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Said A Said, Abd el-Galil E Amr, Nermien M Sabry, Mohamed M Abdalla
A series of diazipine, pyrimidine, fused triazolopyrimidine and imide derivatives were newly synthesized using 4-phenyl-but-3-en-2-one 1 as a starting material and compounds 2 and 9 are intermediates. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds were interestingly less toxic than the reference drug. The pharmacological screening showed that many of these obtained compounds have good analgesic, anticonvulsant and anti-inflammatory activities comparable to Valdecoxib, Carbamazepine and Predensilone as reference drugs...
December 2009: European Journal of Medicinal Chemistry
Jitender B Bariwal, Kuldip D Upadhyay, Atul T Manvar, Jalpa C Trivedi, Jyoti S Singh, Kishor S Jain, Anamik K Shah
1,5-Benzothiazepine and 1,5-benzodiazipine are the two main seven-membered heterocyclic ring systems reported for their cardiac and psychotherapeutic activities. Successful introduction of diltiazem and clentiazem for angina pectoris, hypertension, arrhythmias and other related cardiac disorders proved potential of 1,5-benzothiazepine moiety. Subsequently 1,5-benzodiazepines were highlighted as important biologically active scaffolds. Also, discovery of thiazesim and quetiapine fumarate as psychotropic agents attracted much attention worldwide...
November 2008: European Journal of Medicinal Chemistry
Victoria Faint
Hepatic encephalopathy (HE) is a complicated disorder, the pathophysiology of which remains to be fully understood. This article reviews the current main theories including the potential involvement of ammonia, gamma-aminobutyric acid (GABA)/benzodiazipines and false neurotransmitters. Each theory is critically examined with the evidence for each reviewed carefully, and the potential relationship of ammonia to the remaining two theories explored. Known preciptating factors of HE are also considered as evidence...
March 2006: Nursing in Critical Care
Rooban Thavarajah, Anita Rao, Uma Raman, Saraswathi T Rajasekaran, Elizabeth Joshua, Hemalatha R, Ranganathan Kannan
The aim of this study was to ascertain the prevalence of oral lesions among 500 psychoactive substance users in a hospital-based population. The study group consisted of 500 consecutive patients attending TTK Hospital, a non-governmental organisation involved in rehabilitation of substance users. Patient history was recorded in a pre-determined format and clinical findings were recorded by a trained physician and dental surgeons. Psychoactive substances used by the patients were alcohol (97%), tobacco (72%), arecanut (57...
June 2006: Archives of Oral Biology
Jorge E Torres-Muñoz, Corina Van Waveren, Martha G Keegan, Richard J Bookman, Carol K Petito
Pyramidal neurons in hippocampal subregions are selectively vulnerable in certain disease states. To investigate, we tested the hypothesis that selective vulnerability in human hippocampus is related to regional differences in neuronal cell death and cell receptor gene expression in CA1 vs. CA3 subregions. We used laser capture microdissection to remove approximately 600 CA1 and 600 CA3 pyramidal neurons each from five fresh-frozen normal post-mortem brains, extracted total RNA and double-amplified mRNA. This was reverse transcribed and labeled for hybridization onto human cDNA array chips containing probes to 10,174 genes and unknown ESTs...
August 23, 2004: Brain Research. Molecular Brain Research
D J Mokler, J R Galler, J I Luebke
Prenatal protein malnutrition has been demonstrated to result in alterations in the serotonergic and GABAergic neurotransmitter systems in the rat hippocampus. In the present study, whole-cell patch clamp recordings of CA1 pyramidal cells were employed in an effort to gain insight into the specific cellular locus and functional consequences of the previously reported changes. Hippocampal slices were prepared from Sprague-Dawley rats whose dams were fed either a normal (25% casein) or low (6% casein) protein diet during pregnancy...
2001: Nutritional Neuroscience
John L Zautcke, Steven B Coker, Ralph W Morris, Leslee Stein-Spencer
As the elderly population increases and they lead more active and healthy lifestyles, their exposure to the threats of injury multiply. Undoubtedly, the geriatric population will comprise a growing percentage of trauma patients. The role of alcohol and drug use in geriatric trauma has not been clearly defined. The purpose of this study is to determine the incidence of alcohol and illicit drug use in association with mechanism of injury in all elderly trauma patients presenting to level I and II trauma centers in the State of Illinois over 3 years...
January 2002: American Journal of Emergency Medicine
R Robert, P Blakeney, C Villarreal, W J Meyer
Anxiety is an affective response commonly experienced by persons after emotional and physical trauma, as well as associated with aversive medical treatments. The scientific information related to the conceptualization, assessment, and treatment of anxiety is limited. In order to develop a pilot protocol for anxiety management, nursing directors at 64 burn centers were surveyed. At 89% of the centers, anxiety measures were not used. Most of the teams assess informally through observation of patient (n=21), dialogue with patient (n=12), or both observation and dialogue with patient (n=15)...
September 2000: Burns: Journal of the International Society for Burn Injuries
M A Tsivil'ko, M V Korkina, N N Shinaev, N P Volkova, A Iu Kucherov
Zolpidem, non-benzodiazipine preparation, was used for therapy of 56 patients with insomnia. 4 groups of patients were treated: a) with a prevalence of asthenic symptomatology in psychogenic disorders; b) with polymorphic neurotic symptomatology and autonomic disorders; c) with affective pathology of neurotic level; d) with nervous anorexia and bulimia. Zolpidem was quite effective in all groups of patients in terms of normalization of falling asleep, improvement of quality of sleep without changing of daily activity...
1999: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
L G Magazanik, P N Usherwood
The classical division of mammalian ionotropic L-glutamate (Glu) receptors into N-methyl-D-aspartate (NMDA) and non-NMDA classes is supported by a wealth of biochemical and molecular biological data. In binding studies, selective agonists for non-NMDA receptors such as L-kainate (KA), alpha-amino-3-hydroxy-5-methylisoxazole-propionate (AMPA) and L-domoate have submicromolar affinities; in contrast, a millimolar concentration of NMDA is required significantly to compete with the non-NMDA agonists. Despite the supposed clear-cut selectivities of these amino acids, interactions between the responses to submillimolar concentrations of NMDA and KA have been observed in cells expressing both classes of Glu receptor...
December 20, 1996: Neuroreport
L Bailey, M Ward, M N Musa
No abstract text is available yet for this article.
August 1994: Journal of Clinical Pharmacology
J T Sobota, L Lummis
Laboratory evaluation of illicit drug abuse was conducted in a major correctional institution. Fifty-eight prison inmates were screened for common drugs of abuse in conjunction with a triazolo-benzodiazipine compound tolerance protocol. Urine specimens were collected on days -1, 1, 15, 29, and 49 and assayed for amphetamines, opiates, barbiturates, and alcohol. Quinine was detected in two individuals and was probably derived from cold remedy preparations rather than the illegal use of heroin. While occasional illicit drugs may find their way into a prison population, this study showed no evidences of drug abuse in one correctional institution whose prisoners participated in Phase I drug evaluations...
1974: Clinical Toxicology
A W Heinemann, S Schnoll, M Brandt, R Maltz, M Keen
The validity of self-reported intoxication at time of spinal cord injury (SCI) was examined for 88 cases at admission to an acute SCI center by comparing self-reports with serum and urine analyses. Serum ethanol greater than 50 mg/dl was the most frequently found substance (observed in 40% of the cases) followed by urine analysis evidence of cocaine (14%), cannabinoids (8%), benzodiazipines (5%), and opiates (4%). Evidence of substances with abuse potential was found in urine for 35% of the sample. While 62% of the sample had either serum ethanol greater than 50 mg/dl or a positive urine analysis, only 42% of the sample reported being under the influence of some substance at the time of SCI...
December 1988: Alcoholism, Clinical and Experimental Research
C Stumpf, G Gogolák, S Huck, A Andics
The synergistic action of seven central depressants three benzodiazepines, two neuroleptics on barbiturate and morphine on the anesthetic activity of nitrous oxide was studied in mice. The benzodiazipines and among them nitrazepam and flunitrazepam were found to be the most potent drugs in this respect; morphine on the other hand was innefective even in toxic doses. There was a significant difference in the slope of log dose-response curves; these curves were much steeper for pentobarbitone, droperidol and chlorpromazine than for nitrazepam, flunitrazepam, and diazepam...
June 1975: Der Anaesthesist
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