Naphyrone, also known as NRG-1, is a novel psychoactive substance (NPS), a cathinone with stimulatory properties available on the grey/illicit drug market for almost a decade. It is structurally related to infamously known powerful stimulants with the pyrovalerone structure, such as alpha-pyrrolidinovalerophenone (α-PVP) or methylenedioxypyrovalerone (MDPV) that are labeled as a cheap replacement for cocaine and other stimulants. Despite the known addictive potential of α-PVP and MDPV, there are no studies directly evaluating naphyrone's addictive potential e.g., in conditioned place preference (CPP) test or using self-administration. Therefore, our study was designed to evaluate the addictive potential in a CPP test in male Wistar rats and compare its effect to another powerful stimulant with a high addictive potential - methamphetamine. Naphyrone increased time spent in the drug-paired compartment with 5 and 20 mg/kg s.c. being significant and 10 mg/kg s.c. reaching the threshold (p = 0.07); the effect was comparable to that of methamphetamine 1.5 mg/kg s.c. The lowest dose, naphyrone 1 mg/kg s.c., had no effect on CPP. Interestingly, no dose response effect was detected. Based on these data, we are able to conclude that naphyrone has an addictive potential and may possess a significant risk to users.

• Klíčová slova
• Addictive potential, CPP, Conditioned place preference test, Naphyrone, Novel psychoactive substances,
• MeSH
• alkaloidy farmakologie   MeSH
• chování zvířat účinky léků   MeSH
• klasické podmiňování účinky léků   MeSH
• krysa rodu Rattus MeSH
• methamfetamin aplikace a dávkování   farmakologie   MeSH
• modely nemocí na zvířatech MeSH
• pentanony aplikace a dávkování   farmakologie   MeSH
• poruchy spojené s užíváním psychoaktivních látek * MeSH
• potkani Wistar MeSH
• pyrrolidiny aplikace a dávkování   farmakologie   MeSH
• stimulanty centrálního nervového systému aplikace a dávkování   farmakologie   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• 1-naphthalen-2-yl-2-pyrrolidin-1-ylpentan-1-one MeSH Prohlížeč
• alkaloidy MeSH
• cathinone MeSH Prohlížeč
• methamfetamin MeSH
• pentanony MeSH
• pyrrolidiny MeSH
• stimulanty centrálního nervového systému MeSH

PURPOSE: Trifluridine/tipiracil (FTD/TPI) is approved for advanced colorectal and gastric/gastroesophageal cancer; however, data in patients with renal impairment (RI) are limited. This phase I study evaluated FTD/TPI in patients with advanced solid tumors and varying degrees of RI to develop dosing guidance. METHODS: Patients were enrolled into normal renal function (CrCl ≥ 90 mL/min), mild RI (CrCl 60-89 mL/min), or moderate RI (CrCl 30-59 mL/min) cohorts and administered the recommended FTD/TPI dose (35 mg/m2 twice daily, days 1-5 and 8-12; 28-day cycle). Based on interim pharmacokinetics/safety data, patients with severe RI (CrCl 15-29 mL/min) were enrolled and received FTD/TPI 20 mg/m2 twice daily. RESULTS: Forty-three patients (normal renal function [n = 12]; mild RI [n = 12]; moderate RI [n = 11]; severe RI [n = 8]) were enrolled and treated. At steady state, compared to values in patients with normal renal function, FTD area under the curve (AUC) was not significantly different in patients with RI, but TPI AUC was significantly higher and increased with RI severity. FTD/TPI safety profile was consistent with prior experience, but grade ≥ 3 adverse events (AEs) were more frequent in the RI cohorts (83.3% [mild], 90.9% [moderate], 75.0% [severe], and normal [50.0%]). Hematologic AEs (anemia and neutropenia) were more frequent with RI. Overall, seven patients discontinued because of unrelated, nonhematologic AEs. CONCLUSION: FTD/TPI is safe and tolerable at the recommended 35 mg/m2 dose in patients with mild/moderate RI and at the reduced 20 mg/m2 dose in patients with severe RI. TRIAL REGISTRATION: NCT02301117, registration date: November 21, 2014.

• Klíčová slova
• Pharmacokinetics, Renal impairment, Safety, TAS-102, Trifluridine/tipiracil,
• MeSH
• anemie chemicky indukované   epidemiologie   MeSH
• dospělí MeSH
• fixní kombinace léků MeSH
• kohortové studie MeSH
• lidé středního věku MeSH
• lidé MeSH
• nádory farmakoterapie   MeSH
• nemoci ledvin patofyziologie   MeSH
• neutropenie chemicky indukované   epidemiologie   MeSH
• plocha pod křivkou MeSH
• protokoly antitumorózní kombinované chemoterapie aplikace a dávkování   škodlivé účinky   farmakokinetika   MeSH
• pyrrolidiny aplikace a dávkování   škodlivé účinky   farmakokinetika   MeSH
• senioři nad 80 let MeSH
• senioři MeSH
• stupeň závažnosti nemoci MeSH
• thymin aplikace a dávkování   škodlivé účinky   farmakokinetika   MeSH
• trifluridin aplikace a dávkování   škodlivé účinky   farmakokinetika   MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři nad 80 let MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• klinické zkoušky, fáze I MeSH
• práce podpořená grantem MeSH
• Názvy látek
• fixní kombinace léků MeSH
• pyrrolidiny MeSH
• thymin MeSH
• trifluridin MeSH
• trifluridine tipiracil drug combination MeSH Prohlížeč

The role of opioid kappa1 and kappa2 receptors in reperfusion cardiac injury was studied. Male Wistar rats were subjected to a 45-min coronary artery occlusion followed by a 120-min reperfusion. Opioid kappa receptor agonists were administered intravenously 5 min before the onset of reperfusion, while opioid receptor antagonists were given 10 min before reperfusion. The average value of the infarct size/area at risk (IS/AAR) ratio was 43 - 48% in untreated rats. Administration of the opioid kappa1 receptor agonist (-)-U-50,488 (1 mg/kg) limited the IS/AAR ratio by 42%. Administration of the opioid kappa receptor agonist ICI 199,441 (0.1 mg/kg) limited the IS/AAR ratio by 41%. The non-selective opioid kappa receptor agonist (+)-U-50,488 (1 mg/kg) with low affinity for opioid kappa receptor, the peripherally acting opioid kappa2 receptor agonist ICI 204,448 (4 mg/kg) and the selective opioid ?2 receptor agonist GR89696 (0.1 mg/kg) had no effect on the IS/AAR ratio. Pretreatment with naltrexone, the peripherally acting opioid receptor antagonist naloxone methiodide, or the selective opioid kappa2 receptor antagonist nor-binaltorphimine completely abolished the infarct-reducing effect of (-)-U-50,488 and ICI 199,441. Pretreatment with the selective opioid ? receptor antagonist TIPP[psi] and the selective opioid µ receptor antagonist CTAP did not alter the infarct reducing effect of (-)-U-50,488 and ICI 199,441. Our study is the first to demonstrate the following: (a) the activation of opioid kappa2 receptor has no effect on cardiac tolerance to reperfusion; (b) peripheral opioid kappa1 receptor stimulation prevents reperfusion cardiac injury; (c) ICI 199,441 administration resulted in an infarct-reducing effect at reperfusion; (e) bradycardia induced by opioid kappa receptor antagonists is not dependent on the occupancy of opioid kappa receptor.

• MeSH
• 3,4-dichlor-N-methyl-N-(2-(1-pyrrolidinyl)-cyklohexyl)-benzenacetamid, (trans)-isomer aplikace a dávkování   toxicita   MeSH
• infarkt myokardu metabolismus   patologie   prevence a kontrola   MeSH
• intravenózní podání MeSH
• kardiomyocyty účinky léků   metabolismus   patologie   MeSH
• krysa rodu Rattus MeSH
• modely nemocí na zvířatech MeSH
• narkotika - antagonisté aplikace a dávkování   MeSH
• opioidní analgetika aplikace a dávkování   toxicita   MeSH
• piperaziny aplikace a dávkování   MeSH
• potkani Wistar MeSH
• pyrrolidiny aplikace a dávkování   toxicita   MeSH
• receptory opiátové kappa agonisté   metabolismus   MeSH
• reperfuzní poškození myokardu metabolismus   patologie   prevence a kontrola   MeSH
• signální transdukce MeSH
• srdeční arytmie chemicky indukované   patofyziologie   MeSH
• srdeční frekvence účinky léků   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Názvy látek
• 3,4-dichlor-N-methyl-N-(2-(1-pyrrolidinyl)-cyklohexyl)-benzenacetamid, (trans)-isomer MeSH
• GR 89696 MeSH Prohlížeč
• ICI 199441 MeSH Prohlížeč
• kappa(1) opioid receptor MeSH Prohlížeč
• kappa(2) opioid receptor MeSH Prohlížeč
• narkotika - antagonisté MeSH
• opioidní analgetika MeSH
• piperaziny MeSH
• pyrrolidiny MeSH
• receptory opiátové kappa MeSH

BACKGROUND & AIMS: Eight-week glecaprevir/pibrentasvir leads to high rates of sustained virological response at post-treatment week 12 (SVR12) across HCV genotypes (GT) 1-6 in treatment-naïve patients without cirrhosis. We evaluated glecaprevir/pibrentasvir once daily for 8 weeks in treatment-naïve patients with compensated cirrhosis. METHODS: EXPEDITION-8 was a single-arm, multicenter, phase IIIb trial. The primary and key secondary efficacy analyses were to compare the lower bound of the 95% CI of the SVR12 rate in i) patients with GT1,2,4-6 in the per protocol (PP) population, ii) patients with GT1,2,4-6 in the intention-to-treat (ITT) population, iii) patients with GT1-6 in the PP population, and iv) patients with GT1-6 in the ITT population, to pre-defined efficacy thresholds based on historical SVR12 rates for 12 weeks of glecaprevir/pibrentasvir in the same populations. Safety was also assessed. RESULTS: A total of 343 patients were enrolled. Most patients were male (63%), white (83%), and had GT1 (67%). The SVR12 rate in patients with GT1-6 was 99.7% (n/N = 334/335; 95%CI 98.3-99.9) in the PP population and 97.7% (n/N = 335/343; 95% CI 96.1-99.3) in the ITT population. All primary and key secondary efficacy analyses were achieved. One patient (GT3a) experienced relapse (0.3%) at post-treatment week 4. Common adverse events (≥5%) were fatigue (9%), pruritus (8%), headache (8%), and nausea (6%). Serious adverse events (none related) occurred in 2% of patients. No adverse event led to study drug discontinuation. Clinically significant laboratory abnormalities were infrequent. CONCLUSIONS: Eight-week glecaprevir/pibrentasvir was well tolerated and led to a similarly high SVR12 rate as the 12-week regimen in treatment-naïve patients with chronic HCV GT1-6 infection and compensated cirrhosis. TRIAL REGISTRATION: ClinicalTrials.gov, NCT03089944. LAY SUMMARY: This study was the first to evaluate an 8-week direct-acting antiviral (DAA) regimen active against all major types of hepatitis C virus (HCV) in untreated patients with compensated cirrhosis. High virological cure rates were achieved with glecaprevir/pibrentasvir across HCV genotypes 1-6, and these high cure rates did not depend on any patient or viral characteristics present before treatment. This may simplify care and allow non-specialist healthcare professionals to treat these patients, contributing to global efforts to eliminate HCV.

• Klíčová slova
• Chronic HCV infection, Compensated cirrhosis, Direct-acting antiviral, Glecaprevir/pibrentasvir, HCV elimination, Hepatitis C virus, Pangenotypic, Short duration,
• MeSH
• antivirové látky aplikace a dávkování   škodlivé účinky   MeSH
• benzimidazoly aplikace a dávkování   škodlivé účinky   MeSH
• chinoxaliny aplikace a dávkování   škodlivé účinky   MeSH
• chronická hepatitida C krev   komplikace   farmakoterapie   virologie   MeSH
• cyklopropany aplikace a dávkování   škodlivé účinky   MeSH
• fixní kombinace léků MeSH
• genotyp * MeSH
• Hepacivirus enzymologie   genetika   MeSH
• jaterní cirhóza komplikace   farmakoterapie   MeSH
• kyseliny aminoisomáselné aplikace a dávkování   škodlivé účinky   MeSH
• leucin aplikace a dávkování   škodlivé účinky   analogy a deriváty   MeSH
• lidé středního věku MeSH
• lidé MeSH
• makrocyklické laktamy aplikace a dávkování   škodlivé účinky   MeSH
• polymorfismus genetický MeSH
• prolin aplikace a dávkování   škodlivé účinky   analogy a deriváty   MeSH
• pyrrolidiny aplikace a dávkování   škodlivé účinky   MeSH
• RNA virová krev   genetika   MeSH
• senioři MeSH
• setrvalá virologická odpověď MeSH
• sulfonamidy aplikace a dávkování   škodlivé účinky   MeSH
• virové nestrukturální proteiny genetika   MeSH
• Check Tag
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• klinické zkoušky, fáze III MeSH
• multicentrická studie MeSH
• práce podpořená grantem MeSH
• Názvy látek
• antivirové látky MeSH
• benzimidazoly MeSH
• chinoxaliny MeSH
• cyklopropany MeSH
• fixní kombinace léků MeSH
• glecaprevir MeSH Prohlížeč
• kyseliny aminoisomáselné MeSH
• leucin MeSH
• makrocyklické laktamy MeSH
• NS-5 protein, hepatitis C virus MeSH Prohlížeč
• NS3 protein, hepatitis C virus MeSH Prohlížeč
• pibrentasvir MeSH Prohlížeč
• prolin MeSH
• pyrrolidiny MeSH
• RNA virová MeSH
• sulfonamidy MeSH
• virové nestrukturální proteiny MeSH

BACKGROUND: Cystic fibrosis is caused by mutations in the gene encoding the cystic fibrosis transmembrane conductance regulator (CFTR) protein, and nearly 90% of patients have at least one copy of the Phe508del CFTR mutation. In a phase 2 trial involving patients who were heterozygous for the Phe508del CFTR mutation and a minimal-function mutation (Phe508del-minimal function genotype), the next-generation CFTR corrector elexacaftor, in combination with tezacaftor and ivacaftor, improved Phe508del CFTR function and clinical outcomes. METHODS: We conducted a phase 3, randomized, double-blind, placebo-controlled trial to confirm the efficacy and safety of elexacaftor-tezacaftor-ivacaftor in patients 12 years of age or older with cystic fibrosis with Phe508del-minimal function genotypes. Patients were randomly assigned to receive elexacaftor-tezacaftor-ivacaftor or placebo for 24 weeks. The primary end point was absolute change from baseline in percentage of predicted forced expiratory volume in 1 second (FEV1) at week 4. RESULTS: A total of 403 patients underwent randomization and received at least one dose of active treatment or placebo. Elexacaftor-tezacaftor-ivacaftor, relative to placebo, resulted in a percentage of predicted FEV1 that was 13.8 points higher at 4 weeks and 14.3 points higher through 24 weeks, a rate of pulmonary exacerbations that was 63% lower, a respiratory domain score on the Cystic Fibrosis Questionnaire-Revised (range, 0 to 100, with higher scores indicating a higher patient-reported quality of life with regard to respiratory symptoms; minimum clinically important difference, 4 points) that was 20.2 points higher, and a sweat chloride concentration that was 41.8 mmol per liter lower (P<0.001 for all comparisons). Elexacaftor-tezacaftor-ivacaftor was generally safe and had an acceptable side-effect profile. Most patients had adverse events that were mild or moderate. Adverse events leading to discontinuation of the trial regimen occurred in 1% of the patients in the elexacaftor-tezacaftor-ivacaftor group. CONCLUSIONS: Elexacaftor-tezacaftor-ivacaftor was efficacious in patients with cystic fibrosis with Phe508del-minimal function genotypes, in whom previous CFTR modulator regimens were ineffective. (Funded by Vertex Pharmaceuticals; VX17-445-102 ClinicalTrials.gov number, NCT03525444.).

• MeSH
• aktivátory chloridových kanálů aplikace a dávkování   škodlivé účinky   MeSH
• aminofenoly aplikace a dávkování   škodlivé účinky   MeSH
• benzodioxoly aplikace a dávkování   škodlivé účinky   MeSH
• chinolony aplikace a dávkování   škodlivé účinky   MeSH
• chloridy analýza   MeSH
• cystická fibróza farmakoterapie   genetika   patofyziologie   MeSH
• dítě MeSH
• dospělí MeSH
• dvojitá slepá metoda MeSH
• fixní kombinace léků MeSH
• genotyp MeSH
• indoly aplikace a dávkování   škodlivé účinky   MeSH
• lidé MeSH
• mladiství MeSH
• mladý dospělý MeSH
• mutace * MeSH
• pot chemie   MeSH
• protein CFTR genetika   MeSH
• pyrazoly aplikace a dávkování   škodlivé účinky   MeSH
• pyridiny aplikace a dávkování   škodlivé účinky   MeSH
• pyrrolidiny aplikace a dávkování   škodlivé účinky   MeSH
• usilovný výdechový objem MeSH
• Check Tag
• dítě MeSH
• dospělí MeSH
• lidé MeSH
• mladiství MeSH
• mladý dospělý MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• klinické zkoušky, fáze III MeSH
• multicentrická studie MeSH
• práce podpořená grantem MeSH
• randomizované kontrolované studie MeSH
• Research Support, N.I.H., Extramural MeSH
• Názvy látek
• aktivátory chloridových kanálů MeSH
• aminofenoly MeSH
• benzodioxoly MeSH
• CFTR protein, human MeSH Prohlížeč
• chinolony MeSH
• chloridy MeSH
• elexacaftor MeSH Prohlížeč
• fixní kombinace léků MeSH
• indoly MeSH
• ivacaftor MeSH Prohlížeč
• protein CFTR MeSH
• pyrazoly MeSH
• pyridiny MeSH
• pyrrolidiny MeSH
• tezacaftor MeSH Prohlížeč

BACKGROUND AND PURPOSE: Results regarding protective effects of dipeptidyl peptidase 4 (DPP4) inhibitors in renal ischaemia-reperfusion injury (IRI) are conflicting. Here we have compared structurally unrelated DPP4 inhibitors in a model of renal IRI. EXPERIMENTAL APPROACH: IRI was induced in uninephrectomized male rats by renal artery clamping for 30 min. The sham group was uninephrectomized but not subjected to IRI. DPP4 inhibitors or vehicle were given p.o. once daily on three consecutive days prior to IRI: linagliptin (1.5 mg·kg-1 ·day-1 ), vildagliptin (8 mg·kg-1 ·day-1 ) and sitagliptin (30 mg·kg-1 ·day-1 ). An additional group received sitagliptin until study end (before IRI: 30 mg·kg-1 ·day-1 ; after IRI: 15 mg·kg-1 ·day-1 ). KEY RESULTS: Plasma-active glucagon-like peptide type 1 (GLP-1) increased threefold to fourfold in all DPP4 inhibitor groups 24 h after IRI. Plasma cystatin C, a marker of GFR, peaked 48 h after IRI. Compared with the placebo group, DPP4 inhibition did not reduce increased plasma cystatin C levels. DPP4 inhibitors ameliorated histopathologically assessed tubular damage with varying degrees of drug-specific efficacies. Renal osteopontin expression was uniformly reduced by all DPP4 inhibitors. IRI-related increased renal cytokine expression was not decreased by DPP4 inhibition. Renal DPP4 activity at study end was significantly inhibited in the linagliptin group, but only numerically reduced in the prolonged/dose-adjusted sitagliptin group. Active GLP-1 plasma levels at study end were increased only in the prolonged/dose-adjusted sitagliptin treatment group. CONCLUSIONS AND IMPLICATIONS: In rats with renal IRI, DPP4 inhibition did not alter plasma cystatin C, a marker of glomerular function, but may protect against tubular damage.

• MeSH
• adamantan aplikace a dávkování   analogy a deriváty   chemie   farmakologie   MeSH
• dipeptidylpeptidasa 4 metabolismus   MeSH
• inhibitory dipeptidylpeptidasy 4 aplikace a dávkování   chemie   farmakologie   MeSH
• krysa rodu Rattus MeSH
• ledviny účinky léků   metabolismus   patologie   MeSH
• linagliptin aplikace a dávkování   chemie   farmakologie   MeSH
• molekulární struktura MeSH
• nitrily aplikace a dávkování   chemie   farmakologie   MeSH
• potkani Wistar MeSH
• pyrrolidiny aplikace a dávkování   chemie   farmakologie   MeSH
• reperfuzní poškození farmakoterapie   metabolismus   patologie   MeSH
• sitagliptin fosfát aplikace a dávkování   chemie   farmakologie   MeSH
• vildagliptin MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• vztahy mezi strukturou a aktivitou MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• srovnávací studie MeSH
• Názvy látek
• adamantan MeSH
• dipeptidylpeptidasa 4 MeSH
• DPP4 protein, rat MeSH Prohlížeč
• inhibitory dipeptidylpeptidasy 4 MeSH
• linagliptin MeSH
• nitrily MeSH
• pyrrolidiny MeSH
• sitagliptin fosfát MeSH
• vildagliptin MeSH

Repeated administration of partial agonist of benzodiazepine receptors Ro 19-8022 (a derivative of quinolizine class) does not elicit withdrawal in adult rats. Our older data demonstrated that single injection of Ro 19-2088 to immature rats induces increased sensitivity to convulsant action of pentylenetetrazol as a withdrawal phenomenon. To know if repeated administration of the partial agonist has the same effect we injected rats at postnatal days 7 to 11 with an anticonvulsant dose of Ro 19-8022 (0.5 mg/kg i.p.) and tested them 24 h, 48 h and 4 days after the last injection. Repeated administration of Ro 19-8022 resulted also in an increased sensitivity to convulsant action of pentylenetetrazol in immature rats (higher incidence and severity of seizures). This effect was significant 24 h after the last injection but only outlined 48 h after administration. No signs of hypersensitivity were seen at 4-day interval. There is a difference between immature and adult brain in an appearance of withdrawal symptom after administration of the partial agonist of benzodiazepine receptors Ro 19-8022.

• MeSH
• abstinenční syndrom etiologie   metabolismus   patofyziologie   MeSH
• antikonvulziva aplikace a dávkování   toxicita   MeSH
• časové faktory MeSH
• chinoliziny aplikace a dávkování   toxicita   MeSH
• krysa rodu Rattus MeSH
• modely nemocí na zvířatech MeSH
• mozek účinky léků   metabolismus   patofyziologie   MeSH
• parciální agonismus léků MeSH
• pentylentetrazol MeSH
• potkani Wistar MeSH
• pyrrolidiny aplikace a dávkování   toxicita   MeSH
• receptory GABA-A účinky léků   metabolismus   MeSH
• rozvrh dávkování léků MeSH
• transportní proteiny účinky léků   metabolismus   MeSH
• věkové faktory MeSH
• záchvaty chemicky indukované   metabolismus   patofyziologie   prevence a kontrola   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• antikonvulziva MeSH
• chinoliziny MeSH
• pentylentetrazol MeSH
• pyrrolidiny MeSH
• receptory GABA-A MeSH
• Ro 19-8022 MeSH Prohlížeč
• transportní proteiny MeSH
• Tspo protein, rat MeSH Prohlížeč

The social recognition paradigm was used to investigate the effect of trimethyltin (TMT) in adult male rats. Consequently, the effect of chronic oxiracetam (OXI) treatment in TMT impaired animals was evaluated. In all experiments, a behavioural testing was performed 3 weeks after TMT administration. Experiment 1: A single TMT oral dose, 5 and 7.5 but not 2.5mg/kg, impaired the natural ability of the adults to recognize a juvenile conspecific that they encountered 30 min before. The dose of 5mg/kg TMT was chosen to be used in subsequent experiments. Experiment 2: Chronic OXI pre-+post-treatment, daily 3 or 30 mg/kg sc for 7 days before and 7 days after the insult, protected the adults against recognition deficit produced by TMT. Experiment 3: OXI pre- but not post-treatment (always 3 and 30 mg/kg) had beneficial effects on the social recognition. The findings suggest that social recognition ability of adult male rats pre-treated sufficiently long with OXI is resistant to the neurotoxicity effect of TMT.

• MeSH
• analýza rozptylu MeSH
• časové faktory MeSH
• chování zvířat účinky léků   MeSH
• krysa rodu Rattus MeSH
• lékové interakce MeSH
• náhodné rozdělení MeSH
• neparametrická statistika MeSH
• nootropní látky aplikace a dávkování   terapeutické užití   MeSH
• poruchy paměti chemicky indukované   prevence a kontrola   MeSH
• potkani Wistar MeSH
• pyrrolidiny aplikace a dávkování   terapeutické užití   MeSH
• rozpoznávání (psychologie) účinky léků   MeSH
• rozvrh dávkování léků MeSH
• sociální izolace MeSH
• trimethylcínové sloučeniny * MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• nootropní látky MeSH
• oxiracetam MeSH Prohlížeč
• pyrrolidiny MeSH
• trimethylcínové sloučeniny * MeSH
• trimethyltin MeSH Prohlížeč

• MeSH
• atropin aplikace a dávkování   MeSH
• celková anestezie * MeSH
• dospělí MeSH
• glykopyrrolát aplikace a dávkování   MeSH
• lidé středního věku MeSH
• lidé MeSH
• nervosvalové látky nedepolarizující aplikace a dávkování   antagonisté a inhibitory   MeSH
• pyrrolidiny aplikace a dávkování   MeSH
• senioři MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• atropin MeSH
• glykopyrrolát MeSH
• nervosvalové látky nedepolarizující MeSH
• pyrrolidiny MeSH