Mechanisms of action of antiepileptic drugs
... been proposed that the slow inactivation pathway is more prominent during prolonged depolarisation, as might be expected during epileptiform discharges. Calcium channels. Voltage-gated calcium channels represent another important target for several antiepileptic agents. The efficacy of ethosuximide ...
... been proposed that the slow inactivation pathway is more prominent during prolonged depolarisation, as might be expected during epileptiform discharges. Calcium channels. Voltage-gated calcium channels represent another important target for several antiepileptic agents. The efficacy of ethosuximide ...
FUNCTIONAL NANO- AND MICROPARTICLES FOR DRUG, NUTRITION, AGRO AND ENVIRONMENTAL APPLICATIONS
... The enzymes used for ADEPT must be stable under physiological conditions and able to catalyze a scission reaction of the prodrug. In addition, their catalytic properties should be different from those of any circulating endogenous enzyme and ideally, they should be able to activate a panel of antica ...
... The enzymes used for ADEPT must be stable under physiological conditions and able to catalyze a scission reaction of the prodrug. In addition, their catalytic properties should be different from those of any circulating endogenous enzyme and ideally, they should be able to activate a panel of antica ...
Drug chirality: Stereoselectivity in the action and disposition
... across blood brain barrier. Neurotoxic at high doses Effects of Gantacurium, a chlorofumarate muscle relaxant, can be rapidly reveresed by L-cysteine. Not been introduced in clinical practice. ...
... across blood brain barrier. Neurotoxic at high doses Effects of Gantacurium, a chlorofumarate muscle relaxant, can be rapidly reveresed by L-cysteine. Not been introduced in clinical practice. ...
Modulation of the Partition Coefficient between Octanol and Buffer at
... The optimization of absorption, distribution, metabolism, and excretion properties and prediction of human pharmacokinetics have become important parts of the early selection process in drug discovery. It is well known that the physicochemical properties of a molecule (lipophilicity, molecular weigh ...
... The optimization of absorption, distribution, metabolism, and excretion properties and prediction of human pharmacokinetics have become important parts of the early selection process in drug discovery. It is well known that the physicochemical properties of a molecule (lipophilicity, molecular weigh ...
The war against cancer: Suicide gene therapy
... DNA, ballistic DNA injection, electroporation, sonoporation, magnetofection, and hydroporation[36]. Injection of Naked DNA. Naked DNA or plasmid injection is a type of non-viral vector. Direct injection of free DNA into targeted tissues (tumor tissues) has been shown to produce high levels of gene e ...
... DNA, ballistic DNA injection, electroporation, sonoporation, magnetofection, and hydroporation[36]. Injection of Naked DNA. Naked DNA or plasmid injection is a type of non-viral vector. Direct injection of free DNA into targeted tissues (tumor tissues) has been shown to produce high levels of gene e ...
TOPIC OUTLINE
... Mucosal protecting actions (binds to ulcer base, promote mucin and bicarbonate production) Used in combination regiments to treat H. pylori infection in peptic ulcer (bismuth chelate is a 2nd choice regimen in treatment of H. pylori peptic ulcers) Has toxic effects to bacillus (bactericidal; compare ...
... Mucosal protecting actions (binds to ulcer base, promote mucin and bicarbonate production) Used in combination regiments to treat H. pylori infection in peptic ulcer (bismuth chelate is a 2nd choice regimen in treatment of H. pylori peptic ulcers) Has toxic effects to bacillus (bactericidal; compare ...
Cancer Association of South Africa (CANSA) Fact Sheet
... The phi combines measurements of %fPSA(percent of protein-attached and protein-free PSA circulating in the bloodstream) and a subcategory of free PSA called pro-PSA, and is estimated to be 2.5 times more specific in detecting prostate cancer in patients than a PSA screening. The phi was approved by ...
... The phi combines measurements of %fPSA(percent of protein-attached and protein-free PSA circulating in the bloodstream) and a subcategory of free PSA called pro-PSA, and is estimated to be 2.5 times more specific in detecting prostate cancer in patients than a PSA screening. The phi was approved by ...
Anxiogenic and aversive effects of CRF in the BNST in the
... CRF1 is responsible for the anxiogenic effects of CRF CRF has a higher affinity for CRF1 More CRF1 then CRF2 in BNST ...
... CRF1 is responsible for the anxiogenic effects of CRF CRF has a higher affinity for CRF1 More CRF1 then CRF2 in BNST ...
The behavioral pharmacology of hallucinogens
... twitch response are hallucinogenic. Indeed, head twitches are induced by various serotonergic, but not necessarily hallucinogenic, agents [20,34]. Thus, the induction of a head twitch response should not be taken as prima facie evidence for hallucinogenic effects without further study. Nevertheless, ...
... twitch response are hallucinogenic. Indeed, head twitches are induced by various serotonergic, but not necessarily hallucinogenic, agents [20,34]. Thus, the induction of a head twitch response should not be taken as prima facie evidence for hallucinogenic effects without further study. Nevertheless, ...
Evaluation of analgesic activity of Evodia lunu-ankenda
... Statistical analysis Statistical analysis was performed, using one way analysis of variance (ANOVA) followed by Tukey-kramer Multiple comparison Test. All values were expressed as ±SEM. RESULTS AND DISCUSSION Acute toxicity studies did not reveal any toxic symptoms or death in any of the animals up ...
... Statistical analysis Statistical analysis was performed, using one way analysis of variance (ANOVA) followed by Tukey-kramer Multiple comparison Test. All values were expressed as ±SEM. RESULTS AND DISCUSSION Acute toxicity studies did not reveal any toxic symptoms or death in any of the animals up ...
- Jurnal UGM
... secondary metabolites are important to standardize and to increase quality of the TM. Over 24,000 stuctures of secondary metabolites have been isolated and evaluated its biological activities. Some of them have antinutritional and toxic effect on mammals.6 Moreover, some of plant secondary metaboli ...
... secondary metabolites are important to standardize and to increase quality of the TM. Over 24,000 stuctures of secondary metabolites have been isolated and evaluated its biological activities. Some of them have antinutritional and toxic effect on mammals.6 Moreover, some of plant secondary metaboli ...
IDENTIFICATION OF DUAL AGONISTIC NOVEL LIGANDS FOR INSULIN RECEPTOR AND... THROUGH MOLECULAR DOCKING
... insulin receptor and could be able promote the insulin signaling pathway. At the same time only 2 compounds are docked with PPARγ and could be able to promote PPAR signaling pathway. Hence it is clear that these 2 compounds could phosphorlyate both the insulin receptor and PPARγ there by providing s ...
... insulin receptor and could be able promote the insulin signaling pathway. At the same time only 2 compounds are docked with PPARγ and could be able to promote PPAR signaling pathway. Hence it is clear that these 2 compounds could phosphorlyate both the insulin receptor and PPARγ there by providing s ...
STEROIDS What Are Steroids? Steroids are hormones of 3 types: 1
... 2. Glucocorticosteroids – like cortisone or prednisone, that are anti- inflammatory or immunosuppressants used in swelling, rashes, asthma, or bronchitis. 3. Minerocorticosteroids – like vasopressin, that are produced by the adrenal glands for salt and water regulation. We’ll focus on anabolic stero ...
... 2. Glucocorticosteroids – like cortisone or prednisone, that are anti- inflammatory or immunosuppressants used in swelling, rashes, asthma, or bronchitis. 3. Minerocorticosteroids – like vasopressin, that are produced by the adrenal glands for salt and water regulation. We’ll focus on anabolic stero ...
Pharmacology of the autonomic nervous system for dental students
... Cholinergic antagonists are only muscarinic receptor blockers. Nicotinic receptor blockers are ganglionic blocking drugs or neuromuscular blockers (skeletal muscle relaxants) depending on the location of the nicotinic type acetylcholine receptors. The prototype of muscarinic antagonists is atropine. ...
... Cholinergic antagonists are only muscarinic receptor blockers. Nicotinic receptor blockers are ganglionic blocking drugs or neuromuscular blockers (skeletal muscle relaxants) depending on the location of the nicotinic type acetylcholine receptors. The prototype of muscarinic antagonists is atropine. ...
Chapter 16 Cholinesterase Inhibitors
... Fetal injury Cough Angioedema Hyperkalemia Dysgeusia and rash Renal failure Neutropenia ...
... Fetal injury Cough Angioedema Hyperkalemia Dysgeusia and rash Renal failure Neutropenia ...
Moving mountains to serve cancer patients
... We can target multiple signaling pathways relevant to various cancers with one protein— as APE1 regulates transcription factors (TFs) HIF1a, STAT3, NFkB and others. ...
... We can target multiple signaling pathways relevant to various cancers with one protein— as APE1 regulates transcription factors (TFs) HIF1a, STAT3, NFkB and others. ...
SedaLin - Xymogen
... Magnolia officinalis Magnolia bark is rich in a biphenol compound called honokiol and its isomer magnolol. In experimental animal studies, these compounds have been shown to enhance the activity of gamma-aminobutyric acid (GABA) A receptors and GABA binding, *These statements have not been evaluated ...
... Magnolia officinalis Magnolia bark is rich in a biphenol compound called honokiol and its isomer magnolol. In experimental animal studies, these compounds have been shown to enhance the activity of gamma-aminobutyric acid (GABA) A receptors and GABA binding, *These statements have not been evaluated ...
Guidelines for predicting toxic doses of pharmaceuticals
... drug under review, use case reports for structurally and pharmacologically similar drugs. ...
... drug under review, use case reports for structurally and pharmacologically similar drugs. ...
pdf
... Glucocorticoids are often used for the treatment of ketosis and Isoflupredone acetate and dexamethasone is commonly used for this purpose. In this study, 20 male lambs 12 -15 months that their weight and nutritional status were similar divided in 2 groups (10 cows), and for all of the 10 sheep in ex ...
... Glucocorticoids are often used for the treatment of ketosis and Isoflupredone acetate and dexamethasone is commonly used for this purpose. In this study, 20 male lambs 12 -15 months that their weight and nutritional status were similar divided in 2 groups (10 cows), and for all of the 10 sheep in ex ...
Early treatment of psychosis
... • Partial agonist at D2 receptor • Intrinsic activity depends on synaptic levels of DA • Affinity for muscarinic, α1-adrenergic, serotonin and histamine receptors • Good oral absorption, 3-5 hr to peak plasma concentration, long elimination half life • Few extrapyramidal side effects ...
... • Partial agonist at D2 receptor • Intrinsic activity depends on synaptic levels of DA • Affinity for muscarinic, α1-adrenergic, serotonin and histamine receptors • Good oral absorption, 3-5 hr to peak plasma concentration, long elimination half life • Few extrapyramidal side effects ...
Collaborative researCh Update 2010/2011
... venue for the funding of worthwhile research projects focused on prostate cancer. In 1999, PCFA’s Peer Review Committee (as the Research Committee was then known) was chaired by Professor Roger Reddell (1999 -2003), followed by Professor Robert Baxter (2003-2006). The current Chairman, Professor Joh ...
... venue for the funding of worthwhile research projects focused on prostate cancer. In 1999, PCFA’s Peer Review Committee (as the Research Committee was then known) was chaired by Professor Roger Reddell (1999 -2003), followed by Professor Robert Baxter (2003-2006). The current Chairman, Professor Joh ...
L04 Cannabinoids Part 1 Medicinal Plants
... are synthetic cannabinoid analogues used as an antiemetic by cancer and AIDS patients. This is one of the permissions to be utilized for therapeutic purposes. But why this is limited to these patients only? Because euphoria which is one of the major disadvantages of using Cannabis sativa as a therap ...
... are synthetic cannabinoid analogues used as an antiemetic by cancer and AIDS patients. This is one of the permissions to be utilized for therapeutic purposes. But why this is limited to these patients only? Because euphoria which is one of the major disadvantages of using Cannabis sativa as a therap ...
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 ...
An Innovative Approach to New Antimicrobial Drugs SUMMARY
... 1. Measurement of various kinetic isotope effects (KIEs) for the reactions catalysed by human and E. coli DHFRs. This will require the production of DHFR substrates (NADPH and dihydrofolate ...
... 1. Measurement of various kinetic isotope effects (KIEs) for the reactions catalysed by human and E. coli DHFRs. This will require the production of DHFR substrates (NADPH and dihydrofolate ...
Inertly labeled monoclonal antibodies for PET and optical imaging
... In 1997, rituximab was the first mAb in oncology that was approved by the US Food and Drug Administration (FDA). It is directed against the CD20 antigen and used for patients with non-Hodgkin’s lymphoma (NHL). Hematologic malignancies are relatively easy to target, because the cells are in close con ...
... In 1997, rituximab was the first mAb in oncology that was approved by the US Food and Drug Administration (FDA). It is directed against the CD20 antigen and used for patients with non-Hodgkin’s lymphoma (NHL). Hematologic malignancies are relatively easy to target, because the cells are in close con ...
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.