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Sodium–Glucose Cotransporter Inhibitors: Effects
... SGLT2 inhibitors with improved properties. The first publication demonstrating the potential of a selective SGLT2 inhibitor (T-1095) as a treatment for diabetes in rodent models appeared in 1999 (26). Since then, several SGLT2 inhibitors have been developed and three compounds are currently approved ...
... SGLT2 inhibitors with improved properties. The first publication demonstrating the potential of a selective SGLT2 inhibitor (T-1095) as a treatment for diabetes in rodent models appeared in 1999 (26). Since then, several SGLT2 inhibitors have been developed and three compounds are currently approved ...
Studies of the Biogenic Amine Transporters. 12. Identification of
... allosterically modulated the ability of citalopram to inhibit [3H]5-hydroxytryptamine transport. Others reported apparent allosteric interactions between 5-hydroxytryptamine and [3H]paroxetine binding to human platelet SERT (Andersson and Marcusson, 1989) and between -estradiol and SERT (Chang and ...
... allosterically modulated the ability of citalopram to inhibit [3H]5-hydroxytryptamine transport. Others reported apparent allosteric interactions between 5-hydroxytryptamine and [3H]paroxetine binding to human platelet SERT (Andersson and Marcusson, 1989) and between -estradiol and SERT (Chang and ...
Activity of Argyreia speciosa and Acorus calamus
... Central nervous system (CNS) is vital organ system. Hence, the drugs acting on the CNS are very important by both perspective i.e. their effects and adverse effects. Drugs acting in the central nervous system (CNS) were among the first to be discovered by primitive humans and are still the most wide ...
... Central nervous system (CNS) is vital organ system. Hence, the drugs acting on the CNS are very important by both perspective i.e. their effects and adverse effects. Drugs acting in the central nervous system (CNS) were among the first to be discovered by primitive humans and are still the most wide ...
2,5-Dimethoxy-4-methylphenyl
... Examining a series of ketanserin analogues, we previously reported that 4-fluorobenzoylpiperidinesbind at 5-HT2 sites with high affinity; for example, 11 binds with aKi value of 4 nM.6 Incorporation of this carbonyl moiety into anilino analogue 9 had little effect on affinity (12; Ki = 70 nM) but re ...
... Examining a series of ketanserin analogues, we previously reported that 4-fluorobenzoylpiperidinesbind at 5-HT2 sites with high affinity; for example, 11 binds with aKi value of 4 nM.6 Incorporation of this carbonyl moiety into anilino analogue 9 had little effect on affinity (12; Ki = 70 nM) but re ...
Macrolids
... (usually containing 14 or 16 atoms) to which deoxy sugars are attached. The prototype drug, erythromycin, which consists of two sugar moieties attached to a 14-atom lactone ring, was obtained in 1952 from Streptomyces erythreus. Clarithromycin and azithromycin are semisynthetic derivatives of erythr ...
... (usually containing 14 or 16 atoms) to which deoxy sugars are attached. The prototype drug, erythromycin, which consists of two sugar moieties attached to a 14-atom lactone ring, was obtained in 1952 from Streptomyces erythreus. Clarithromycin and azithromycin are semisynthetic derivatives of erythr ...
New Approaches to Chronic Anticoagulation
... • Rivaroxaban did not affect ECG parameters • Rivaroxaban did not have any substance-specific effects on laboratory parameters (except for clotting tests) • LFT increases with BAY 597939 did not exceed the level observed with enoxaparin – There was no dose-dependent increase in transaminase levels ...
... • Rivaroxaban did not affect ECG parameters • Rivaroxaban did not have any substance-specific effects on laboratory parameters (except for clotting tests) • LFT increases with BAY 597939 did not exceed the level observed with enoxaparin – There was no dose-dependent increase in transaminase levels ...
Management of PUD, H. pylori infection
... -Little interference with cytochrome P450 -Reversible drug-induced hepatitis with all H2-antagonists ...
... -Little interference with cytochrome P450 -Reversible drug-induced hepatitis with all H2-antagonists ...
1158-1161 Lovelyn Joseph 317 - International Journal of Bioassays
... with more than one possible mechanism of action. The interaction could be pharmacokinetic or pharmacodynamic. Large scale studies at various dose ratios and with more parameters including the adverse effect profile of the combination at preclinical and clinical level are required to explore potentia ...
... with more than one possible mechanism of action. The interaction could be pharmacokinetic or pharmacodynamic. Large scale studies at various dose ratios and with more parameters including the adverse effect profile of the combination at preclinical and clinical level are required to explore potentia ...
General - EmergencyPedia
... 11. Heparin induced mild thrombocytopenia is caused by – glycosaminoglycan produced by macrophages and mast cells a. ...
... 11. Heparin induced mild thrombocytopenia is caused by – glycosaminoglycan produced by macrophages and mast cells a. ...
Medical University of Lodz USE OF DENDRIMERS IN THE
... thrombin. From the point of view of systemic administration, examined compounds could be regarded safe when considering hemostasis system because for the potential average circulating plasma concentration I did not report any statistically important changes in kinetic parameters of the process of cl ...
... thrombin. From the point of view of systemic administration, examined compounds could be regarded safe when considering hemostasis system because for the potential average circulating plasma concentration I did not report any statistically important changes in kinetic parameters of the process of cl ...
Current Perspectives on Pharmacotherapy Treatments for Erectile
... injected subcutaneously, to initiate potent erections in men with nonorganic ED [35-36]. PT141 is a synthetic cyclic nonselective melanocortin receptor agonist, with a high affinity to MC receptors 1, 3, and 4, and it is believed to be a metabolite of melanotan-II (MT-II) [36]. Theoretically, MC rec ...
... injected subcutaneously, to initiate potent erections in men with nonorganic ED [35-36]. PT141 is a synthetic cyclic nonselective melanocortin receptor agonist, with a high affinity to MC receptors 1, 3, and 4, and it is believed to be a metabolite of melanotan-II (MT-II) [36]. Theoretically, MC rec ...
NIH Public Access - The Scripps Research Institute
... coupled receptors CB1 and CB2. Two endocannabinoids have been identified in mammals, N-arachidonoyl ethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG) (Figure 1), and the biological actions of these signaling lipids are terminated by enzymatic hydrolysis (1-4). Two principal enzymes th ...
... coupled receptors CB1 and CB2. Two endocannabinoids have been identified in mammals, N-arachidonoyl ethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG) (Figure 1), and the biological actions of these signaling lipids are terminated by enzymatic hydrolysis (1-4). Two principal enzymes th ...
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, KARNATAKA
... plant (Withaferin A, Sitoindosides VII- X) are reported to have antioxidant activity which may contribute atleast in part to the reported antistress, immunomodulatory, cognition facilitating, antiinflammatory and antiageing properties. WS is reported to modulate GABAergic [γ-aminobutyric acid (GABA) ...
... plant (Withaferin A, Sitoindosides VII- X) are reported to have antioxidant activity which may contribute atleast in part to the reported antistress, immunomodulatory, cognition facilitating, antiinflammatory and antiageing properties. WS is reported to modulate GABAergic [γ-aminobutyric acid (GABA) ...
The Design and Synthesis of Novel Antimicrobial Agents for Use in
... Domagk in 1935.1-3 Prontosil was later found to be a prodrug that was metabolized in vivo to its active metabolite sulfanilamide (Figure 1.1).4 Prontosil was the first of the “sulfa” drugs discovered, and its discovery ushered in the era of antibiotics. Antibacterial agents, or antibiotics, are a cl ...
... Domagk in 1935.1-3 Prontosil was later found to be a prodrug that was metabolized in vivo to its active metabolite sulfanilamide (Figure 1.1).4 Prontosil was the first of the “sulfa” drugs discovered, and its discovery ushered in the era of antibiotics. Antibacterial agents, or antibiotics, are a cl ...
C 2 R
... contains a heme and reductase domain fused in a single polypeptide, which might explain why this enzyme has the highest activity ever reported for a P450 (1, 2). By using sitedirected and/or random mutagenesis, several research groups have succeeded in broadening the substrate selectivity of this en ...
... contains a heme and reductase domain fused in a single polypeptide, which might explain why this enzyme has the highest activity ever reported for a P450 (1, 2). By using sitedirected and/or random mutagenesis, several research groups have succeeded in broadening the substrate selectivity of this en ...
Atorvastatin
... -------------------------------------------------------------------------------Description: Atorvastatin is a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is primarily used to lower cholesterol and triglycerides in patients with hypercholesterolemia and mixed dyslipidemia. At the ...
... -------------------------------------------------------------------------------Description: Atorvastatin is a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is primarily used to lower cholesterol and triglycerides in patients with hypercholesterolemia and mixed dyslipidemia. At the ...
Cough and Angioedema in Patients Receiving Angiotensin
... free periods of 2 weeks to 3 months. In another series published in the same year, the same authors reported that more than 50% of patients developed complete disappearance of symptoms despite continuing with treatment. (18) However, no other studies focused on this finding of continuation of ACEIs, ...
... free periods of 2 weeks to 3 months. In another series published in the same year, the same authors reported that more than 50% of patients developed complete disappearance of symptoms despite continuing with treatment. (18) However, no other studies focused on this finding of continuation of ACEIs, ...
Introduction to Fragment-Based Drug Discovery
... inactivate proteins. Examples of these types of compounds are shown in Fig. 2: all of them are small, fragment-like molecules. Molecule 1 and molecules 2 and 3 were all reported to inhibit PTP1B by generating hydrogen peroxide in the presence of buffers containing reducing agents, a common and gener ...
... inactivate proteins. Examples of these types of compounds are shown in Fig. 2: all of them are small, fragment-like molecules. Molecule 1 and molecules 2 and 3 were all reported to inhibit PTP1B by generating hydrogen peroxide in the presence of buffers containing reducing agents, a common and gener ...
In vivo and in vitro studies on drug metabolism and
... CYP2C19 (1%) are the minor isoforms (Ged et al. 1988, Romkes et al. 1991). CYP2C9 exhibits genetic polymorphism (Miners & Birkett 1998). Individual homozygous for the Leu359 allele are associated with PM of CYP2C9. Approximately 1% of individuals in Caucasian populations are the PM phenotype (Vermei ...
... CYP2C19 (1%) are the minor isoforms (Ged et al. 1988, Romkes et al. 1991). CYP2C9 exhibits genetic polymorphism (Miners & Birkett 1998). Individual homozygous for the Leu359 allele are associated with PM of CYP2C9. Approximately 1% of individuals in Caucasian populations are the PM phenotype (Vermei ...
C 5 P450
... been applied to identify inhibitors in mixtures which were generated by on-line electrochemical conversion of commercially available p38-inhibitors (23). However, although electrochemistry in some cases has been shown to produce human-relevant oxidation products, it cannot mimic all P450-dependent ...
... been applied to identify inhibitors in mixtures which were generated by on-line electrochemical conversion of commercially available p38-inhibitors (23). However, although electrochemistry in some cases has been shown to produce human-relevant oxidation products, it cannot mimic all P450-dependent ...
Front Matter
... proportion as in natural milk. This artificial milk did not improve survival rates, yet the mice thrived on powdered natural milk. This led Lunin to conclude that milk must contain unknown substances essential for growth and the maintenance of good health.1 Soon after publishing his results, Lunin l ...
... proportion as in natural milk. This artificial milk did not improve survival rates, yet the mice thrived on powdered natural milk. This led Lunin to conclude that milk must contain unknown substances essential for growth and the maintenance of good health.1 Soon after publishing his results, Lunin l ...
INTRODUCTION: - PharmaStreet
... A . As an alternative to penicillin 1. Streptococcal pharyngitis, tonsillitis, mastoiditis and community acquired respiratory infections caused by pneumococci and H. influenzae respond equally well to erythromycin. • It is an alternative drug for prophylaxis of rheumatic fever and SABE. 2. Diphtheri ...
... A . As an alternative to penicillin 1. Streptococcal pharyngitis, tonsillitis, mastoiditis and community acquired respiratory infections caused by pneumococci and H. influenzae respond equally well to erythromycin. • It is an alternative drug for prophylaxis of rheumatic fever and SABE. 2. Diphtheri ...
Structure and mechanism of inhibition of plant
... The structures of the catalytic subunit from yeast [40,48,51] and A. thaliana [41] have been determined. Discussion of these is deferred until Section 3. The first regulatory subunit structure to be published [26] (PDB code 2F1F) was for one of the three isoenzymes (AHASIII) found in E. coli. The pr ...
... The structures of the catalytic subunit from yeast [40,48,51] and A. thaliana [41] have been determined. Discussion of these is deferred until Section 3. The first regulatory subunit structure to be published [26] (PDB code 2F1F) was for one of the three isoenzymes (AHASIII) found in E. coli. The pr ...
Mass versus molar doses, similarities and
... Fibrates belong chemically to the group of amphipathic carboxylic acids, which are antagonists of peroxisome proliferator-activated receptor (PPAR-alpha). Pharmacologically, fibrates belongs to of lipid-modifying agents. Treatment with fibrates results in a substantial decrease in plasma levels of t ...
... Fibrates belong chemically to the group of amphipathic carboxylic acids, which are antagonists of peroxisome proliferator-activated receptor (PPAR-alpha). Pharmacologically, fibrates belongs to of lipid-modifying agents. Treatment with fibrates results in a substantial decrease in plasma levels of t ...
Psychotropic Medications Metabolized by Cytochromes P450 (CYP
... widest range of drugs, such as beta blockers, antidepressants, and opioids. They are found mainly in liver, small intestine, lungs, kidneys, placenta and Consists of more than 50 isoforms. Cytochromes P450 (CYPs) are major source of catalytic activity for drug oxidation [1-3]. CYP2D6 is a member of ...
... widest range of drugs, such as beta blockers, antidepressants, and opioids. They are found mainly in liver, small intestine, lungs, kidneys, placenta and Consists of more than 50 isoforms. Cytochromes P450 (CYPs) are major source of catalytic activity for drug oxidation [1-3]. CYP2D6 is a member of ...