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Chromens are naturally occurring or synthetically obtaining compounds and these are oxygen containing heterocycles, abundantly found in nature in the form of flavone, isoflavones, flavanones, catechins, anthocyanins and collective...
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Chromens are naturally occurring or synthetically obtaining compounds and these are oxygen containing heterocycles, abundantly found in nature in the form of flavone, isoflavones, flavanones, catechins, anthocyanins and collectively known as flavonoids and isoflavonoids. A large number of synthetic analogues of c hromenones have been evaluated for their anticancer, anticonvulsant, angioprotective, antiallergic, antihistaminic, antimicrobial, antioxidant, anti-HIV etc activity. A variety of cellular targets (receptors) are interacting with the derivatives of benzopyran moiety and that can be responsible for their wide ranging biological activities. The motive of the present paper on chromen and there derivatives was to review the available information on this field.
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ImportanceValproate is an antiepileptic drug (AED) used in the treatment of epilepsy and many other neurological and psychiatric disorders. Its use in pregnancy is associated with increased risks of congenital malformations and ad...
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ImportanceValproate is an antiepileptic drug (AED) used in the treatment of epilepsy and many other neurological and psychiatric disorders. Its use in pregnancy is associated with increased risks of congenital malformations and adverse neurodevelopment in the offspring and may be associated with an increased risk of attention-deficit/hyperactivity disorder (ADHD).ObjectiveTo determine whether prenatal exposure to valproate and other AEDs is associated with an increased risk of ADHD in the offspring.Design, Setting, and ParticipantsThis was a population-based cohort study of all live-born singleton children in Denmark from January 1, 1997, to December 31, 2011 (N?=?913?302). Information on prenatal exposure to AEDs, including valproate, was obtained from the Danish National Prescription Registry and all children with ADHD were identified (children with diagnosed ADHD in the Danish Psychiatric Central Research Register or children who redeemed a prescription for ADHD medication). The cohort was followed up from birth until the day of the ADHD diagnosis, death, emigration, or December 31, 2015, whichever came first. Data were analyzed in September 2018.ExposuresMaternal use of valproate and other AEDs in pregnancy.Main Outcomes and MeasuresCox regression estimates of the hazard ratio of ADHD. Estimates were adjusted for potential confounders.ResultsThe cohort included 913?302 children (mean age at end of study, 10.1 years; median age, 9.4 years; interquartile range, 7.2-12.8 years; 468?708 [51.3%] male). A total of 580 were identified as having been exposed to valproate during pregnancy; of them, 49 (8.4%) had ADHD. Among the 912?722 children who were unexposed to valproate, 29?396 (3.2%) had ADHD. Children with prenatal valproate exposure had a 48% increased risk of ADHD (adjusted hazard ratio, 1.48; 95% CI, 1.09-2.00) compared with children with no valproate exposure. The absolute 15-year risk of ADHD was 4.6% (95% CI, 4.5%-4.6%) in children unexposed to valproate and 11.0% (95% CI, 8.2%-14.2%) in children who were exposed to valproate in pregnancy. No associations were found between other AEDs and ADHD.Conclusions and RelevanceMaternal use of valproate, but not other AEDs, during pregnancy was associated with an increased risk of ADHD in the offspring. These findings have important implications for the counseling of women of childbearing potential using valproate.
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Craterocapsa tarsodes (Campanulaceae) is one of the plants used by the Northern Sotho people in an herbal remedy to treat epilepsy. A phytochemical investigation of this plant resulted in the isolation of three major secondary met...
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Craterocapsa tarsodes (Campanulaceae) is one of the plants used by the Northern Sotho people in an herbal remedy to treat epilepsy. A phytochemical investigation of this plant resulted in the isolation of three major secondary metabolites. By using NMR spectroscopy and MS spectrometry these three compounds were identified as the known acteoside (verbascoside), pinocembrin 7-beta-neohesperidoside and shanzhiside methyl ester. A literature search revealed that neurosedative properties are associated with acteoside and that flavonoids related to pinocembrin interact with benzodiazepine receptors. Therefore, the presence of acteoside and pinocembrin neohesperidoside in C. tarsodes may account for the use of this plant against epilepsy. [References: 20]
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The study examined the effect of 9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo[1,2-alpha] benzimidazole dihydrochloride (RU-1205) on the latency of seizures provoked by corazol, bicuculline, or picrotoxin. This agent (10 and 20 ...
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The study examined the effect of 9-(2-morpholinoethyl)-2-(4-fluorophenyl)imidazo[1,2-alpha] benzimidazole dihydrochloride (RU-1205) on the latency of seizures provoked by corazol, bicuculline, or picrotoxin. This agent (10 and 20 mg/kg) increased the seizure latency in the experimental models of epileptogenesis. The blockers of GABA(A) and GABA (A) -rho receptors picrotoxin and (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid, respectively, were employed to study the effects of RU-1205 on electrical activity of somatosensory cortical neurons and on formation of pathological rhythms in the rat brain. RU-1205 inhibited the focal background rhythm and eliminated the epileptiform activity, which can be mediated by interaction with GABA(A) receptors.
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Objectives: Oxcarbazepine (OXC) is a 10-keto analogue of carbamazepine used in patients with partial and secondary generalized seizures. We evaluated ingestions of OXC reported to US poison centers for adverse effects from suprath...
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Objectives: Oxcarbazepine (OXC) is a 10-keto analogue of carbamazepine used in patients with partial and secondary generalized seizures. We evaluated ingestions of OXC reported to US poison centers for adverse effects from supratherapeutic doses and/or overdose.
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Heterocyclic compounds and their derivatives gained more attention due to their valuable biological and pharmacological properties. Benzothiazole is a heterocyclic structure containing a bicyclic ring system with a large panel of ...
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Heterocyclic compounds and their derivatives gained more attention due to their valuable biological and pharmacological properties. Benzothiazole is a heterocyclic structure containing a bicyclic ring system with a large panel of applications. The benzothiazole is present in many new products undergoing research hoping that it possesses various biological activities.
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OBJECTIVE: We examined predictors of weight loss with topiramate, an anticonvulsant associated with weight loss in adults. RESEARCH METHODS AND PROCEDURES: In this uncontrolled, prospective clinical trial, topiramate was added to ...
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OBJECTIVE: We examined predictors of weight loss with topiramate, an anticonvulsant associated with weight loss in adults. RESEARCH METHODS AND PROCEDURES: In this uncontrolled, prospective clinical trial, topiramate was added to existing anticonvulsants in adults (40 to 110 kg) with partial-onset seizures. Primary measurements were change from baseline weight after 3 months and 1 year in patients completing 1 year of topiramate treatment (N = 38). Physiological and metabolic measures were analyzed for correlation with weight loss during topiramate treatment. RESULTS: In patients who completed 1 year of topiramate treatment, baseline weight was reduced in 82% at 3 months and in 86% at 1 year. Mean body weight was reduced 3.0 kg (3.9% of baseline) at 3 months and 5.9 kg (7.3%) at 1 year. In obese patients [body mass index (BMI) >/= 30 kg/m(2)], mean weight loss was 4.2 kg (4.3%) at 3 months and 10.9 kg (11.0%) at 1 year. Weight loss was primarily caused by reduction in body fat mass. For all patients, weight loss at 3 months correlated most strongly with reduced caloric intake (p = 0.02). At 1 year, caloric intake had returned to baseline levels; weight loss correlated most strongly with higher baseline BMI (p = 0.0007). DISCUSSION: Our results suggest that weight loss occurs in most adults treated with topiramate and is sustained for at least 1 year. Reduced caloric intake may account, in part, for weight loss during early treatment. The pattern of weight loss differs according to baseline BMI, with obese patients experiencing greater weight loss during continued therapy.
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Purpose of Review Treatment-resistant epilepsy comprises approximately 36.3% of neurology clinic-based populations in the USA. Despite new drug development over the past 50 years, the rates of drug-resistant epilepsy remain the sa...
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Purpose of Review Treatment-resistant epilepsy comprises approximately 36.3% of neurology clinic-based populations in the USA. Despite new drug development over the past 50 years, the rates of drug-resistant epilepsy remain the same. The need for continued drug trials with novel mechanisms of action remains paramount in patients with drug-resistant epilepsy. In particular, patients with severe epilepsy syndromes such as Dravet syndrome (DS) and Lennox Gastaut syndrome (LGS) continue to be the most severely affected due to the increased rates of status epilepticus and sudden unexpected death (SUDEP). Recent Findings Fenfluramine has recently been FDA-approved for DS and LGS. There is substantial evidence highlighting the efficacy of fenfluramine in the treatment of seizures associated with DS and LGS. There are a growing number of studies investigating alternative uses of fenfluramine for treatment-resistant epilepsies. Summary The completed studies suggest that fenfluramine is both a safe and efficacious adjunctive therapy in the treatment of convulsive seizures and drop seizures associated with DS and LGS. Fenfluramine's suggested mechanism of action and available human evidence likely support its efficacy as an add-on therapy for more seizure types and calls for further research to expand its clinical use.
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Objective: To eavaluate the CNS activity of Bramhi Ghrita, a polyherbal formulation containing Bacopa monneh, Evolvulus alsinoids, Acorus calamus, Saussurea Zappa and cow's ghee.Materials and Methods: The effect of Bramhi Ghrita o...
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Objective: To eavaluate the CNS activity of Bramhi Ghrita, a polyherbal formulation containing Bacopa monneh, Evolvulus alsinoids, Acorus calamus, Saussurea Zappa and cow's ghee.Materials and Methods: The effect of Bramhi Ghrita on motor coordination, behavior, sleep, convulsions, locomotion and analgesia was evaluated in mice using standard procedures.Results: The formulation exhibited reduced alertness, spontaneous locomotor activity and reactivity. It also antagonized the behavioral effects of d-amphetamine, potentiated the pentobarbitone-induced sleep and increased the pain threshold. Bramhi Ghrita protected mice from maximum electroshock and pentylene tetrazole-induced convulsions.Conclusion: The Bramhi Ghrita was found to be a CNS depressant with anticonvulsant activity.
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C23H25Cl2N3O4Sn, triclinic, P (1) over bar (no. 2), a = 10.371(3) angstrom, b = 10.721(3) angstrom, c = 12.615(4) angstrom, alpha = 109.698(4)degrees, beta = 97.556(5)degrees, gamma = 109.116(4)degrees, V = 1200.8 angstrom(3), Z =...
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C23H25Cl2N3O4Sn, triclinic, P (1) over bar (no. 2), a = 10.371(3) angstrom, b = 10.721(3) angstrom, c = 12.615(4) angstrom, alpha = 109.698(4)degrees, beta = 97.556(5)degrees, gamma = 109.116(4)degrees, V = 1200.8 angstrom(3), Z = 2, R-gt(F) = 0.050, wR(ref)(F-2) = 0.134, T = 293 K.
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