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Energy Homeostasis and Cancer Prevention: The AMP
... (49). Although metformin is an insulin sensitizer in glucose responsive cells (e.g., liver, muscle), it suppresses insulinand insulin-like growth factor-I (IGF-I)–stimulated growth of human breast cancer cells. AMPKα1 siRNA rescues cells from the antiproliferative actions of the drug, confirming tha ...
... (49). Although metformin is an insulin sensitizer in glucose responsive cells (e.g., liver, muscle), it suppresses insulinand insulin-like growth factor-I (IGF-I)–stimulated growth of human breast cancer cells. AMPKα1 siRNA rescues cells from the antiproliferative actions of the drug, confirming tha ...
Vinca Alkaloids
... vinca alkaloid, vinflunine that is currently approved in Europe for medicinal treatment.[5,6] ...
... vinca alkaloid, vinflunine that is currently approved in Europe for medicinal treatment.[5,6] ...
Facilitative effects of an adenosine A1/A2 receptor blockade on
... an 8-arm radial maze task which requires the integrity of the hippocampal formation. We investigated the effects of the unselective adenosine A1/A2 receptor antagonist theophylline on acquisition and retention of spatial working and reference memory. As there is evidence that brain extracellular ade ...
... an 8-arm radial maze task which requires the integrity of the hippocampal formation. We investigated the effects of the unselective adenosine A1/A2 receptor antagonist theophylline on acquisition and retention of spatial working and reference memory. As there is evidence that brain extracellular ade ...
IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS)
... extract was also subjected to column chromatography to obtain four fractions, these fractions were preliminary tested for antiplasmodial potency and methanol fraction which gave the most potent effect was fully evaluated and was refractionated to obtain the phenolic compounds. Phytochemical test, Th ...
... extract was also subjected to column chromatography to obtain four fractions, these fractions were preliminary tested for antiplasmodial potency and methanol fraction which gave the most potent effect was fully evaluated and was refractionated to obtain the phenolic compounds. Phytochemical test, Th ...
Muscarinic antagonist
... to cross the blood-brain barrier. At higher than therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. Hyoscine has anti-emetic activity, so is used for motion sickness. Antimuscarinics are also used as anti-park ...
... to cross the blood-brain barrier. At higher than therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. Hyoscine has anti-emetic activity, so is used for motion sickness. Antimuscarinics are also used as anti-park ...
Atropine
... to cross the blood-brain barrier. At higher than therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. Hyoscine has anti-emetic activity, so is used for motion sickness. Antimuscarinics are also used as anti-park ...
... to cross the blood-brain barrier. At higher than therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. Hyoscine has anti-emetic activity, so is used for motion sickness. Antimuscarinics are also used as anti-park ...
Intravenous Agents - RAH
... reversibly to albumin, high protein binding ~ 75-85% therefore the free fraction varies from 0.15 to 0.25 steady state VdSS ~ 1.7-2.5 l/kg, is greater than body volume, reflecting extensive tissue uptake the combination of low clearance and large volume of distribution results in the relatively long ...
... reversibly to albumin, high protein binding ~ 75-85% therefore the free fraction varies from 0.15 to 0.25 steady state VdSS ~ 1.7-2.5 l/kg, is greater than body volume, reflecting extensive tissue uptake the combination of low clearance and large volume of distribution results in the relatively long ...
Curr.Med. Chem._Martínez, A._2015 - digital
... different chemical features: a known and small AChE inhibitor to interact with the catalytic site, a linker of different length and nature located along the gorge of the enzyme, and a chemical framework able to interact efficiently in the peripheral site, mainly with the Trp 279 (Fig. 3). Common fra ...
... different chemical features: a known and small AChE inhibitor to interact with the catalytic site, a linker of different length and nature located along the gorge of the enzyme, and a chemical framework able to interact efficiently in the peripheral site, mainly with the Trp 279 (Fig. 3). Common fra ...
Morphine
... Primary effect on CNS, eliminate or ease pain selectively, to lessen the nervous of patients, these agents relieve pain without producing a loss of consciousness. They are used primarily to relieve acute and chronicity pain of any origin. ...
... Primary effect on CNS, eliminate or ease pain selectively, to lessen the nervous of patients, these agents relieve pain without producing a loss of consciousness. They are used primarily to relieve acute and chronicity pain of any origin. ...
Serotonergic Modulation of Rat Pineal Gland Activity: In Vivo
... higher affinity for the 5-HT2B/C than for 5-HT2A receptor (Kennett et al., 1994). To this purpose, 36 rats (weighing 200 –250 g) were used. At 9:15 PM, in dark conditions, rats were divided in three groups (12 animals each): one group received orally 20 mg/kg SB 200646A in a 2-ml/kg volume, one grou ...
... higher affinity for the 5-HT2B/C than for 5-HT2A receptor (Kennett et al., 1994). To this purpose, 36 rats (weighing 200 –250 g) were used. At 9:15 PM, in dark conditions, rats were divided in three groups (12 animals each): one group received orally 20 mg/kg SB 200646A in a 2-ml/kg volume, one grou ...
patrick_tb_ch21
... Feedback: Normorphine is the name of the compound. The prefix 'nor' is often used to indicate the absence of a methyl group from the parent compound. Noradrenaline is another example of this terminology. The names given in the other options are fictitious. Page reference: 623 a. Desmorphine b. Demet ...
... Feedback: Normorphine is the name of the compound. The prefix 'nor' is often used to indicate the absence of a methyl group from the parent compound. Noradrenaline is another example of this terminology. The names given in the other options are fictitious. Page reference: 623 a. Desmorphine b. Demet ...
The Midlands Prostate Cancer Study - Faculty of Medical and Health
... For New Zealand men, prostate cancer is the most commonly registered cancer. Māori men are less likely to be diagnosed with prostate cancer, but when diagnosed they are twice as likely to die. Prostate specific antigen (PSA) testing is commonly carried out in New Zealand with approximately 80% of te ...
... For New Zealand men, prostate cancer is the most commonly registered cancer. Māori men are less likely to be diagnosed with prostate cancer, but when diagnosed they are twice as likely to die. Prostate specific antigen (PSA) testing is commonly carried out in New Zealand with approximately 80% of te ...
Inhibition of platelet aggregability by losartan in essential hypertension
... mediating the antithrombotic effects of the Ang II antago-nist remains to be determined. Thrombin may trigger platelet aggregability by a direct action on platelets 21 or by increased release of TxA27, 22. Losartan may have prevented binding of Ang II to platelets, thus preventing thrombin release. ...
... mediating the antithrombotic effects of the Ang II antago-nist remains to be determined. Thrombin may trigger platelet aggregability by a direct action on platelets 21 or by increased release of TxA27, 22. Losartan may have prevented binding of Ang II to platelets, thus preventing thrombin release. ...
Bisgaier 1998
... HepG2 cells, and chimeric receptor studies in kidney 293 cells suggest that PD 72953 is a ligand for the peroxisomal proliferation activated receptor alpha (PPARa), and PPARg. Overall, PD 72953 may act through a peroxisomal proliferation activated receptor and result in plasma triglycerides and apoB ...
... HepG2 cells, and chimeric receptor studies in kidney 293 cells suggest that PD 72953 is a ligand for the peroxisomal proliferation activated receptor alpha (PPARa), and PPARg. Overall, PD 72953 may act through a peroxisomal proliferation activated receptor and result in plasma triglycerides and apoB ...
Structure- Activity Relationships (SAR)
... • Most drugs act at a specific site such as an enzyme or receptor. Compounds with similar structures often tend to have similar pharmacological activity. However, they usually exhibit difference in potency and unwanted side effects and in some cases different activities. These structurally related d ...
... • Most drugs act at a specific site such as an enzyme or receptor. Compounds with similar structures often tend to have similar pharmacological activity. However, they usually exhibit difference in potency and unwanted side effects and in some cases different activities. These structurally related d ...
Inhibitors of transglutaminase 2: A therapeutic option in
... Escherichia coli cells producing recombinant TG2 were centrifuged at 3,700 rpm for 20 min after an induction period of 20 hours at 20°C. The pellet was resuspended in buffer and lysed by high pressure homogenization. After centrifugation, the supernatant was applied to a column containing Ni-NTA res ...
... Escherichia coli cells producing recombinant TG2 were centrifuged at 3,700 rpm for 20 min after an induction period of 20 hours at 20°C. The pellet was resuspended in buffer and lysed by high pressure homogenization. After centrifugation, the supernatant was applied to a column containing Ni-NTA res ...
2048998_Open_OCTREOTIDE ACETATE INJECTION SAG US.cdr
... acetate is variable but extends up to 12 hours depending upon the type of tumor. About 32% of the dose is excreted unchanged into the urine. In an elderly population, dose adjustments may be necessary due to a significant increase in the half-life (46%) and a significant decrease in the clearance (2 ...
... acetate is variable but extends up to 12 hours depending upon the type of tumor. About 32% of the dose is excreted unchanged into the urine. In an elderly population, dose adjustments may be necessary due to a significant increase in the half-life (46%) and a significant decrease in the clearance (2 ...
HERE - INDIGO Biosciences
... diclofenac and celecoxib could bind to this receptor was further investigated by using the reverse docking platform Pharmmapper. Diclofenac and celecoxib structures were submitted to the webserver and the ability to bind to TRβ was demonstrated as a list of possible protein data bank files in whose a ...
... diclofenac and celecoxib could bind to this receptor was further investigated by using the reverse docking platform Pharmmapper. Diclofenac and celecoxib structures were submitted to the webserver and the ability to bind to TRβ was demonstrated as a list of possible protein data bank files in whose a ...
Saw Palmetto
... to BPH (68, 5). In Germany and Austria, herbal medicines are the firstline treatment more than 90% of the time for patients with early and moderate outflow tract obstruction due to BPH (68). Over 50% of German urologists are reported to prefer herbal medicines to chemically derived agents in the tre ...
... to BPH (68, 5). In Germany and Austria, herbal medicines are the firstline treatment more than 90% of the time for patients with early and moderate outflow tract obstruction due to BPH (68). Over 50% of German urologists are reported to prefer herbal medicines to chemically derived agents in the tre ...
A Rare Adverse Effect of Montelukast Treatment
... Asthma is one of the most prevalent long-term diseases; it affects nearly 300 million people, and there may be 100 million new patients by 2025.1 Allergic rhinitis is also a common disease; it affects 10 – 40% of the population in the United States.2,3 Evidence for the association between allergic r ...
... Asthma is one of the most prevalent long-term diseases; it affects nearly 300 million people, and there may be 100 million new patients by 2025.1 Allergic rhinitis is also a common disease; it affects 10 – 40% of the population in the United States.2,3 Evidence for the association between allergic r ...
Journal of Chemical and Pharmaceutical Research __________________________________________________
... and the side effect profile. Some antihistamines commonly used as vestibular suppressants have significant antiemetic properties (e.g. meclizine). When an oral agent is appropriate, this agent is generally the first to be used, because it rarely causes adverse effects any more severe than drowsiness ...
... and the side effect profile. Some antihistamines commonly used as vestibular suppressants have significant antiemetic properties (e.g. meclizine). When an oral agent is appropriate, this agent is generally the first to be used, because it rarely causes adverse effects any more severe than drowsiness ...
... in the last years. Based on two case reports of apparent dependence (6,23), Kashkin and Kleber (13) proposed the “anabolic steroid addiction hypothesis,” although without support from the scientific research at that time. Soon afterwards, several studies showed that AAS abuse can lead, in some cases ...
Anabolic steroid induced acute myocardial infarction ABSTRACT
... higher than recommended therapeutic dosage, abuse of these drugs is commonly associated with cardiovascular side-effects that can lead to acute myocardial infarction and sudden death. We report here three cases of acute myocardial infarction in local young bodybuilders who were using Stanazolol, an ...
... higher than recommended therapeutic dosage, abuse of these drugs is commonly associated with cardiovascular side-effects that can lead to acute myocardial infarction and sudden death. We report here three cases of acute myocardial infarction in local young bodybuilders who were using Stanazolol, an ...
Anti-Catabolic Effects Of Anabolic Steroids
... oiliness of the skin are anabolic processes in those tissues. The steroids with the most potent anabolic effect are also those with the greatest androgenic effect. Steroid Receptors Steroid hormones work by stimulation of receptor molecules in muscle cells, which activate specific genes to produce p ...
... oiliness of the skin are anabolic processes in those tissues. The steroids with the most potent anabolic effect are also those with the greatest androgenic effect. Steroid Receptors Steroid hormones work by stimulation of receptor molecules in muscle cells, which activate specific genes to produce p ...
Discovery and development of antiandrogens
![](https://commons.wikimedia.org/wiki/Special:FilePath/Androgen_receptor.png?width=300)
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.