Behavioural and neurochemical changes induced by stress
... (BDNF), and also affect HPA axis hyperactivity (Duman et al. 1999 ; Kunugi et al. 2010 ; Luo et al. 2004 ; Malberg et al. 2000 ; Nibuya et al. 1996 ; Xu et al. 2003). Hence, the long-term beneficial effects of antidepressant treatment could partially be related to their delayed effect on synaptic plasti ...
... (BDNF), and also affect HPA axis hyperactivity (Duman et al. 1999 ; Kunugi et al. 2010 ; Luo et al. 2004 ; Malberg et al. 2000 ; Nibuya et al. 1996 ; Xu et al. 2003). Hence, the long-term beneficial effects of antidepressant treatment could partially be related to their delayed effect on synaptic plasti ...
Acute Effects of d-Amphetamine on the Differential Reinforcement of
... the IRT frequency distribution. For instance, the IRT data reported by two previous studies (3, 27) were categorized into a bin with a longer duration (3 s) instead of a shorter one, and no detailed information was presented for the frequencies of the IRTs beyond the reinforced bin. Thus, it was dif ...
... the IRT frequency distribution. For instance, the IRT data reported by two previous studies (3, 27) were categorized into a bin with a longer duration (3 s) instead of a shorter one, and no detailed information was presented for the frequencies of the IRTs beyond the reinforced bin. Thus, it was dif ...
Kinetic analysis of drug-target interactions with
... to estimate the affinity of labeled compounds, for example, CFT,4 fallypride,5 and fluorocarazolol.6 Further, if a reference region devoid of specific target sites exists, the pseudoequilibrium method or multiple ligand concentration receptor assay can be applied using different SA injections, allow ...
... to estimate the affinity of labeled compounds, for example, CFT,4 fallypride,5 and fluorocarazolol.6 Further, if a reference region devoid of specific target sites exists, the pseudoequilibrium method or multiple ligand concentration receptor assay can be applied using different SA injections, allow ...
Fatty acid amide hydrolase - The Scripps Research Institute
... regions of the nervous system under persistent stimulation. In disorders such as inflammatory or chronic pain, which are typically associated with hyperexicitability in damaged neural pathways [35], FAAH inhibition might increase endocannabinoid tone selectively in these circuits, resulting in analg ...
... regions of the nervous system under persistent stimulation. In disorders such as inflammatory or chronic pain, which are typically associated with hyperexicitability in damaged neural pathways [35], FAAH inhibition might increase endocannabinoid tone selectively in these circuits, resulting in analg ...
Phase 3 Efficacy and Safety Trials
... All investigators and/or their institutions received research grant support from King Pharmaceuticals R&D Drs. Barrett and Pixton are employees of King Pharmaceuticals R&D ...
... All investigators and/or their institutions received research grant support from King Pharmaceuticals R&D Drs. Barrett and Pixton are employees of King Pharmaceuticals R&D ...
Psychiatric Meds and Opiates
... schizophrenia, organic mental disorders, anxiety disorders, mixed anxiety depressive illness, and anxiety-agitation accompanying dementia. ► They are dopamine antagonists to varying degrees: – most neuroleptics efficacy related to affinity for the D2 receptor in mesolimbic system and basal ganglia – ...
... schizophrenia, organic mental disorders, anxiety disorders, mixed anxiety depressive illness, and anxiety-agitation accompanying dementia. ► They are dopamine antagonists to varying degrees: – most neuroleptics efficacy related to affinity for the D2 receptor in mesolimbic system and basal ganglia – ...
Advanced Medicinal Chemistry
... Also known as the “Me-Too” or “Me-Better” Approach Pfizer Issues: short duration ...
... Also known as the “Me-Too” or “Me-Better” Approach Pfizer Issues: short duration ...
Fragment-Based Drug Discovery Applied to Hsp90
... conformational stability, maturation, and function of other substrate proteins, which are known as clients.1 Heat shock protein 90 (Hsp90a) is a molecular chaperone, and many of its clients are oncology targets that are known to play critical roles in cancer progression.2,3 In fact it has been argue ...
... conformational stability, maturation, and function of other substrate proteins, which are known as clients.1 Heat shock protein 90 (Hsp90a) is a molecular chaperone, and many of its clients are oncology targets that are known to play critical roles in cancer progression.2,3 In fact it has been argue ...
Chapter 34 Antihypertension Drugs
... the patient, the severity of organ damage (if any) due to high blood pressure, and the presence of cardiovascular risk factors must all be considered. ------Begin the drug treatment or not. ...
... the patient, the severity of organ damage (if any) due to high blood pressure, and the presence of cardiovascular risk factors must all be considered. ------Begin the drug treatment or not. ...
april11
... regimens not proven; unproven which exposure parameter best predicts pharmacological response 8. Measure faecal sterol excretion in clinical study Effects on reverse cholesterol transport in humans have not been proven ...
... regimens not proven; unproven which exposure parameter best predicts pharmacological response 8. Measure faecal sterol excretion in clinical study Effects on reverse cholesterol transport in humans have not been proven ...
HERE - INDIGO Biosciences
... a number of different nuclear receptors; docking analysis confirmed a theoretical ability for diclofenac and celecoxib but not naproxen to bind to TRβ. Key findings: Results from TRβ luciferase reporter assays confirmed that both diclofenac and celecoxib display TRβ antagonistic properties; celecoxib, ...
... a number of different nuclear receptors; docking analysis confirmed a theoretical ability for diclofenac and celecoxib but not naproxen to bind to TRβ. Key findings: Results from TRβ luciferase reporter assays confirmed that both diclofenac and celecoxib display TRβ antagonistic properties; celecoxib, ...
use of a reporter gene assay to predict and rank the potency and
... in the rat CYP3A4 ortholog CYP3A23 (Quattrochi et al., 1995; Huss et al., 1996). Later experiments identified a novel nuclear receptor, the human pregnane X receptor (hPXR), which bound to both ER6 and DR3 motifs (Lehmann et al., 1998). Such motifs are present at approximately ⫺150 bp and also as an ...
... in the rat CYP3A4 ortholog CYP3A23 (Quattrochi et al., 1995; Huss et al., 1996). Later experiments identified a novel nuclear receptor, the human pregnane X receptor (hPXR), which bound to both ER6 and DR3 motifs (Lehmann et al., 1998). Such motifs are present at approximately ⫺150 bp and also as an ...
9-Methyl-7-Bromoeudistomin D, a Caffeine Like
... had no effect on this binding (fig.5). These results suggest that in rat liver microsomes, 3H-MBED probably binds to CYP1A1 and CYP2B. We have previously reported that caffeine can allosterically inhibit 3H-MBED binding to rabbit liver microsomes and that the 3H-MBED binding site is distinct from bu ...
... had no effect on this binding (fig.5). These results suggest that in rat liver microsomes, 3H-MBED probably binds to CYP1A1 and CYP2B. We have previously reported that caffeine can allosterically inhibit 3H-MBED binding to rabbit liver microsomes and that the 3H-MBED binding site is distinct from bu ...
1) Lead compound discovery
... out-of-pocket for expensive sleep medication, the patent for Ambien expired on April 21, 2007, following a 6-month patent extension. Manufactured by sanofi-aventis Group, which includes U.S. subsidiary Aventis Pharmacuticals, Inc., Ambien was ranked the 13th most popular brand name drug in terms of ...
... out-of-pocket for expensive sleep medication, the patent for Ambien expired on April 21, 2007, following a 6-month patent extension. Manufactured by sanofi-aventis Group, which includes U.S. subsidiary Aventis Pharmacuticals, Inc., Ambien was ranked the 13th most popular brand name drug in terms of ...
Targeted erythropoietin selectively stimulates red blood cell
... The design of cell-targeted protein therapeutics can be informed by natural protein–protein interactions that use cooperative physical contacts to achieve cell type specificity. Here we applied this approach in vivo to the anemia drug erythropoietin (EPO), to direct its activity to EPO receptors (EP ...
... The design of cell-targeted protein therapeutics can be informed by natural protein–protein interactions that use cooperative physical contacts to achieve cell type specificity. Here we applied this approach in vivo to the anemia drug erythropoietin (EPO), to direct its activity to EPO receptors (EP ...
Chapter 15
... An ionic bond is an attraction between oppositely charged ions. Compounds that contain ionic bonds are called ionic compounds. Ionic compounds are: ...
... An ionic bond is an attraction between oppositely charged ions. Compounds that contain ionic bonds are called ionic compounds. Ionic compounds are: ...
Inhibitors of transglutaminase 2: A therapeutic option in
... residues in peptides. Amongst others, the enzyme is involved in the pathogenesis of celiac disease, a T-cell mediated inflammatory disorder of the small intestine. Here, gluten peptides are the environmental factors required for disease activation in genetically predisposed individuals. TG2 deamidat ...
... residues in peptides. Amongst others, the enzyme is involved in the pathogenesis of celiac disease, a T-cell mediated inflammatory disorder of the small intestine. Here, gluten peptides are the environmental factors required for disease activation in genetically predisposed individuals. TG2 deamidat ...
Antipsychotic Drugs - Pharmacological Reviews
... shows that the selectivity is low and had been overestimated previously owing to overestimation of the Ki at the D2 receptor when determined in competition versus [3H]spiperone. Problems with the use of high-affinity ligands can also be seen in the in vivo scanning techniques. For example, some of t ...
... shows that the selectivity is low and had been overestimated previously owing to overestimation of the Ki at the D2 receptor when determined in competition versus [3H]spiperone. Problems with the use of high-affinity ligands can also be seen in the in vivo scanning techniques. For example, some of t ...
Reward Processing by the Opioid System in the Brain
... opiate addiction represents a major public health issue (for review, see Ref. 394). The existence of opioid binding sites in the brain was established in 1973, and these were later referred as to mu, delta, and kappa opioid receptors. In 1975, two pentapeptides, Met- and Leu-enkephalin, were charact ...
... opiate addiction represents a major public health issue (for review, see Ref. 394). The existence of opioid binding sites in the brain was established in 1973, and these were later referred as to mu, delta, and kappa opioid receptors. In 1975, two pentapeptides, Met- and Leu-enkephalin, were charact ...
Biomarkers and surrogate endpoints: How and when might they
... In vitro screening usually includes some type of binding to a specific receptor or cell surface proteins. Subsequently, these candidates are usually evaluated for their activity in preclinical in vivo models of efficacy and simultaneously evaluated for their pharmacokinetic and formulation propertie ...
... In vitro screening usually includes some type of binding to a specific receptor or cell surface proteins. Subsequently, these candidates are usually evaluated for their activity in preclinical in vivo models of efficacy and simultaneously evaluated for their pharmacokinetic and formulation propertie ...
5-meo-dmt.5ht1a.para..
... The observed blockade of the stimulus effects of DOM, LSD, and mescaline by 5-HT antagonists that were considered relatively selective for the 5-HT2 receptor subtype led Glennon and colleagues to hypothesize that classical hallucinogens act as 5-HT2 agonists (14,17,18,30). Subsequently, the close co ...
... The observed blockade of the stimulus effects of DOM, LSD, and mescaline by 5-HT antagonists that were considered relatively selective for the 5-HT2 receptor subtype led Glennon and colleagues to hypothesize that classical hallucinogens act as 5-HT2 agonists (14,17,18,30). Subsequently, the close co ...
Provisional PDF - Malaria Journal
... mean elimination half-life of NP046 following oral administration was 4.4 hours and 3.1 hours for the 50 mg/kg and 10 mg/kg doses, respectively, while for the IV route it was 3.2 hours, indicating a moderate elimination half-life. The compound has a very high volume of distribution (16.9 L/kg), indi ...
... mean elimination half-life of NP046 following oral administration was 4.4 hours and 3.1 hours for the 50 mg/kg and 10 mg/kg doses, respectively, while for the IV route it was 3.2 hours, indicating a moderate elimination half-life. The compound has a very high volume of distribution (16.9 L/kg), indi ...
Back_to_basics_pharmacology 1, 2 and 3 2011
... All opioids have the same basic side effects: – euphoria – constipation – N&V – somnolence – respiratory depression (especially important if patient is not awake) – potential for addiction – hypotension – skin itchiness – seizures ...
... All opioids have the same basic side effects: – euphoria – constipation – N&V – somnolence – respiratory depression (especially important if patient is not awake) – potential for addiction – hypotension – skin itchiness – seizures ...