Potential role of N-methyl-D-aspartate receptors as executors of
... mechanism of action. This assessment does not, however, take into account the fact that memantine is accumulated in intracellular compartments (primarily by lysosomes) (Honegger et al., 1993). Indeed, the analysis of memantine levels in brain homogenates in rats revealed 30-fold higher values than t ...
... mechanism of action. This assessment does not, however, take into account the fact that memantine is accumulated in intracellular compartments (primarily by lysosomes) (Honegger et al., 1993). Indeed, the analysis of memantine levels in brain homogenates in rats revealed 30-fold higher values than t ...
Melatonin as a potential anticarcinogen for non-small
... by Borin et al. [17] reported that melatonin was effective in controlling metastatic breast cancer in vitro and in vivo, not only via suppression of the proliferation of cancer cells but also through suppression of cancer metastasis by ROCK-1 inhibition. Whether melatonin treatment inhibits NSCLC me ...
... by Borin et al. [17] reported that melatonin was effective in controlling metastatic breast cancer in vitro and in vivo, not only via suppression of the proliferation of cancer cells but also through suppression of cancer metastasis by ROCK-1 inhibition. Whether melatonin treatment inhibits NSCLC me ...
Role of Mu- and Delta-Opioid Receptors in the
... reinstatement of cocaine seeking, and intra-NAc morphine infusions induce a conditioned place preference (van der Kooy et al, 1982). Opioid receptors are highly expressed by NAc neurons (Mansour et al, 1995, 1987), and local opioid infusions in the NAc modulate behavior in a biphasic manner. Thus, m ...
... reinstatement of cocaine seeking, and intra-NAc morphine infusions induce a conditioned place preference (van der Kooy et al, 1982). Opioid receptors are highly expressed by NAc neurons (Mansour et al, 1995, 1987), and local opioid infusions in the NAc modulate behavior in a biphasic manner. Thus, m ...
Selective inhibitor of LRRK2, a protein kinase
... Figure 1 Enzymatic activity of LRRK2-IN-1 and its selectivity. (a) Chemical structure of the LRRK2 inhibitor LRRK2-IN-1. (b) GST-LRRK2 (1326-2517), GSTLRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2517) and GSTLRRK2 [A2016T+G2019S] (1326-2517) were assayed using 20M Nictide in the presence o ...
... Figure 1 Enzymatic activity of LRRK2-IN-1 and its selectivity. (a) Chemical structure of the LRRK2 inhibitor LRRK2-IN-1. (b) GST-LRRK2 (1326-2517), GSTLRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2517) and GSTLRRK2 [A2016T+G2019S] (1326-2517) were assayed using 20M Nictide in the presence o ...
Dopamine, behavioral economics, and effort
... animals, the overall relation between ratio size and response output is inverted-U shaped. Up to a point, as ratio requirements get larger, animals adjust to this challenge by increasing response output. However, if the ratio requirement is high enough (i.e., if the cost is too high), the animal rea ...
... animals, the overall relation between ratio size and response output is inverted-U shaped. Up to a point, as ratio requirements get larger, animals adjust to this challenge by increasing response output. However, if the ratio requirement is high enough (i.e., if the cost is too high), the animal rea ...
Antiemesis - proLekare.cz
... The risk of nausea/vomiting for persons receiving chemotherapy of high and moderate emetic risk lasts for at least 3 days for high and 2 days for moderate after the last dose of chemotherapy. Patients need to be protected throughout the full period of risk. • Oral and intravenous 5-HT3 antagonists ...
... The risk of nausea/vomiting for persons receiving chemotherapy of high and moderate emetic risk lasts for at least 3 days for high and 2 days for moderate after the last dose of chemotherapy. Patients need to be protected throughout the full period of risk. • Oral and intravenous 5-HT3 antagonists ...
Insulin-like actions of vanadium: Potential as a
... insulin have been under intensive investigation for many years. Vanadium as an insulin mimetic/enhancing agent is one of the potential candidates for oral therapy in type 1 diabetes. Several studies have shown that chronic treatment with vanadium salts restores plasma glucose levels and corrects hyp ...
... insulin have been under intensive investigation for many years. Vanadium as an insulin mimetic/enhancing agent is one of the potential candidates for oral therapy in type 1 diabetes. Several studies have shown that chronic treatment with vanadium salts restores plasma glucose levels and corrects hyp ...
Advances in phage display technology for drug discovery
... billions of components with a fast screening or selection procedure [3-8]. One of the most widely used library methods is based on the use of filamentous phages, which seems to play an increasingly important role in the future of drug discovery [1,2,9,10]. Phage display was first described more than ...
... billions of components with a fast screening or selection procedure [3-8]. One of the most widely used library methods is based on the use of filamentous phages, which seems to play an increasingly important role in the future of drug discovery [1,2,9,10]. Phage display was first described more than ...
Product Monograph
... No drug-dependence has been reported with the use of leuprolide acetate. Endocrine and Metabolism Changes in Bone Density Decreased bone mineral density can be anticipated with long-term use of an LHRH agonist. Androgen deprivation therapy is associated with increased risks of osteoporosis and skele ...
... No drug-dependence has been reported with the use of leuprolide acetate. Endocrine and Metabolism Changes in Bone Density Decreased bone mineral density can be anticipated with long-term use of an LHRH agonist. Androgen deprivation therapy is associated with increased risks of osteoporosis and skele ...
Overall Research Focus - MD Anderson Cancer Center
... Overall Research Focus Molecular and Preclinical Approaches to Prevention of Colorectal and other Aero-digestive Tract Cancers: Research in my lab is focused on cancer chemoprevention with major goal to design and develop efficacious strategies for clinical prevention of colorectal cancer and other ...
... Overall Research Focus Molecular and Preclinical Approaches to Prevention of Colorectal and other Aero-digestive Tract Cancers: Research in my lab is focused on cancer chemoprevention with major goal to design and develop efficacious strategies for clinical prevention of colorectal cancer and other ...
Salvia divinorum and Salvinorin A: An Update on Pharmacology and
... olism of salvinorin A or of other compounds in the plant that exhibit an antidepressant activity. If salvinorin A is metabolized to an either active or inactive metabolite, then the binding affinity and the pharmacological profile studied in vitro are at jeopardy. A further study evaluated the effec ...
... olism of salvinorin A or of other compounds in the plant that exhibit an antidepressant activity. If salvinorin A is metabolized to an either active or inactive metabolite, then the binding affinity and the pharmacological profile studied in vitro are at jeopardy. A further study evaluated the effec ...
Introduction
... brain is consistent with the ability of cannabinoids to alter pain perception, affect motor function, impair cognition and memory, and stimulate feeding (Hohmann and Herkenham, 2000; Herkenham et al., 1990; Matsuda et al., 1993; Freund et al., 2003). Those actions are effectively inhibited by the CB ...
... brain is consistent with the ability of cannabinoids to alter pain perception, affect motor function, impair cognition and memory, and stimulate feeding (Hohmann and Herkenham, 2000; Herkenham et al., 1990; Matsuda et al., 1993; Freund et al., 2003). Those actions are effectively inhibited by the CB ...
100 Essential Drugs - University of Toledo
... MOA: for antidepressant effect: it may decrease supersensitivity of dopamine receptors, increase acetylcholine, enhance 5-HT activity for depression; for anti-mania effect: it may prevent recycling of phosphoinositides, thereby causing depletion of IP3 and DAG, which diminishes excess catecholamines ...
... MOA: for antidepressant effect: it may decrease supersensitivity of dopamine receptors, increase acetylcholine, enhance 5-HT activity for depression; for anti-mania effect: it may prevent recycling of phosphoinositides, thereby causing depletion of IP3 and DAG, which diminishes excess catecholamines ...
Performance Enhancing Hormone Doping in Sport
... envisaged as a contest based solely on natural endowments and, similarly, some sports once maintained a distinction between amateurs and professionals. The philosophical foundations of the concept of fairness is a deep and complex issue 2,3 where the focus has been mainly on distributive justice. Le ...
... envisaged as a contest based solely on natural endowments and, similarly, some sports once maintained a distinction between amateurs and professionals. The philosophical foundations of the concept of fairness is a deep and complex issue 2,3 where the focus has been mainly on distributive justice. Le ...
DMSO inhibits human platelet activation through cyclooxygenase
... a rare but serious complication observed following DES deployment [30,31]. Furthermore, platelet activation is also a relevant contributing factor in the regulation of tissue factor (TF) expression [7] – the key regulator of the coagulation cascade. In fact, platelets were shown to not only lead to ...
... a rare but serious complication observed following DES deployment [30,31]. Furthermore, platelet activation is also a relevant contributing factor in the regulation of tissue factor (TF) expression [7] – the key regulator of the coagulation cascade. In fact, platelets were shown to not only lead to ...
Corticotropin-Releasing Factor: Physiology, Pharmacology, And
... the mRNA and the second encodes the entire prepro-CRF precursor polypeptide, which is 187 to 196 amino acids long; the carboxy end of the precursor contains the 41amino acid peptide sequence. The high incidence of homology among species suggests that the gene has been highly conserved through evolut ...
... the mRNA and the second encodes the entire prepro-CRF precursor polypeptide, which is 187 to 196 amino acids long; the carboxy end of the precursor contains the 41amino acid peptide sequence. The high incidence of homology among species suggests that the gene has been highly conserved through evolut ...
Decreased Serum Concentrations of Tamoxifen
... converts androgens to estrogens in peripheral fat tissue (3). This conversion is the main estrogen source in postmenopausal women. In addition, aminoglutethimide may reduce the con centration of plasma estrogens by enhancement of estrogen metabolism (10, 11). Aminoglutethimide causes response rates ...
... converts androgens to estrogens in peripheral fat tissue (3). This conversion is the main estrogen source in postmenopausal women. In addition, aminoglutethimide may reduce the con centration of plasma estrogens by enhancement of estrogen metabolism (10, 11). Aminoglutethimide causes response rates ...
38: Opioids
... binding protein (G-protein)–binding receptor superfamily. However, the extracellular and intracellular segments differ from one another. These nonhomologous segments probably represent the ligand binding and signal transduction regions, respectively, which would be expected to differ among the three ...
... binding protein (G-protein)–binding receptor superfamily. However, the extracellular and intracellular segments differ from one another. These nonhomologous segments probably represent the ligand binding and signal transduction regions, respectively, which would be expected to differ among the three ...
IDENTIFICATION OF NATURAL PRODUCTS AS ANTIDIABETIC AGENTS Laura Guasch Pàmies
... 1. Introduction: diabetes – an emerging epidemic of the 21st century Diabetes mellitus (DM) is a metabolic syndrome that constitutes a major health problem [1,2]. It is estimated that 246 million people worldwide have diabetes and that 380 million people will be afflicted with diabetes by 2025. In a ...
... 1. Introduction: diabetes – an emerging epidemic of the 21st century Diabetes mellitus (DM) is a metabolic syndrome that constitutes a major health problem [1,2]. It is estimated that 246 million people worldwide have diabetes and that 380 million people will be afflicted with diabetes by 2025. In a ...
Abstract Ethnopharmacological relevance Achillea millefolium L
... the noncompetitive GABAA receptor antagonist picrotoxin and the BDZ antagonist flumazenil and by [3H]-flunitrazepam binding to the BDZ site on the GABAA receptor. Results Achillea millefolium exerted anxiolytic-like effects in the elevated plus-maze and marble-burying test after acute and chronic (2 ...
... the noncompetitive GABAA receptor antagonist picrotoxin and the BDZ antagonist flumazenil and by [3H]-flunitrazepam binding to the BDZ site on the GABAA receptor. Results Achillea millefolium exerted anxiolytic-like effects in the elevated plus-maze and marble-burying test after acute and chronic (2 ...
The following information was generated from the Hazardous
... temporarily, since these are signs of excessive dosage; if therapy with testosterone is reinstituted, a lower dosage should be used. [McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplemen ...
... temporarily, since these are signs of excessive dosage; if therapy with testosterone is reinstituted, a lower dosage should be used. [McEvoy, G.K. (ed.). American Hospital Formulary Service- Drug Information 2005. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2005 (Plus Supplemen ...
Antidote–Opioids
... Pure opioid antagonists produce no clinical effects in opioid-naïve or nondependent patients even when administered in massive doses.7 When patients dependent on opioid agonists are exposed to opioid antagonists or agonist– antagonists such as pentazocine, they exhibit opioid withdrawal, including ...
... Pure opioid antagonists produce no clinical effects in opioid-naïve or nondependent patients even when administered in massive doses.7 When patients dependent on opioid agonists are exposed to opioid antagonists or agonist– antagonists such as pentazocine, they exhibit opioid withdrawal, including ...
Recent advances in the use of metformin: Can treating diabetes... cancer? Diana Hatoum
... glycolysis is generally accepted. Metformin acts by interfering with cellular processes that facilitate insulin signalling and glucose synthesis. Some of these proposed signalling pathways are described in this section and illustrated in Figure 1. There is a general consensus that the organic cation ...
... glycolysis is generally accepted. Metformin acts by interfering with cellular processes that facilitate insulin signalling and glucose synthesis. Some of these proposed signalling pathways are described in this section and illustrated in Figure 1. There is a general consensus that the organic cation ...
Prostate Cancer - European Association of Urology
... oncologist, a radiologist and a pathologist. ...
... oncologist, a radiologist and a pathologist. ...
Discovery and development of antiandrogens
In the 1960s, the first antiandrogen, or androgen antagonist, was discovered. Antiandrogens antagonise the androgen receptor (AR) and thereby block the biological effects of testosterone and dihydrotestosterone (DHT). Antiandrogens are important for men with hormonally responsive diseases like prostate cancer, benign prostatic hyperplasia (BHP), acne, seborrhea, hirsutism and androgen alopecia. Antiandrogens are mainly used for the treatment of prostate diseases. Research from 2010 suggests that ARs could be linked to the disease progression of triple-negative breast cancer and that antiandrogens can potentially be used to treat it.As of 2010 antiandrogens are small molecules and can be either steroidal or nonsteroidal depending on ligand chemistry. Steroidal antiandrogens share a similar steroid structure, while nonsteroidal antiandrogens may have structurally distinctive pharmacophores. Only a limited number of compounds are available for clinical use despite the fact that a very large variety of antiandrogen compounds have been discovered and researched.