Effects of Pharmaceuticals on Aquatic Invertebrates. Part II: The
... This is of concern because some residues have been detected in drinking water (Ternes 2000). Although most of these compounds occur in surface waters in the nanogram-per-liter range, hazards for aquatic biota cannot be excluded because of high biological activity. This has been demonstrated for endo ...
... This is of concern because some residues have been detected in drinking water (Ternes 2000). Although most of these compounds occur in surface waters in the nanogram-per-liter range, hazards for aquatic biota cannot be excluded because of high biological activity. This has been demonstrated for endo ...
Psilocybin links binocular rivalry switch rate to attention and
... address this issue. These models generally propose that groups of neurons associated with the two rivalry percepts will directly suppress each other through mutual inhibitory connections. Over time, the dominant neurons will “fatigue”, and their inhibitory effects will be reduced, resulting in a swi ...
... address this issue. These models generally propose that groups of neurons associated with the two rivalry percepts will directly suppress each other through mutual inhibitory connections. Over time, the dominant neurons will “fatigue”, and their inhibitory effects will be reduced, resulting in a swi ...
Preclinical Evaluation of the Effects of a Novel Antisense Compound
... Spainhour). Mice were acclimated for approximately 10 days and were approximately 8 to 9 weeks old at initiation of the study. Upon receipt mice were housed individually in stainless-steel cages and given free access to water and aliquoted certified rodent chow. Groups of 10 male and 10 female mice ...
... Spainhour). Mice were acclimated for approximately 10 days and were approximately 8 to 9 weeks old at initiation of the study. Upon receipt mice were housed individually in stainless-steel cages and given free access to water and aliquoted certified rodent chow. Groups of 10 male and 10 female mice ...
A novel panel of mouse models to evaluate the role of human
... II enzymes as well as transporters on the one hand and their selectivity for different ligands in distinct species on the other can give rise to profound differences in drug bioavailability, distribution, toxicity, and efficacy between animals and humans. To overcome these problems, humanized mouse ...
... II enzymes as well as transporters on the one hand and their selectivity for different ligands in distinct species on the other can give rise to profound differences in drug bioavailability, distribution, toxicity, and efficacy between animals and humans. To overcome these problems, humanized mouse ...
Natural Organic Chemicals on Development
... maturation, whereas survivorship was not effected. These sublethal exposures to carbaryl reduced Daphnia population growth rate (productivity) by about 15% (at 5 ppb), enough to have significant ecological effects on the rest of the lake community. The insecticide carbaryl showed synergistic interac ...
... maturation, whereas survivorship was not effected. These sublethal exposures to carbaryl reduced Daphnia population growth rate (productivity) by about 15% (at 5 ppb), enough to have significant ecological effects on the rest of the lake community. The insecticide carbaryl showed synergistic interac ...
Commentary: Reproductive Risks of Leflunomide (ArravaR
... margins are even higher. It has been shown that the pharmacodynamic effects of leflunomide, namely dihydroorotate dehydrogenase (DHO-DH) inhibition and anti-proliferative activity, considered to be responsible for the embryotoxic and teratogenic effects, are species-specific and significantly differ ...
... margins are even higher. It has been shown that the pharmacodynamic effects of leflunomide, namely dihydroorotate dehydrogenase (DHO-DH) inhibition and anti-proliferative activity, considered to be responsible for the embryotoxic and teratogenic effects, are species-specific and significantly differ ...
Dynamic mimicry in an Indo Malyan Octopus
... can be regarded as Batesian, in which case selection is expected to favour the evolution of mimicry of a range of models, because novel forms of mimicry are less likely to be detected by predators and will tend to create a lower ratio of mimics to models. Mimicry of multiple models occurs through ge ...
... can be regarded as Batesian, in which case selection is expected to favour the evolution of mimicry of a range of models, because novel forms of mimicry are less likely to be detected by predators and will tend to create a lower ratio of mimics to models. Mimicry of multiple models occurs through ge ...
Binding Studies of Type I, II, and III Kinase Inhibitors against Bcr
... for some of the A-loop mutants to complete resistance for the T315I mutation which precludes imatinib from binding. The steady rate of developing resistance to imatinib has suggested that new kinase inhibitors could be of clinical value, if they could override imatinib resistance and bind with highe ...
... for some of the A-loop mutants to complete resistance for the T315I mutation which precludes imatinib from binding. The steady rate of developing resistance to imatinib has suggested that new kinase inhibitors could be of clinical value, if they could override imatinib resistance and bind with highe ...
Pharmacology of Antiepileptic Drugs
... – Very strong sedation; Cognitive impairment; Behavioral changes – Very long half-life (up to ~5days); #Induces P450 – Tolerance may arise; Risk of dependence – Primidone, another barbiturate metabolized to Phenobarbital, and Phenobarbital are now seldom used in initial therapy, owing to side-effect ...
... – Very strong sedation; Cognitive impairment; Behavioral changes – Very long half-life (up to ~5days); #Induces P450 – Tolerance may arise; Risk of dependence – Primidone, another barbiturate metabolized to Phenobarbital, and Phenobarbital are now seldom used in initial therapy, owing to side-effect ...
Seizure
... – Very strong sedation; Cognitive impairment; Behavioral changes – Very long half-life (up to ~5days); #Induces P450 – Tolerance may arise; Risk of dependence – Primidone, another barbiturate metabolized to Phenobarbital, and Phenobarbital are now seldom used in initial therapy, owing to side-effect ...
... – Very strong sedation; Cognitive impairment; Behavioral changes – Very long half-life (up to ~5days); #Induces P450 – Tolerance may arise; Risk of dependence – Primidone, another barbiturate metabolized to Phenobarbital, and Phenobarbital are now seldom used in initial therapy, owing to side-effect ...
Epinephrine
... Recommended therapeutic dosage of epinephrine for allergic emergencies is 0.1 to 0.3 mg as a subcutaneous injection. For treatment of myocardial infarction or cardiac arrest (resuscitation efforts) a dosage of 0.5 to 1 mg every 5 min is recommended [5]. Epinephrine may be toxic and even fatal at ele ...
... Recommended therapeutic dosage of epinephrine for allergic emergencies is 0.1 to 0.3 mg as a subcutaneous injection. For treatment of myocardial infarction or cardiac arrest (resuscitation efforts) a dosage of 0.5 to 1 mg every 5 min is recommended [5]. Epinephrine may be toxic and even fatal at ele ...
DOCTORAL THESIS
... of researchers working in the field. Based on previously obtained results for several peptoid hits that showed activity as uncompetitive TRPV1 antagonists, and that allowed to propose a basic pharmacophoric hypothesis consisting on one cationic and two identical aromatic moieties, this thesis focuse ...
... of researchers working in the field. Based on previously obtained results for several peptoid hits that showed activity as uncompetitive TRPV1 antagonists, and that allowed to propose a basic pharmacophoric hypothesis consisting on one cationic and two identical aromatic moieties, this thesis focuse ...
A Brief History of Great Discoveries in Pharmacology: In Celebration
... number of documents on a given subject, one is often presented from different perspectives. To deal with this situation, I have tried to explore as many diverse accounts that I felt were needed to paint as accurate a picture as possible. ...
... number of documents on a given subject, one is often presented from different perspectives. To deal with this situation, I have tried to explore as many diverse accounts that I felt were needed to paint as accurate a picture as possible. ...
Genetically engineered organisms and the environment: Current
... distinguishes them from previous varieties (e.g., Snow 2003). In this report, we use the terms genetic engineering, genetic modification, transgenics, and recombinant DNA technology interchangeably. The goal of predicting how genetic engineering will affect organisms that live and disperse outdoors ...
... distinguishes them from previous varieties (e.g., Snow 2003). In this report, we use the terms genetic engineering, genetic modification, transgenics, and recombinant DNA technology interchangeably. The goal of predicting how genetic engineering will affect organisms that live and disperse outdoors ...
Modulation of ventral tegmental area dopamine receptors inhibit
... The present findings indicate that nicotine injection into the central amygdala (CeA) decreased % open arm time spent (%OAT) and % open arm entries (OAE %) in the elevated plus maze (EPM) test, suggesting an anxiogenic-like effect. Although, this is consistent with previous studies showing an anxioge ...
... The present findings indicate that nicotine injection into the central amygdala (CeA) decreased % open arm time spent (%OAT) and % open arm entries (OAE %) in the elevated plus maze (EPM) test, suggesting an anxiogenic-like effect. Although, this is consistent with previous studies showing an anxioge ...
In Vitro Metabolism of Haloperidol and Sila-Haloperidol
... silicon compounds compared with their corresponding carbon analogs. Silicon (1.74, Allred-Rochow scale) is less electronegative than carbon (2.50), leading to different polarizations of analogous carbonand silicon-element bonds, manifested by, for example, an increased acidity of silanols compared w ...
... silicon compounds compared with their corresponding carbon analogs. Silicon (1.74, Allred-Rochow scale) is less electronegative than carbon (2.50), leading to different polarizations of analogous carbonand silicon-element bonds, manifested by, for example, an increased acidity of silanols compared w ...
Bioisosterism: A Rational Approach in Drug Design
... been correlated with some substituent constants commonly employed in QSAR studies. These observations are consistent with the fact that bioisosteric replacements often provide the foundation for the development of QSAR in drug design.4,6 Recent advances in molecular biology, such as cloning of the v ...
... been correlated with some substituent constants commonly employed in QSAR studies. These observations are consistent with the fact that bioisosteric replacements often provide the foundation for the development of QSAR in drug design.4,6 Recent advances in molecular biology, such as cloning of the v ...
Cannabidiol: Pharmacology and potential therapeutic role
... To present a summary of current scientific evidence about the cannabinoid, cannabidiol (CBD) with regard to its relevance to epilepsy and other selected neuropsychiatric disorders. We summarize the presentations from a conference in which invited participants reviewed relevant aspects of the physiol ...
... To present a summary of current scientific evidence about the cannabinoid, cannabidiol (CBD) with regard to its relevance to epilepsy and other selected neuropsychiatric disorders. We summarize the presentations from a conference in which invited participants reviewed relevant aspects of the physiol ...
NUSRAT ADUSEI HAMENOO - Kwame Nkrumah University of
... The hepatoprotective assessment was determined biochemically (using Liver Function Test, LFTs), morphologically (histopathological) and functionally (using Pentobarbitone-induced sleep time) in rodents. In general toxicological assessment, the effects of the extract on haematological, biochemical, m ...
... The hepatoprotective assessment was determined biochemically (using Liver Function Test, LFTs), morphologically (histopathological) and functionally (using Pentobarbitone-induced sleep time) in rodents. In general toxicological assessment, the effects of the extract on haematological, biochemical, m ...
The Glycine Transporter-1 Inhibitor SSR103800 Displays a
... Schizophrenia has been initially associated with dysfunction in dopamine neurotransmission. However, the observation that antagonists of the glutamate N-methyl-D-aspartate (NMDA) receptor produce schizophrenic-like symptoms in humans has led to the idea of a dysfunctioning of the glutamatergic syste ...
... Schizophrenia has been initially associated with dysfunction in dopamine neurotransmission. However, the observation that antagonists of the glutamate N-methyl-D-aspartate (NMDA) receptor produce schizophrenic-like symptoms in humans has led to the idea of a dysfunctioning of the glutamatergic syste ...
Stahl_3rd_ch12_Part1..
... major depression is the current challenge for those who treat this disorder; this is the reason for learning the mechanisms of action of so many drugs, the complex biological rationale for combining specific sets of drugs, and the practical tactics for tailoring a unique drug treatment portfolio to ...
... major depression is the current challenge for those who treat this disorder; this is the reason for learning the mechanisms of action of so many drugs, the complex biological rationale for combining specific sets of drugs, and the practical tactics for tailoring a unique drug treatment portfolio to ...
Psychedelic Drugs - American College of Neuropsychopharmacology
... diastereomer of chlorobutyl LSD, is at least 50% more potent than LSD. In ligand binding at 5-HT2, 5-HT1A, D1, and D2 receptors, the (R)-2-butylamide substituent is likewise more potent. Cloning of the 5-HT-2 receptor permitted replacement of aspartate 120 in second transmembrane domain with asparag ...
... diastereomer of chlorobutyl LSD, is at least 50% more potent than LSD. In ligand binding at 5-HT2, 5-HT1A, D1, and D2 receptors, the (R)-2-butylamide substituent is likewise more potent. Cloning of the 5-HT-2 receptor permitted replacement of aspartate 120 in second transmembrane domain with asparag ...
Hidden Dangers: Herbal and Dietary Supplement Induced
... used today, were transcribed 2000 years later in the great herbal book, Shen Nung Pen Tsao Ching. Numerous herbs including turmeric were mentioned in Aryuvedic books in India nearly 3000 years ago. In Egypt, the Ebers Papyrus (ca. 1550 B.C.) details over 800 formulas of 700 different plants. The anc ...
... used today, were transcribed 2000 years later in the great herbal book, Shen Nung Pen Tsao Ching. Numerous herbs including turmeric were mentioned in Aryuvedic books in India nearly 3000 years ago. In Egypt, the Ebers Papyrus (ca. 1550 B.C.) details over 800 formulas of 700 different plants. The anc ...
ALBIZIA RATS PROCERA ROXB
... necrosis after undergoing bio-activation to a toxic electrophile, Nacetyl-p-benzoquinoneimine(NAPQI) by cytochrome P-450 monooxygenase[19]. NAPQI binds to macromolecules and cellular proteins. Liver enzymes, ALT, AST, and ALP are usually low in normal control. Injury to the liver results in the rele ...
... necrosis after undergoing bio-activation to a toxic electrophile, Nacetyl-p-benzoquinoneimine(NAPQI) by cytochrome P-450 monooxygenase[19]. NAPQI binds to macromolecules and cellular proteins. Liver enzymes, ALT, AST, and ALP are usually low in normal control. Injury to the liver results in the rele ...
Toxicodynamics
Toxicodynamics, termed pharmacodynamics in pharmacology, describes the dynamic interactions of a toxicant with a biological target and its biological effects. A biological target, also known as the site of action, can be binding proteins, ion channels, DNA, or a variety of other receptors. When a toxicant enters an organism, it can interact with these receptors and produce structural or functional alterations. The mechanism of action of the toxicant, as determined by a toxicant’s chemical properties, will determine what receptors are targeted and the overall toxic effect at the cellular level and organismal level.Toxicants have been grouped together according to their chemical properties by way of quantitative structure-activity relationships (QSARs), which allows prediction of toxic action based on these properties. endocrine disrupting chemicals (EDCs) and carcinogens are examples of classes of toxicants that can act as QSARs. EDCs mimic or block transcriptional activation normally caused by natural steroid hormones. These types of chemicals can act on androgen receptors, estrogen receptors and thyroid hormone receptors. This mechanism can include such toxicants as dichlorodiphenyltrichloroethane (DDE) and polychlorinated biphenyls (PCBs). Another class of chemicals, carcinogens, are substances that cause cancer and can be classified as genotoxic or nongenotoxic carcinogens. These categories include toxicants such as polycyclic aromatic hydrocarbon (PAHs) and carbon tetrachloride (CCl4). The process of toxicodynamics can be useful for application in environmental risk assessment by implementing toxicokinetic-toxicodynamic (TKTD) models. TKTD models include phenomenas such as time-varying exposure, carry-over toxicity, organism recovery time, effects of mixtures, and extrapolation to untested chemicals and species. Due to their advantages, these types of models may be more applicable for risk assessment than traditional modeling approaches.