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Novel Approaches to Neuroprotection
Novel Approaches to Neuroprotection

... atom by atom into the binding pocket,” Dr. Hanneken said. “All of the molecular interactions of each atom within that pocket are calculated and converted into a mathematical format that predicts the likelihood that a compound will fit in that space. The program can look at hydrogen bonds and steric ...
File - Wk 1-2
File - Wk 1-2

...  Among receptors directly coupled to ion channels, desensitisation is often rapid and pronounced  State is caused by the conformational change in the receptor, resulting in a tight binding of the agonist without the opening of the ion channel.  Phosphorylation of the intracellular regions of the ...
DENS 211 4th Lecture
DENS 211 4th Lecture

... the right (the slope of the curve will be reduced)  Agonist potency may or may not be affected  Example: the noncompetitive antagonist action of crystal violet (CrV) on nicotinic acetylcholine receptors is explained by an allosteric mechanism in which the binding of CrV to the extracellular mouth ...
• • • • •
• • • • •

... • Aldosterone is a very powerful mineralocorticoid, but it has a week glucocorticoid activity. • Its release from the adrenal cortex is controlled by the renin-angiotensin system. • It acts on collecting tubules causing reabsorption of sodium, bicarbonate & water. Potassium & H + are lost in the uri ...


... Hormonal therapy. Gonadotropin-releasing hormone agonists inhibit the secretion of testosterone. The side effects are hot flashes, decreased libido, and impotence. Annual cost is approximately $5,000 (Keetch, 1997). Andrenergic receptor blockade. A nonsteroidal antiandrogen such as flutamide compete ...
4th Lecture 1433
4th Lecture 1433

...  It does not bind to the same receptor sites as the agonist. It would either: bind to a distinctly separate binding site from the agonist decreased affinity of the receptor for the agonist, “allosteric inhibition”,  So, it prevents conformational changes in the receptor required for receptor act ...
CN510 Lecture 4 Drugs and the Brain and
CN510 Lecture 4 Drugs and the Brain and

... Effects are hard to study; especially long-term effects CN 510 Lecture 20 ...
Localized Prostate Cancer
Localized Prostate Cancer

... interstitial prostate brachytherapy and external beam radiation therapy. With interstitial prostate brachytherapy, small radioactive “seeds” are planted in the prostate. Before treatment, the size (volume) of the prostate is checked by TRUS to decide the dosage of seeds. These seeds are then placed ...
The importance of residence and recognition time of drug
The importance of residence and recognition time of drug

... •Short overview on the use of SPR in drug discovery •Why binding kinetics is closely connected with PK/PD and therefore also efficacy •The value of residence/recognition time for Structure Kinetic Relations (SKR) •Q&A session ...
Naloxone as a Mu-Receptor Antagonist
Naloxone as a Mu-Receptor Antagonist

... hydromorphone given to RC after surgery, are not selective for one type of MOR so both effects are seen with their use (2). As more drug binds the MOR, the analgesic and respiratory depressive effects become enhanced. In an overdose, respiratory depression overpowers the analgesia, causing a lifethr ...
Role of the Androgen Receptor in Human Breast Cancer
Role of the Androgen Receptor in Human Breast Cancer

... into ovariectomized athymic mice has provided a model to examine in vivo effects of androgens on breast cancer growth. Again, in the presence and absence of exogenous E2 , DHT inhibited tumor growth and this effect of DHT was reversed by simultaneous administration of hydroxyflutam ide (22). Thus th ...
Analysis of Germline Cancer Pharmacogenetic Variants and Solid
Analysis of Germline Cancer Pharmacogenetic Variants and Solid

... The effectiveness and toxicity of a number of medications commonly prescribed to cancer patients varies with the patient’s genetic makeup. Testing for a number of well-known genetic variations can enable more effective treatments and better outcomes. Targeted panels of these variations can be tested ...
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Document

... • Systemic administration, short half life of ~ 2h • Topical ocular admin, longer half life. – Bind to iris pigments and are released over days ,darker irises bind more ...
Pharmacology 6 – SNS Antagonists
Pharmacology 6 – SNS Antagonists

... 1. Name common examples of non-selective and selective SNS antagonists and what are they clinically used for. 2. How do SNS antagonists produce their anti-hypertensive effects and what are their side effects. 3. Compare the effects produced by selective and non-selective antagonists, name examples o ...
How? Morphine is a pain medication of the opiate type which is
How? Morphine is a pain medication of the opiate type which is

... Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are distributed widely in the brain, and are also found in the spinal cord and digestive t ...
Data Sheet Sorafenib Tosylate
Data Sheet Sorafenib Tosylate

... that inhibits cell proliferation by targeting receptor tyrosine kinases, including VEGFR-2 and PDGFR--β and their associated signaling cascades of the ERK pathway and angiogenesis. It was originally developed as a Raf kinase inhibitor. It has been shown to have activity against several receptor tyro ...
A new international, multicenter study has found that incretin
A new international, multicenter study has found that incretin

... antidiabetic agents (2.9 times higher with exenatide, 2.7 times higher with sitagliptin). Incretin-based drugs include dipeptidyl peptidase-4 (DPP-4) inhibitors (eg, linagliptin, sitagliptin, vildagliptin, saxagliptin) and glucagon-like peptide-1 receptor agonists (eg, exenatide, liraglutide). Previ ...
Endocrinology Drug List
Endocrinology Drug List

...  radioactive half life = 8 days  must be isolated to avoid pregnant women and children ...
Prostate cancer is the second most common cancer diagnosed
Prostate cancer is the second most common cancer diagnosed

... whom it is not recommended due to the adverse balance of certain harms with unclear long-term benefit. Proper lesion selection is a second key consideration in choosing to undertake focal treatment of localized prostate cancer. Although prostate cancer has always been regarded as a multifocal diseas ...
Culture of Human Prostate Tumors Ex Vivo Evidence for Efficacy of
Culture of Human Prostate Tumors Ex Vivo Evidence for Efficacy of

... Purpose: Targeting Hsp90 has significant potential as a treatment for prostate cancer, but prototypical agents such as 17-allylamino-17 demethoxygeldanamycin (17-AAG) have been ineffective in clinical trials. Recently, a phase I study aimed at defining a biologically active dose reported the first r ...
page as PDF
page as PDF

... Great Interest in Apoptosis and IAP Antagonists as targets for cancer therapies All the cells in our body have the ability to self-destruct by activating an intrinsic cell suicide program termed Apoptosis, which greatly limits the accumulation of damaged and potentially dangerous cells. Cancer cells ...
to file - Planet Ross 2K2
to file - Planet Ross 2K2

... 2. Physostigmine – crosses BBB, use to treat antimuscarinic toxicity by atropine, Scopolamine 3. Neostigmine – does not cross BBB, use to treat myasthenia gravis, can directly activate Nm 4. Tacrine – used for early Alzheimer’s ...
DIM-Evail - Designs for Health
DIM-Evail - Designs for Health

... Can DIM be Taken with Medications? DIM is safe when taken with Tamoxifen, birth control pills and other herbs such as St. John’s Wort that affect cytochrome p450 enzymes. Because of its effects on CYP enzymes, I3C, however, should not be taken with any of these. I3C blocks ovulation, can interfere w ...
P R O S T A T E Patient Guide
P R O S T A T E Patient Guide

... beam radiation therapy. With interstitial prostate brachytherapy, small radioactive “seeds” are planted in the prostate. Before treatment, the size (volume) of the prostate is checked by TRUS to decide the dosage of seeds. These seeds are then placed into the prostate using needles that go through t ...
Benign Prostatic Hyperplasia
Benign Prostatic Hyperplasia

... urinary flow rate. The patient will be asked to describe symptoms in order to determine if the condition is worsening. b- Medication 5-Alpha reductase inhibitors such as finasteride (Proscar®) prevent the conversion of testosterone to the hormone dihydrotestosterone (DHT). In many cases, a treatment ...
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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.
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