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Untitled
Untitled

... serious endometrial hyperplasia earlier in life than untreated animals [44]. Some MGA-treated felids with endometrial hyperplasia also developed endometrial polyps, endometritis and pyometra, [44] conditions that likely would also result in infertility. Furthermore, most felids with endometrial canc ...
Cannabinoids for Gastrointestinal Diseases: Potential Therapeutic
Cannabinoids for Gastrointestinal Diseases: Potential Therapeutic

... that include plant-derived cannabinoids and synthetic analogues of these compounds. Of these, ∆9-THC, ∆8-THC and cannabinol are constituents of marijuana, whereas HU-210 (11-hydroxy-∆8-THC-demethylheptyl) is a synthetic cannabinoid. ∆9-THC and ∆8-THC bind both CB1 and CB2 receptors at submicromolar ...
Chemotherapy-Induced Nausea and Vomiting
Chemotherapy-Induced Nausea and Vomiting

... upper small intestine (bottom of figure). After the administration of chemotherapy, free radicals are generated, leading to localized exocytotic release of 5-hydroxytryptamine (5-HT) from the enterochromaffin cells; 5-HT then interacts with 5-hydroxytryptamine3 (5-HT3) receptors on vagal afferent te ...
Document
Document

... upper small intestine (bottom of figure). After the administration of chemotherapy, free radicals are generated, leading to localized exocytotic release of 5-hydroxytryptamine (5-HT) from the enterochromaffin cells; 5-HT then interacts with 5-hydroxytryptamine3 (5-HT3) receptors on vagal afferent te ...


... may occur [7]. Mediators may act on target cells within the airways to induce features typical of asthma, such as bronchoconstriction, mucus plugging, airway wall oedema through microvascular leakage, eosinophil infiltration and bronchial hyperresponsiveness [8]. Although many mediators are likely t ...
Development of 5-Substituted N-Methylmorphinan-6
Development of 5-Substituted N-Methylmorphinan-6

... activity of 14-methoxymetopon was also established using [35 S]GTPγS functional assays in rat brain [14, 26], calf striatum [28], and Chinese hamster ovary (CHO) cells expressing mouse MOR splice variants [28]. When compared to 14-O-methyloxymorphone (1), the 5-methyl analogue 13 showed less than th ...
DRUG NAME: Pamidronate
DRUG NAME: Pamidronate

... Breastfeeding is not recommended due to the potential secretion into breast milk. ...
STUDY OF THE NEUROMODULATORY EFFECTS OF DOPAMINE
STUDY OF THE NEUROMODULATORY EFFECTS OF DOPAMINE

... a wide variety of physiological functions, from the coordination of neuroendocrine, autonomic, and somatomoter responses to the initiation of reward, stress, and anxiety responses (Deyama et al., 2007; Dong and Swanson, 2003; Dong and Swanson, 2004; Dong and Swanson, 2006; Erb and Stewart, 1999; Eil ...
Dopamine receptor agonist treatment of Parkinson`s disease
Dopamine receptor agonist treatment of Parkinson`s disease

... agonists as a form of treatment for this disease. The aims of this systematic review and metaanalysis were to establish the efficacy of different subclasses of dopamine receptor agonist in the treatment of animal models of PD, to examine the relationship between details of the methods used in these ...
Chronic Treatment with Dopamine Receptor Antagonists
Chronic Treatment with Dopamine Receptor Antagonists

... -In- vivo ji’upentixol specificity. Male Sprague-Dawley rats (160-l 80 gm; Simonsen) were iniected (i.n.) with EEDO (8 mrr/ka) freshlv dissolved in ethr&ol/wate; (1:l voi/vol) or vehicle alone. To determine whether EEDQ had the same EC,, for D, and D, dopamine receptors, a dose-response for EEDQ was ...
Desensitization of Cannabinoid-Mediated Presynaptic Inhibition of
Desensitization of Cannabinoid-Mediated Presynaptic Inhibition of

... networks. This inhibition was readily reversed during a 10min washout period (Fig. 2A). This effect was concentration dependent with an EC50 of 2.7 ⫾ 0.3 nM in good agreement with our previous studies (Shen et al., 1996). Cultures treated for 18 to 24 h with 100 nM Win55,212-2 were considerably less ...
assessment of the opiate properties of two constituents of a toxic
assessment of the opiate properties of two constituents of a toxic

... SUMMARY ...
Analysing the effect of I1 imidazoline receptor ligands on DSS
Analysing the effect of I1 imidazoline receptor ligands on DSS

... Imidazoline receptors (IRs) have been recognized as promising targets in the treatment of numerous diseases, and moxonidine and rilmenidine, agonists of I1-IRs are widely used as antihypertensive agents. Some evidence suggests that IR ligands may induce anti-inflammatory effects acting on I1-IRs or ...
patrick_tb_ch22
patrick_tb_ch22

... What physical feature other than logP is important to the activity of cimetidine analogues? Feedback: To be precise, the orientation of the dipole moment is important to the activity rather than the size of the dipole moment. Page reference: 660 a. Hydrophobicity b. Basicity ...
Histamine in Atopic Disorders: Atopic Dermatitis and
Histamine in Atopic Disorders: Atopic Dermatitis and

... involved in the induction of proinflammatory cytokines in activated monocytes and macrophages by enhanced IL-31 release (Kasraie et al., 2010). Stimulation of the H4 receptor also inhibits the antigen-specific human T cell responses by decreased IFN-g and IL-5 expression (Sugata et al., 2007). Th17 ...
The Strange Case of Strontium Ecklonia Cava Extract
The Strange Case of Strontium Ecklonia Cava Extract

... Ecklonia Cava Extract (ECE) is a standardized natural complex of unique marine molecules that originate from a specific species of brown algae (Ecklonia cava). ECE represents a unique category of polyphenols often called phlorotannins. ECE is considered a "super antioxidant" as it has up to eight in ...
Current clinical trials in LAM
Current clinical trials in LAM

... • Known allergy to letrozole • Inability to comply with pulmonary function tests or follow up visits. • Treatment with investigational agents within 30 days • Hormonal therapy (e.g. estrogen, progestin, LHRH agonists or antagonists, estrogen receptor blockers, estrogen receptor down regulators, arom ...
Steroids and athletes: Genes work overtime
Steroids and athletes: Genes work overtime

... and deepening of the voice (some of these effects are irreversible!). Another problem with taking the natural form of testosterone is that it is not very effective when given orally. After oral administration, testosterone is absorbed from the intestine into the bloodstream, which takes it to the li ...
sveikatos technologijos vertinimas - Lietuvos Respublikos sveikatos
sveikatos technologijos vertinimas - Lietuvos Respublikos sveikatos

... C0001. What kind of harms can use of the cryotherapy cause to the patient? ........................... 58 C0002; C0004. What is the dose relationship of the harms? How does the frequency or severity of harms change over time or in different settings? ................................................. ...
COMMITTEE OPINION Committee on Gynecologic Practice Number 484 • April 2011
COMMITTEE OPINION Committee on Gynecologic Practice Number 484 • April 2011

... promote growth of skeletal muscle, increase hemoglobin concentration, and mediate secondary sexual characteristics. These substances have been in use since the 1930s to promote muscle growth, improve athletic performance, and enhance cosmetic appearance. Although anabolic steroids are controlled sub ...
Omalizumab in ABPA - Stanford University
Omalizumab in ABPA - Stanford University

... – Frequent toxicities (vori>itra). Absorption, metabolism, drug interactions mandate drug level monitoring; resistance 4-8% ...
Modulating the cystic fibrosis transmembrane regulator – breaking
Modulating the cystic fibrosis transmembrane regulator – breaking

... review, designated PTC124 and also known as Ataluren.34 Ataluren binds to eukaryotic ribosomes and suppresses PTCs in cell- and animal-based disease models. There have been three randomised open-label dose-ascending Phase II trials in CF. The results of all showed tolerability to Ataluren in the sho ...
Nefazodone in the rat: mimicry and antagonism of [À]-DOM
Nefazodone in the rat: mimicry and antagonism of [À]-DOM

... specifically, as the dose of nefazodone administered intraperitoneally is increased, we observe an elevation in [ ]DOM appropriate responding. The interaction of a drug with its receptors may be characterized by the affinity of the drug for the receptors and its intrinsic activity at the receptors ( ...


NIH Public Access
NIH Public Access

... pteridine ring. MTX differs from aminopterin in having the addition of a methyl group at the N10 position, in a bridge between the pteridine and p-amino-benzoic acid moieties. These structural differences from folic acid confer on these analogs an extremely high affinity for DHFR. The primary action ...
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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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