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A 2D-QSPR approach to predict blood-brain barrier penetration of drugs acting on the central nervous system BJPS
Sá,Matheus Malta de; Pasqualoto,Kerly Fernanda Mesquita; Rangel-Yagui,Carlota de Oliveira.
Drugs acting on the central nervous system (CNS) have to cross the blood-brain barrier (BBB) in order to perform their pharmacological actions. Passive BBB diffusion can be partially expressed by the blood/brain partition coefficient (logBB). As the experimental evaluation of logBB is time and cost consuming, theoretical methods such as quantitative structure-property relationships (QSPR) can be useful to predict logBB values. In this study, a 2D-QSPR approach was applied to a set of 28 drugs acting on the CNS, using the logBB property as biological data. The best QSPR model [n = 21, r = 0.94 (r² = 0.88), s = 0.28, and Q² = 0.82] presented three molecular descriptors: calculated n-octanol/water partition coefficient (ClogP), polar surface area (PSA), and...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Two-dimensional quantitative structure-property relationships (2D-QSPR); Calculated n-octanol/water partition coefficient (ClogP); Blood-brain barrier; Benzodiazepines.
Ano: 2010 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502010000400016
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Interaction between repeated restraint stress and concomitant midazolam administration on sweet food ingestion in rats BJMBR
Silveira,P.P.; Xavier,M.H.; Souza,F.H.; Manoli,L.P.; Rosat,R.M.; Ferreira,M.B.C.; Dalmaz,C..
Emotional changes can influence feeding behavior. Previous studies have shown that chronically stressed animals present increased ingestion of sweet food, an effect reversed by a single dose of diazepam administered before testing the animals. The aim of the present study was to evaluate the response of animals chronically treated with midazolam and/or submitted to repeated restraint stress upon the ingestion of sweet food. Male adult Wistar rats were divided into two groups: controls and exposed to restraint 1 h/day, 5 days/week for 40 days. Both groups were subdivided into two other groups treated or not with midazolam (0.06 mg/ml in their drinking water during the 40-day treatment). The animals were placed in a lighted area in the presence of 10 pellets...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Feeding behavior; Chronic stress; Benzodiazepines; Midazolam; Sweet taste; Rats.
Ano: 2000 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000001100013
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Participation of the GABAergic system in the anesthetic effect of Lippia alba (Mill.) N.E. Brown essential oil BJMBR
Heldwein,C.G.; Silva,L.L.; Reckziegel,P.; Barros,F.M.C.; Bürger,M.E.; Baldisserotto,B.; Mallmann,C.A.; Schmidt,D.; Caron,B.O.; Heinzmann,B.M..
The objective of this study was to identify the possible involvement of the GABAergic system in the anesthetic effect of Lippia alba essential oil (EO). We propose a new animal model using silver catfish (Rhamdia quelen) exposed to an anesthetic bath to study the mechanism of action of EO. To observe the induction and potentiation of the anesthetic effect of EO, juvenile silver catfish (9.30 ± 1.85 g; 10.15 ± 0.95 cm; N = 6) were exposed to various concentrations of L. alba EO in the presence or absence of diazepam [an agonist of high-affinity binding sites for benzodiazepinic (BDZ) sites coupled to the GABA A receptor complex]. In another experiment, fish (N = 6) were initially anesthetized with the EO and then transferred to an anesthetic-free aquarium...
Tipo: Info:eu-repo/semantics/article Palavras-chave: False-melissa; Silver catfish; Benzodiazepines; Flumazenil; GABA.
Ano: 2012 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2012000500009
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The brain decade in debate: II. Panic or anxiety? From animal models to a neurobiological basis BJMBR
Andreatini,R.; Blanchard,C.; Blanchard,R.; Brandão,M.L.; Carobrez,A.P.; Griebel,G.; Guimarães,F.S.; Handley,S.L.; Jenck,F.; Leite,J.R.; Rodgers,J.; Schenberg,L.C.; Da Cunha,C.; Graeff,F.G..
This article is a transcription of an electronic symposium sponsored by the Brazilian Society of Neuroscience and Behavior (SBNeC). Invited researchers from the European Union, North America and Brazil discussed two issues on anxiety, namely whether panic is a very intense anxiety or something else, and what aspects of clinical anxiety are reproduced by animal models. Concerning the first issue, most participants agreed that generalized anxiety and panic disorder are different on the basis of clinical manifestations, drug response and animal models. Also, underlying brain structures, neurotransmitter modulation and hormonal changes seem to involve important differences. It is also common knowledge that existing animal models generate different types of...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Panic; Anxiety; Fear; Anxiolytics; 5-HT; Benzodiazepines; Serotonin; Amygdala; Periaqueductal gray matter; Animal models.
Ano: 2001 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2001000200001
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Ultrastructure of Fetal Mice Hepatocytes Exposed in Utero to Diazepam International Journal of Morphology
Márquez-Orozco,María Cristina; de la Fuente-Juárez,Graciela; Márquez-Orozco,Amalia.
Previous research has shown that fetal mice hepatic cells from females treated with diazepam (Valium) during pregnancy depict cytoplasmic and nuclear modifications when observed with photonic microscope. The purpose of this work is to investigate if diazepam administered subcutaneously (SC) to pregnant mice females induces ultraestructural alterations in the cytoplasmic organelles and nucleus to fetal hepatocytes. Transmission electron microscopy observations of fetal hepatocytes from pregnant females treated with a single daily dose of diazepam 2.7 mg/kg/bw/SC administered from 6th to 15th days of gestation revealed that they frequently presented disorganized and dilated rough endoplasmic reticulum cisterns, membranous elements, abundant Golgi complex and...
Tipo: Journal article Palavras-chave: Benzodiazepines; Diazepam; Fetal hepatocytes; Ultrastructure.
Ano: 2015 URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-95022015000400040
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