for directed movement toward the egg. 钙调素拮抗剂抑制海胆精子向卵子定向运动所必需的超极化。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

B E Galindo, A Darszon

{"title":"Calmodulin antagonists inhibit sea urchin sperm hyperpolarization necessary for directed movement toward the egg.","authors":"B E Galindo, A Darszon","doi":"","DOIUrl":"","url":null,"abstract":"Speract, a decapeptide from Strongylocentrotus purpuratus sea urchin eggs, transiently stimulates a membrane guanylyl cyclase and activates a K(+)-selective channel that hyperpolarizes the sperm. Membrane potential recordings with fluorescent dyes in sperm flagellar vesicles were used to determine if calmodulin participates in the signal transduction induced by speract. The vesicle hyperpolarization induced by speract was inhibited by the calmodulin antagonists: trifluoperazine, mastoparan; N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide, (W-7); and N-(6-Aminohexyl)-1-naphthalenesulfonamide, (W-5). Since that inhibition occurred at concentrations at which calmodulin action is inhibited by these compounds, the overall findings suggested that calmodulin could be involved in the speract response. The speract response was Ca(2+)-independent however. Ten millimolar EGTA does not inhibit the hyperpolarization and 2 mM BAPTA only partially inhibited the response. High concentrations of calmodulin-dependent kinase II and phosphatase inhibitors did not alter the response of the flagella vesicles to speract. Taken as a whole, these results indicate that the speract-induced hyperpolarization involves the participation of calmodulin in a Ca2+ independent manner.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30506985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Cellular damage markers in the temporal lobe of a patient with Dyke-Davidoff-Masson Syndrome. Dyke-Davidoff-Masson综合征患者颞叶细胞损伤标志物。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

M A Alonso-Vanegas, L Osorio-Rico, Juana Villeda-Hernández

{"title":"Cellular damage markers in the temporal lobe of a patient with Dyke-Davidoff-Masson Syndrome.","authors":"M A Alonso-Vanegas, L Osorio-Rico, Juana Villeda-Hernández","doi":"","DOIUrl":"","url":null,"abstract":"We studied the cellular damage in a patient with Dyke-Davidoff-Masson Syndrome and a history of chronic temporal lobe epilepsy resistant to treatment. The epileptogenic zone was localized to the right temporal lobe, and an extensive surgical removal of the temporal neocortex plus amygdala and hippocampus was performed. The specimens were immediately frozen in liquid nitrogen and stored at -75 degrees C for biochemical studies. Specimens were immersed and fixed in freshly prepared 4% paraformaldehyde for histopathological evaluation. Neurotransmitter levels were highest in the hippocampus compared to the temporal neocortex (T1, T2, and T3). In the amygdala, GABA was found whereas other amino acids were absent. We found marked dislamination in all areas of the cortex, neuronal loss, amylaceous bodies, and neuronal cytomegaly with cytoskeletal disorganization containing dense fibrillar cytoplasmic aggregates, nodular heterotopias, dysplastic and large neurons with high Nissl staining, intermixed with balloon cells with atypical nuclei, often with binucleation, and abundant glassy eosinophilic cytoplasm. Positive immunoreactive cells with nestin, vimentin, and enhanced expression of astrocytes were observed in all brain regions. This patient's syndrome should be considered as a postinfectious/post-stroke event that caused hemiparesis and later recurrent seizures. Higher expression of nestin and vimentin has been observed in proliferative neuronal cells, the expression in astrocytes may mainly reflect an early response of these cells to injury. Nestin may play a role in protecting the brain from injury. It has been proposed that re-expression of embryonic genes by mature cells is associated with morphological plasticity.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507238","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of varying dose and administration of streptozotocin on blood sugar in male CD1 mice. 链脲佐菌素不同剂量及给药对雄性CD1小鼠血糖的影响。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

J Ventura-Sobrevilla, V D Boone-Villa, C N Aguilar, R Román-Ramos, E Vega-Avila, E Campos-Sepúlveda, F Alarcón-Aguilar

{"title":"Effect of varying dose and administration of streptozotocin on blood sugar in male CD1 mice.","authors":"J Ventura-Sobrevilla, V D Boone-Villa, C N Aguilar, R Román-Ramos, E Vega-Avila, E Campos-Sepúlveda, F Alarcón-Aguilar","doi":"","DOIUrl":"","url":null,"abstract":"Streptozotocin (STZ) is used to induce experimental diabetes in rodents. There is however, controversy as to whether STZ induced diabetes models type 1 or 2 diabetes. We show that the grade of STZ-induced hyperglycemia in male CD1 mice is dependent on STZ dose. A single injection of high dose (130 or 150 mg/Kg body weight) or multiple injections (2, 3, 4 or 5) of low dose (40 mg/Kg body weight) STZ was administered intraperitonealy in non-fasted mice. Blood glucose and body weight were measured over 21 days for high dose and 21 and 28 days for low dose administration. On day three, high dose treatment produced hyperglycemia and body weight loss in comparison to mice without STZ, however unstable hyperglycemias and several deaths were observed during treatment. Hyperglycemia and body weight loss were seen with three or more injections of STZ at 21 days, whereas 4 and 5 injections produced severe hyperglycemia but not death. Mild hyperglycemia (250-450 mg/dL) was seen after 28 days following three injections of STZ. Therefore we concluded that a high dose STZ produces severe hyperglycemia in mice similar to a type 1 diabetic, and three successive administrations of STZ induces mild hyperglycemia in mice similar to type 2 diabetics.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507241","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of orlistat on lipid peroxidation, Na+, K+ ATPase, glutathione and serotonin in rat brain. 奥利司他对大鼠脑脂质过氧化、Na+、K+ atp酶、谷胱甘肽和血清素的影响。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

D Calderón Guzmán, E Hernández García, A Juárez Jacobo, L Segura Abarca, G Barragán Mejía, R Rodríguez Pérez, H Juárez Olguín

引用次数: 0

Tio2-dopamine complex implanted unilaterally in the caudate nucleus improves motor activity and behavior function of rats with induced hemiparkinsonism. 尾状核单侧植入tio2 -多巴胺复合物可改善半帕金森大鼠的运动活动和行为功能。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

Patricia Vergara-Aragón, Leonardo Eduardo Domínguez-Marrufo, Patricia Ibarra-Guerrero, Heidi Hernandez-Ramírez, Beatriz Hernández-Téllez, Irma Elena López-Martínez, Ivonne Sánchez-Cervantes, Patricia Santiago-Jacinto, Jorge Alberto García-Macedo, Guadalupe Valverde-Aguilar, Julio Santiago

{"title":"Tio2-dopamine complex implanted unilaterally in the caudate nucleus improves motor activity and behavior function of rats with induced hemiparkinsonism.","authors":"Patricia Vergara-Aragón, Leonardo Eduardo Domínguez-Marrufo, Patricia Ibarra-Guerrero, Heidi Hernandez-Ramírez, Beatriz Hernández-Téllez, Irma Elena López-Martínez, Ivonne Sánchez-Cervantes, Patricia Santiago-Jacinto, Jorge Alberto García-Macedo, Guadalupe Valverde-Aguilar, Julio Santiago","doi":"","DOIUrl":"","url":null,"abstract":"Parkinson's disease (PD) is characterized by malfunction of dopaminergic systems, and the current symptomatic treatment is to replace lost dopamine. For investigating mechanisms of pathogenesis and alternative treatments to compensate lack of dopamine (DA) activity in PD, the 6-hydroxydopamine (6-OHDA)-lesioned rat model of PD has been useful, these animals display apomorphine-induced contralateral rotational behavior, when they are examined after lesion. The purpose of this study was to assess Titania-dopamine (TiO2-DA) complexes implanted on the caudate nucleus for diminishing motor behavior alterations of the 6-OHDA rat model. Rats with 6-OHDA unilateral lesions received TiO2 alone or TiO2-DA implants, and were tested for open field (OF) gross motor crossing and rearing behaviors, and apomorphine-induced rotation (G) behavior. TiO2 complex have no effects on rearing OF and G behaviors, and a significant reducing effect on crossing motor behavior of normal rats compared to control non-treated rats throughout 56 days of observation. Interestingly, TiO2-DA treatment significant recovered motor crossing and rearing behaviors in 6-OHDA-lesioned rats, and diminished the G behaviors during 56 days of examination. Additionally, in the 6-OHDA-lesioned rats TiO2 treatment had a moderate recovering effect only on crossing behavior compared to lesioned non treated rats. Our results suggest that continuous release of dopamine in the caudate nucleus from TiO2-DA complex is capable of reversing gross motor deficits observed in the 6-OHDA-lesioned rat model of PD. Thistype of delivery system of DA represents a promising therapy for PD in humans.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507165","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A role for cyclic nucleotide-gated channels in the capacitation of mammalian sperm. 环核苷酸门控通道在哺乳动物精子获能中的作用。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

A Cisneros-Mejorado, D Sánchez

引用次数: 0

Anticonvulsant drugs, oxidative stress and nitric oxide. 抗惊厥药物，氧化应激和一氧化氮。

Proceedings of the Western Pharmacology Society Pub Date : 2011-01-01

L A Vega Rasgado, G M Ceballos Reyes, M F Vega-Diaz

{"title":"Anticonvulsant drugs, oxidative stress and nitric oxide.","authors":"L A Vega Rasgado, G M Ceballos Reyes, M F Vega-Diaz","doi":"","DOIUrl":"","url":null,"abstract":"Nitric Oxide (NO) is thought to play a fundamental role in the genesis and the spreading of epileptiform hyperactivity, although its function is unclear and controversial. As a free radical, NO may cause oxidative stress, which is emerging as an important mechanism in the etiology of seizure-induced neuronal death. Here we investigated the role of NO in seizure mechanisms through oxidative stress generation by studying the effect of anticonvulsant drugs such as amino oxyacetic acid (AAOA), valproate (VALP), diazepam (DIAZ) and gabapentin (GBPTNA) on oxidative stress in the brain, estimated as free carbonyls by the method of Dalle and Rossi, and by measuring NO by the indirect method based on the Griess reaction. Results show that, except for AAOA and VALP, anticonvulsants did not significantly affect or decreased free carbonyls, but reversed the oxidative stress produced by pentylenetetrazole (PTZ) induced convulsions. Anticonvulsants except AAOA diminished NO levels and with the exception of VALP, counteracted the increase in NO generated by PTZ. Anticonvulsants decreased oxidative stress and NO especially in hippocampus (HI) and cortex (CX), and reversed PTZ effects on both parameters. PTZ diminished NO in HI, which could be explained since PTZ caused an increase on endothelial NO synthase but a decrease in neuronal NOS expression in this brain area. Since the drugs studied are modulating GABA levels, our results suggest that seizures generated by alterations in GABAergic transmission produce oxidative stress caused by NO, which can be reversed by anticonvulsants. The effects described differ among the brain regions studied and the NO synthase isoform affected.","PeriodicalId":20701,"journal":{"name":"Proceedings of the Western Pharmacology Society","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2011-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30507171","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0