... In a number of previous studies, we analyzed the effects of AAS on agonistic behavior in mice, finding that different doses, substances and duration of treatment in addition to individual features have different, often contradictory, impacts on offensive behavior in gonadally intact male mice. A sin ...
Cancer Therapy – Opioid growth factors E
... arresting pancreatic cancer cell growth in patients, Penn State College of Medicine researchers report. “ Our previous laboratory and animal studies showed that opioid growth factor, called OGF, can markedly slow down the proliferation of pancreatic cancer cells,” said Ian S. Zagon, Ph.D., professor ...
... arresting pancreatic cancer cell growth in patients, Penn State College of Medicine researchers report. “ Our previous laboratory and animal studies showed that opioid growth factor, called OGF, can markedly slow down the proliferation of pancreatic cancer cells,” said Ian S. Zagon, Ph.D., professor ...
... Recent years have witnessed major advances in our understanding of the pathogenesis of benign prostatic hyperplasia (BPH) and prostate cancer at both the molecular and cellular level. These developments were based essentially on fundamental research that as yet has not been substantially translated ...
Activation instead of blocking mesolimbic dopaminergic reward
... expressed in Spodoptera frugiperda insect cells that stimulation of DA receptors by the pure D2 receptor agonist Bromocriptine resulted in proliferation of D2 receptors over a 14 day period. In the same study it was shown that administration of a DA antagonist caused the proliferation of D2 antagoni ...
... expressed in Spodoptera frugiperda insect cells that stimulation of DA receptors by the pure D2 receptor agonist Bromocriptine resulted in proliferation of D2 receptors over a 14 day period. In the same study it was shown that administration of a DA antagonist caused the proliferation of D2 antagoni ...
PAIN AND OPIOID ANALGESICS
... 1. All of the following opioid receptors are correctly matched with their physiological effects, except: A) – analgesia and respiratory depression; B) k – analgesia and dysphoria; C) – miosis and physical dependence; D) - euphoria and reduced GIT motility. 2. Which of the following analgesics ...
... 1. All of the following opioid receptors are correctly matched with their physiological effects, except: A) – analgesia and respiratory depression; B) k – analgesia and dysphoria; C) – miosis and physical dependence; D) - euphoria and reduced GIT motility. 2. Which of the following analgesics ...
noradrenergic neuroeffector transmission as a target of drug action.
... Most of the agonists selective at 2adrenoceptors that are used as bronchodilator drugs are neither substrates for uptake nor for enzymatic degradation by MAO or COMT Salbutamol is also useful as a relaxant of uterine smooth muscle when attempting to ...
... Most of the agonists selective at 2adrenoceptors that are used as bronchodilator drugs are neither substrates for uptake nor for enzymatic degradation by MAO or COMT Salbutamol is also useful as a relaxant of uterine smooth muscle when attempting to ...
Herbal Cancer Treatment
... 9-aminocamptothecin, and CPT-11. Camptothecin and these analogs are being investigated to treat a variety of cancers, but the compounds are quite toxic, and only topotecan (Hycamtin®) and irinotecan HCl (Camptosar®) have met with the FDA approval; Hycamtin® has been approved for ovarian cancer thera ...
... 9-aminocamptothecin, and CPT-11. Camptothecin and these analogs are being investigated to treat a variety of cancers, but the compounds are quite toxic, and only topotecan (Hycamtin®) and irinotecan HCl (Camptosar®) have met with the FDA approval; Hycamtin® has been approved for ovarian cancer thera ...
Unexpected Suppression of Immunoassay Results by Cross
... posed major analytical challenges, which most likely stem from the delicate balance between chemical equilibrium and our ever-increasing quest for speed of analysis, simplicity of procedure, and improved reliability. In attempts to enhance these criteria, we often face limitations imposed by the fun ...
... posed major analytical challenges, which most likely stem from the delicate balance between chemical equilibrium and our ever-increasing quest for speed of analysis, simplicity of procedure, and improved reliability. In attempts to enhance these criteria, we often face limitations imposed by the fun ...
View PDF or right
... Thus, in the absence of proven severe androgen deficiency, testosterone replacement should not be offered routinely to healthy elderly men in the hope of reversing age related changes in the body composition. Longer term studies, including much larger number subjects, with clinically relevant end po ...
... Thus, in the absence of proven severe androgen deficiency, testosterone replacement should not be offered routinely to healthy elderly men in the hope of reversing age related changes in the body composition. Longer term studies, including much larger number subjects, with clinically relevant end po ...
Molecular Basis of Multidrug Transport by ATP
... Most eukaryotic multidrug ABC transporters (e.g., Pglycoprotein) comprise four domains which are fused into a single polypeptide. Two of these domains, the transmembrane domains, are hydrophobic and span the membrane multiple times. There is now compelling evidence that each membrane domain of P-gly ...
... Most eukaryotic multidrug ABC transporters (e.g., Pglycoprotein) comprise four domains which are fused into a single polypeptide. Two of these domains, the transmembrane domains, are hydrophobic and span the membrane multiple times. There is now compelling evidence that each membrane domain of P-gly ...
Effect of rejuvenation hormones on spermatogenesis
... Mechanism of Action Exogenous testosterone inhibits spermatogenesis by suppressing the HPG axis. Specifically, testosterone therapy results in negative feedback on the HPG axis. It inhibits gonadotropinreleasing hormone (GnRH), thereby inhibiting the secretion of follicle-stimulating hormone (FSH) an ...
... Mechanism of Action Exogenous testosterone inhibits spermatogenesis by suppressing the HPG axis. Specifically, testosterone therapy results in negative feedback on the HPG axis. It inhibits gonadotropinreleasing hormone (GnRH), thereby inhibiting the secretion of follicle-stimulating hormone (FSH) an ...
Effects of ()-HA-966, CGS-19755, Phencyclidine, and Dizocilpine on
... key lights, a correct response turned all the keys blue and a correct response in the presence of the blue key lights produced a 0.5-s flash of the hopper light and restarted the cycle in red. On the fifth time through the cycle (FR5), a correct response in the presence of the blue light resulted in ...
... key lights, a correct response turned all the keys blue and a correct response in the presence of the blue key lights produced a 0.5-s flash of the hopper light and restarted the cycle in red. On the fifth time through the cycle (FR5), a correct response in the presence of the blue light resulted in ...
evaluation of the interaction of loratadine and desloratadine with p
... safety record. This result supports some structure-activity relationship studies showing that less lipophilic (hydrophobic) compounds are often less likely to interact with the substrate binding site of P-gp (Klopman et al., 1997; Litman et al., 1997). As DL is the descarboethoxy oxidized L, it is l ...
... safety record. This result supports some structure-activity relationship studies showing that less lipophilic (hydrophobic) compounds are often less likely to interact with the substrate binding site of P-gp (Klopman et al., 1997; Litman et al., 1997). As DL is the descarboethoxy oxidized L, it is l ...
Estrogens, Progestins, and Specific Estrogen
... complex. Gene repression occurs in a ligand-dependent fashion by the recruitment of nuclear corepressor proteins to the transcription complex. This latter effect is an important mechanism of action of estrogen antagonism. Activation of steroid hormone receptors by their cognate ligands proceeds thro ...
... complex. Gene repression occurs in a ligand-dependent fashion by the recruitment of nuclear corepressor proteins to the transcription complex. This latter effect is an important mechanism of action of estrogen antagonism. Activation of steroid hormone receptors by their cognate ligands proceeds thro ...
in silico for prediction of resistance
... abstract | Elucidation of the genetic processes leading to neoplastic transformation has identified cancerpromoting molecular alterations that can be selectively targeted by rationally designed therapeutic agents. Protein kinases are druggable targets and have been studied intensively. New methodolo ...
... abstract | Elucidation of the genetic processes leading to neoplastic transformation has identified cancerpromoting molecular alterations that can be selectively targeted by rationally designed therapeutic agents. Protein kinases are druggable targets and have been studied intensively. New methodolo ...
Novel Agents on the Horizon for Cancer Therapy
... These include monoclonal antibodies such as cetuximab and panitumumab for colorectal cancers, trastuzumab for breast cancers, and small-molecule inhibitors, such as erlotinib, for lung and pancreatic cancers. These anticancer drugs are now readily available to the general oncology community, and rev ...
... These include monoclonal antibodies such as cetuximab and panitumumab for colorectal cancers, trastuzumab for breast cancers, and small-molecule inhibitors, such as erlotinib, for lung and pancreatic cancers. These anticancer drugs are now readily available to the general oncology community, and rev ...
the PDF
... high affinity toward GABAB receptors (IC50 = 2 nM; inhibition of binding of [3H]baclofen to GABAB receptors of cat cerebellum; Bittiger et al., 1988; Froestl et al., 1995a). Due to its 15 times higher potency, high specific binding, and the possibility to carry out filtration assays, [3H]CGP27492 ha ...
... high affinity toward GABAB receptors (IC50 = 2 nM; inhibition of binding of [3H]baclofen to GABAB receptors of cat cerebellum; Bittiger et al., 1988; Froestl et al., 1995a). Due to its 15 times higher potency, high specific binding, and the possibility to carry out filtration assays, [3H]CGP27492 ha ...
Stahl_3rd_ch04_Part2..
... action of the natural neurotransmitter agonist may be desirable. This is the property of an antagonist. Antagonists produce a conformational change in the G protein-linked receptor that causes no change in signal transduction - including no change in whatever amount of any "constitutive" activity th ...
... action of the natural neurotransmitter agonist may be desirable. This is the property of an antagonist. Antagonists produce a conformational change in the G protein-linked receptor that causes no change in signal transduction - including no change in whatever amount of any "constitutive" activity th ...
525_09_lecture2
... •Long history of use •The mechanism was thought to be urine acidification •Now E. coli (other pathogens also) adhesion inhibitors are known to be present but not in other juices. Several proanthocyanidins are likely the active compounds •Need about 8-16 oz (240-480ml) of juice (not drink or cocktail ...
... •Long history of use •The mechanism was thought to be urine acidification •Now E. coli (other pathogens also) adhesion inhibitors are known to be present but not in other juices. Several proanthocyanidins are likely the active compounds •Need about 8-16 oz (240-480ml) of juice (not drink or cocktail ...
No Slide Title
... Useful for structures with unusual substituents Useful for quantifying the biological effects of molecular features that cannot be quantified or tabulated by the Hansch method ...
... Useful for structures with unusual substituents Useful for quantifying the biological effects of molecular features that cannot be quantified or tabulated by the Hansch method ...
Antidepressant specificity of serotonin transporter suggested by three LeuT–SSRI structures Zheng Zhou
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
new-local anaethetic
... The carbonyl group must be conjugated with an aromatic nucleus whereas reversed esters have no local anesthetic activity. The esters of cinnamic acid are more active than those of phenyl acetic acid due to interruption of the extended conjugation by methylene gp between the aromatic ring and carbony ...
... The carbonyl group must be conjugated with an aromatic nucleus whereas reversed esters have no local anesthetic activity. The esters of cinnamic acid are more active than those of phenyl acetic acid due to interruption of the extended conjugation by methylene gp between the aromatic ring and carbony ...
Brexpiprazole II: Antipsychotic-Like and Procognitive Effects of a
... robust clinical activity and to adverse effects related to increased D2 receptor tonus, including nausea, vomiting, insomnia, and motor effects, such as hyperkinesias and restlessness (Fleischhacker, 2005; Casey et al., 2008), whereas excessive D2 antagonist activity results in an increased risk for ...
... robust clinical activity and to adverse effects related to increased D2 receptor tonus, including nausea, vomiting, insomnia, and motor effects, such as hyperkinesias and restlessness (Fleischhacker, 2005; Casey et al., 2008), whereas excessive D2 antagonist activity results in an increased risk for ...
Optimising the Use of p-Adrenoceptor Antagonists in Coronary
... contraindicated. Benefits from P-adrenoceptor antagonists are presumed to be a class effect. However, specific P-adrenoceptor antagonists may provide additional benefits in selected patients, though retrospective analysis of post-Mi trials has not differentiated the specific types of P-adrenoceptor ...
... contraindicated. Benefits from P-adrenoceptor antagonists are presumed to be a class effect. However, specific P-adrenoceptor antagonists may provide additional benefits in selected patients, though retrospective analysis of post-Mi trials has not differentiated the specific types of P-adrenoceptor ...
HU 210: A Potent Tool for Investigations of the Cannabinoid System
... can be classified into at least four groups: classic CBs, bicyclic or nonclassic CBs, aminoalkylindoles, and fatty-acid amines and esters (18,74). HU 210 [(–)3–(1,1-dimethylheptyl)-(–)11-hydroxy-D8-tetrahydrocannabinol] has been synthesized by Mechoulam’s laboratory and belongs to the group of class ...
... can be classified into at least four groups: classic CBs, bicyclic or nonclassic CBs, aminoalkylindoles, and fatty-acid amines and esters (18,74). HU 210 [(–)3–(1,1-dimethylheptyl)-(–)11-hydroxy-D8-tetrahydrocannabinol] has been synthesized by Mechoulam’s laboratory and belongs to the group of class ...
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.