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Studies of the Biogenic Amine Transporters. 12. Identification of
... Shelton, CT) after overnight extraction in 0.6 ml of liquid scintillation cocktail (MP Biomedicals, Solon, OH). Typical total and nonspecific cpms observed for the rat brain transporter uptake inhibition assays were 18,000 and 1000, respectively. [3H]MPPⴙ Release Assays. This assay measures the abil ...
... Shelton, CT) after overnight extraction in 0.6 ml of liquid scintillation cocktail (MP Biomedicals, Solon, OH). Typical total and nonspecific cpms observed for the rat brain transporter uptake inhibition assays were 18,000 and 1000, respectively. [3H]MPPⴙ Release Assays. This assay measures the abil ...
Lucrin® PDs Depot 3.75 mg
... injections During the early phase of therapy, sex steroids temporarily rise above withachieved a terminal elimination of approximately hours based Delusion Not known on Transient increases in acid phosphatase levels sometimes occurred early baseline because of the physiological effect of the drug. T ...
... injections During the early phase of therapy, sex steroids temporarily rise above withachieved a terminal elimination of approximately hours based Delusion Not known on Transient increases in acid phosphatase levels sometimes occurred early baseline because of the physiological effect of the drug. T ...
Testosterone deficiency and testosterone replacement therapy
... Testosterone is the main “male hormone” or androgen in men. As you get older, the levels of testosterone in your body tend to gradually decline about 1% each year. This change usually affects your sex drive or erections. In some men, however, low concentrations of testosterone are associated with im ...
... Testosterone is the main “male hormone” or androgen in men. As you get older, the levels of testosterone in your body tend to gradually decline about 1% each year. This change usually affects your sex drive or erections. In some men, however, low concentrations of testosterone are associated with im ...
Inhaled Adrenergic Bronchodilators: Historical
... Isoproterenol (isoprenaline). Isoproterenol has an isopropyl group attached to the terminal nitrogen, giving it a larger group at this site and, in keeping with the keyhole theory of -2 specificity, shifts its activity from ␣ to largely  stimulation. Since the catechol nucleus remains the same as ...
... Isoproterenol (isoprenaline). Isoproterenol has an isopropyl group attached to the terminal nitrogen, giving it a larger group at this site and, in keeping with the keyhole theory of -2 specificity, shifts its activity from ␣ to largely  stimulation. Since the catechol nucleus remains the same as ...
Invited Review - International Journal of Pharmaceutical Science
... pair of electrons from the sulfur atom completing the needed 6 π electrons to satisfy Huckel’s rule. The resonance forms ...
... pair of electrons from the sulfur atom completing the needed 6 π electrons to satisfy Huckel’s rule. The resonance forms ...
Ca 2+
... • Bind to specific sites on the alpha1 subunit of the L-type Ca2+ channel • Reduce the probability of channel opening rather then calcium current flow through an open channel • Tissue selectivity is one of the most beneficial properties of Ca2+ antagonists • In general, skeletal muscle, bronchial, t ...
... • Bind to specific sites on the alpha1 subunit of the L-type Ca2+ channel • Reduce the probability of channel opening rather then calcium current flow through an open channel • Tissue selectivity is one of the most beneficial properties of Ca2+ antagonists • In general, skeletal muscle, bronchial, t ...
Chapter 16 Cholinesterase Inhibitors
... • Antihistamines are of little use in treatment • Epinephrine is the drug of choice for treatment (see Chapter 17) ...
... • Antihistamines are of little use in treatment • Epinephrine is the drug of choice for treatment (see Chapter 17) ...
Medication for the treatment of lung cancer
... cells or increase the tolerance of the healthy cells. This latter modification allows the subsequent administration of higher dosages of chemotherapy. The p53 gene, dysfunction of which is related to drug resistance, is a very potent agent, which can reverse malignant activity through its integratio ...
... cells or increase the tolerance of the healthy cells. This latter modification allows the subsequent administration of higher dosages of chemotherapy. The p53 gene, dysfunction of which is related to drug resistance, is a very potent agent, which can reverse malignant activity through its integratio ...
Pain control in cancer: recent findings and trends
... receptor. This induces a ligand-gated Na+ current to produce rapid depolarization. Sustained Na+ flux activates the NMDA receptor to develop a high affinity for glutamate. Activation of AMPA, NMDA and other receptors alters the sensitivity of these receptors and affects their shuttling to active zon ...
... receptor. This induces a ligand-gated Na+ current to produce rapid depolarization. Sustained Na+ flux activates the NMDA receptor to develop a high affinity for glutamate. Activation of AMPA, NMDA and other receptors alters the sensitivity of these receptors and affects their shuttling to active zon ...
Jacob, Reza: Docking Algorithms of Virtual Ligand Screening
... of a closely related compound. For example, if two similar compounds differ only by an R- group, then knowing the docked conformation of one might greatly facilitate the docking of the other. In any case, researchers suggest manual screening of the top 300 or so hits from a virtual ligand screening ...
... of a closely related compound. For example, if two similar compounds differ only by an R- group, then knowing the docked conformation of one might greatly facilitate the docking of the other. In any case, researchers suggest manual screening of the top 300 or so hits from a virtual ligand screening ...
Therapeutic targeting of microRNAs: current status and
... miRNAs is common in human disease has led to considerable interest in the therapeutic targeting of miRNAs. To date, three main approaches have been taken: expression vectors (miRNA sponges), small-molecule inhibitors and antisense oligonucleotides (ASOs) (FIG. 3). Vector-based strategies rely on the ...
... miRNAs is common in human disease has led to considerable interest in the therapeutic targeting of miRNAs. To date, three main approaches have been taken: expression vectors (miRNA sponges), small-molecule inhibitors and antisense oligonucleotides (ASOs) (FIG. 3). Vector-based strategies rely on the ...
Ciprofloxacin sensitizes hormone-refractory prostate cancer cell
... In general, a clinical chemotherapeutic regimen consists of combination of drugs in order to achieve a therapeutic efficacy higher than that provided by single drugs, to decrease systemic toxicity and to circumvent drug resistance [9, 16, 38, 39]. Ideally, the combined drugs should have proven singl ...
... In general, a clinical chemotherapeutic regimen consists of combination of drugs in order to achieve a therapeutic efficacy higher than that provided by single drugs, to decrease systemic toxicity and to circumvent drug resistance [9, 16, 38, 39]. Ideally, the combined drugs should have proven singl ...
Psilocybin and Consciousness
... Because they are not chemically identical to serotonin, they have manifest varied effects, particularly at the 5-HT2A receptor. ...
... Because they are not chemically identical to serotonin, they have manifest varied effects, particularly at the 5-HT2A receptor. ...
cHAPTER 7 The specificity of different selective and non
... is intended to result in an anxiolytic compound that is devoid of the unwanted effects of existing benzodiazepines. There are two options to attain this selectivity: selective affinity and selective efficacy for a certain subtype. The first option first resulted in sleep inducers with a higher affinity ...
... is intended to result in an anxiolytic compound that is devoid of the unwanted effects of existing benzodiazepines. There are two options to attain this selectivity: selective affinity and selective efficacy for a certain subtype. The first option first resulted in sleep inducers with a higher affinity ...
Adrenergic Agonists
... thus increasing blood flow to the kidneys and other viscera (see Figure 6.12). These receptors are not affected by α or β-blocking drugs. Therefore, dopamine is clinically useful in the treatment of shock, in which significant increases in sympathetic activity might compromise renal function. [Note: ...
... thus increasing blood flow to the kidneys and other viscera (see Figure 6.12). These receptors are not affected by α or β-blocking drugs. Therefore, dopamine is clinically useful in the treatment of shock, in which significant increases in sympathetic activity might compromise renal function. [Note: ...
Herbal Medicine for the Family Physician
... Regulatory Status Herbs are sold as “dietary supplements” like Vitamins Dietary Supplement Health and Education Act of 1994 • --Safe, unless proven unsafe by FDA • --Not required to show bioequivalence • --Large variances between brands and lots • --”Standardized” means a specified concentration of ...
... Regulatory Status Herbs are sold as “dietary supplements” like Vitamins Dietary Supplement Health and Education Act of 1994 • --Safe, unless proven unsafe by FDA • --Not required to show bioequivalence • --Large variances between brands and lots • --”Standardized” means a specified concentration of ...
Functional assays for screening GPCR targets
... Several GPCRs clearly activate multiple G proteins [9,10]. Although multiplicity of coupling in some cases can be an artifact of receptor overexpression in recombinant expression systems, it has also been clearly estabCurrent Opinion in Biotechnology 2005, 16:655–665 ...
... Several GPCRs clearly activate multiple G proteins [9,10]. Although multiplicity of coupling in some cases can be an artifact of receptor overexpression in recombinant expression systems, it has also been clearly estabCurrent Opinion in Biotechnology 2005, 16:655–665 ...
Sebaceous-disorders-I
... • Most patients have normal levels of androgens, thus an end-organ hyperresponsiveness may be present • Sebaceous activity is predominantly dependent on androgens, thus, abnormally high levels of sebum secretion could result from high overall androgen production, or increased availability of free a ...
... • Most patients have normal levels of androgens, thus an end-organ hyperresponsiveness may be present • Sebaceous activity is predominantly dependent on androgens, thus, abnormally high levels of sebum secretion could result from high overall androgen production, or increased availability of free a ...
Disorders of Hemostasis Hereditary Disorders of Hemostasis Von
... o Factor replacement therapy – either plasma-derived concentrates that have been treated by viral attenuation, or, more commonly now, recombinant factor VIII or factor IX o Obtain hematology consult for perioperative management advice. o DDAVP will increase plasma factor VIII and vWF concentrations ...
... o Factor replacement therapy – either plasma-derived concentrates that have been treated by viral attenuation, or, more commonly now, recombinant factor VIII or factor IX o Obtain hematology consult for perioperative management advice. o DDAVP will increase plasma factor VIII and vWF concentrations ...
Opioid Receptors - Science Mission
... “rewarding”. These effects may lead to “craving” or “hunger” for the drug, with resultant spontaneous activity or work for drug acquisition and self-administration. Primary sites of actions of drugs of abuse with respect to their reward or reinforcing effects have been identified as specific brain r ...
... “rewarding”. These effects may lead to “craving” or “hunger” for the drug, with resultant spontaneous activity or work for drug acquisition and self-administration. Primary sites of actions of drugs of abuse with respect to their reward or reinforcing effects have been identified as specific brain r ...
Shared Care Guideline for Testosterone
... Secondary hypogonadism (secondary testicular failure) is due to failure of the hypothalamus and/or pituitary also either as a result of congenital or pituitary causes. Late-onset hypogonadism (LOH) is defined as ‘A clinical and syndrome associated with advancing age and characterised by typical symp ...
... Secondary hypogonadism (secondary testicular failure) is due to failure of the hypothalamus and/or pituitary also either as a result of congenital or pituitary causes. Late-onset hypogonadism (LOH) is defined as ‘A clinical and syndrome associated with advancing age and characterised by typical symp ...
Clomid to increase muscle
... an anabolic steroid, but a prescription drug as a fertility aid. What is Clomid and how does it work? Clomid is an oral medication that can be used to stimulate ovulation. It works by blocking estrogen receptors at the. Using Testosterone for Muscle Gains written by Growth Factor. If you were to giv ...
... an anabolic steroid, but a prescription drug as a fertility aid. What is Clomid and how does it work? Clomid is an oral medication that can be used to stimulate ovulation. It works by blocking estrogen receptors at the. Using Testosterone for Muscle Gains written by Growth Factor. If you were to giv ...
Inquiry into early detection and treatment of prostate cancer
... We agree with this emphasis and believe the Ministry of Health should encourage and promote the case for men to seek up-to-date evidence-based information from their general practitioner on the pros and cons of early testing and treatment of prostate cancer, so that they can make an active choice th ...
... We agree with this emphasis and believe the Ministry of Health should encourage and promote the case for men to seek up-to-date evidence-based information from their general practitioner on the pros and cons of early testing and treatment of prostate cancer, so that they can make an active choice th ...
The New Generation of Targeted Therapies for
... Erlotinib-Another agent that has been studied in women with advanced breast cancer is erlotinib. Much like gefitinib, erlotinib is orally active and was well tolerated in phase I trials.[ 1,16] An open-label phase II trial of erlotinib in metastatic breast cancer was recently completed.[17] Two coho ...
... Erlotinib-Another agent that has been studied in women with advanced breast cancer is erlotinib. Much like gefitinib, erlotinib is orally active and was well tolerated in phase I trials.[ 1,16] An open-label phase II trial of erlotinib in metastatic breast cancer was recently completed.[17] Two coho ...
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.