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https://www.readbyqxmd.com/read/28526959/adjuvant-tamoxifen-but-not-aromatase-inhibitor-therapy-decreases-serum-levels-of-the-wnt-inhibitor-dickkopf-1-while-not-affecting-sclerostin-in-breast-cancer-patients
#1
Andy Göbel, Jan D Kuhlmann, Theresa Link, Pauline Wimberger, Andrew J Browne, Martina Rauner, Lorenz C Hofbauer, Tilman D Rachner
PURPOSE: Endocrine therapies, including tamoxifen or aromatase inhibitors, are indispensable for the treatment of patients with estrogen receptor (ER)- and/or progesterone-positive breast cancer. Whereas tamoxifen displays partial ER agonistic effects in bone, aromatase inhibitors increase bone resorption and fracture risk. The Wnt inhibitors dickkopf-1 (DKK-1) and sclerostin negatively impact bone formation and are considered targets for the treatment of bone disorders. However, the effect of endocrine therapies on serum DKK-1 and sclerostin levels in patients with primary breast cancer remains elusive...
May 19, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28521469/licochalcone-e-induces-caspase-dependent-death-of-human-pharyngeal-squamous-carcinoma-cells-through-the-extrinsic-and-intrinsic-apoptotic-signaling-pathways
#2
Sang-Joun Yu, In-A Cho, Kyeong-Rok Kang, Yi-Ra Jung, Seung Sik Cho, Goo Yoon, Ji-Su Oh, Jae-Seek You, Yo-Seob Seo, Gyeong-Je Lee, Sook-Young Lee, Do Kyung Kim, Chun Sung Kim, Su-Gwan Kim, Mi-Ae Jeong, Jae-Sung Kim
The aim of the present study was to investigate licochalcone-E (Lico-E)-induced apoptosis and the associated apoptotic signaling pathway in FaDu cells, a human pharyngeal squamous carcinoma cell line. Treatment with Lico-E exhibited significant cytotoxicity on FaDu cells in a concentration-dependent manner. The IC50 value of Lico-E in FaDu cells was ~50 µM. Treatment with Lico-E increased the number of dead FaDu cells. Furthermore, chromatin condensation, which is associated with apoptotic cell death, was observed in FaDu cells treated with Lico-E for 24 h...
May 2017: Oncology Letters
https://www.readbyqxmd.com/read/28512306/structure-based-docking-studies-towards-exploring-potential-anti-androgen-activity-of-selected-phytochemicals-against-prostate-cancer
#3
Anshika N Singh, Meghna M Baruah, Neeti Sharma
Prostate cancer (PCa) is the second most common malignancy amongst men worldwide. Under PCa maintenance therapy drugs acting as antagonists/partial agonists of hormone receptors against the prostate tissue are used in clinical practices. Prominent drugs being Cyproterone acetate, Flutamide, Bicalutamide, they not only cause acute and long-term toxicity, but also develops drug resistance among patients. Our focus has been on phytochemicals which do not exhibit any cytotoxicity and have significant androgen receptor (AR) inhibition activity...
May 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28512009/combining-d-cycloserine-with-appetitive-extinction-learning-modulates-amygdala-activity-during-recall
#4
Claudia Ebrahimi, Stefan P Koch, Eva Friedel, Ilsoray Crespo, Thomas Fydrich, Andreas Ströhle, Andreas Heinz, Florian Schlagenhauf
Appetitive Pavlovian conditioning plays a crucial role in the pathogenesis of drug addiction and conditioned reward cues can trigger craving and relapse even after long phases of abstinence. Promising preclinical work showed that the NMDA-receptor partial agonist D-cycloserine (DCS) facilitates Pavlovian extinction learning of fear and drug cues. Furthermore, DCS-augmented exposure therapy seems to be beneficial in various anxiety disorders, while the supposed working mechanism of DCS during human appetitive or aversive extinction learning is still not confirmed...
May 13, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28511005/characterization-of-l-theanine-excitatory-actions-on-hippocampal-neurons-towards-the-generation-of-novel-n-methyl-d-aspartate-receptor-modulators-based-on-its-backbone
#5
Fatiha Sebih, Matthieu Rousset, Salima Bellahouel, Marc Rolland, Marie Celeste de Jesus Ferreira, Janique Guiramand, Catherine Cohen-Solal, Gérard Barbanel, Thierry Cens, Mohammed Abouazza, Adrien Tassou, Maud Gratuze, Céline Meunier, Pierre Charnet, Michel Vignes, Valérie Rolland
L-Theanine (or L-γ-N-ethyl-glutamine) is the major amino acid found in Camellia sinensis. It has received much attention because of its pleiotropic physiological and pharmacological activities leading to health benefits in humans, especially. We describe here a new, easy, efficient and environmentally-friendly chemical synthesis of L-Theanine and L-γ-N-propyl-Gln and their corresponding D isomers. L-Theanine, and its derivatives obtained so far, exhibited partial co-agonistic action at N-methyl-D-aspartate (NMDA) receptors, with no detectable agonist effect at other glutamate receptors, on cultured hippocampal neurons...
May 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28509722/rationale-for-nebivolol-valsartan-combination-for-hypertension-review-of-preclinical-and-clinical-data
#6
Thomas D Giles, John R Cockcroft, Bertram Pitt, Abhijeet Jakate, Harold M Wright
: To treat hypertension, combining two or more antihypertensive drugs from different classes is often necessary. β-Blockers and renin-angiotensin-aldosterone system inhibitors, when combined, have been deemed 'less effective' based on partially overlapping mechanisms of action and limited evidence. Recently, the single-pill combination (SPC) of nebivolol (Neb) 5 mg - a vasodilatory β1-selective antagonist/β3 agonist - and valsartan 80 mg, an angiotensin II receptor blocker, was US Food and Drug Administration-approved for hypertension...
May 15, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28503134/aquaporin-4-mediated-glutamate-induced-astrocyte-swelling-is-partially-mediated-through-metabotropic-glutamate-receptor-5-activation
#7
Zhongfang Shi, Wei Zhang, Yang Lu, Yi Lu, Lixin Xu, Qing Fang, Min Wu, Mei Jia, Yujiao Wang, Liping Dong, Xu Yan, Shaohua Yang, Fang Yuan
Astrocytes are one of the most abundant cell types in the mammalian central nervous system (CNS), and astrocyte swelling is the primary event associated with brain edema. Glutamate, the principal excitatory amino acid neurotransmitter in the CNS, is released at high levels after brain injury including cerebral ischemia. This leads to astrocyte swelling, which we previously demonstrated is related to metabotropic glutamate receptor (mGluR) activation. Aquaporin 4 (AQP4), the predominant water channel in the brain, is expressed in astrocyte endfeet and plays an important role in brain edema following ischemia...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28500623/simultaneous-inhibition-of-nmda-and-mglu1-5-receptors-by-levo-corydalmine-in-rat-spinal-cord-attenuates-bone-cancer-pain
#8
Wen-Ling Dai, Bing Yan, Nan Jiang, Juan-Juan Wu, Xiu-Feng Liu, Ji-Hua Liu, Bo-Yang Yu
Bone cancer pain is a challenge for its not completely clarified mechanism and broad clinical morbidity. Therefore, novel and more effective drugs are urgent needed for improvement of patients' quality of life. Glutamate receptors have been associated with the development of the central sensitization of chronic pain. Inhibition of N-methyl-D-aspartate (NMDA) and metabotropic glutamate (mGlu) receptors can effectively attenuate bone cancer pain respectively. Herein, our results indicated that levo-Corydalmine (l-CDL), a compound from Corydalis yanhusuo W...
May 13, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28496466/validated-spectrophtometric-method-for-simultaneous-determination-of-buprenorphine-and-naloxone-in-pharmaceutical-dosage-forms
#9
Effat Souri, Farzaneh Sadat Ahmadi, Maliheh Barazandeh Tehrani, Majid Mohammad Hosseini, Sedigheh Fadaye Vatan
Buprenorphine is a partial mu agonist and kappa antagonist which is used for the treatment of pain and opioid addiction. A mixture of buprenorphine hydrochloride and naloxone hydrochloride has been approved for the treatment of opioid dependence. In this study a third order derivative spectrophotometric method based on zero-crossing technique has been used for the simultaneous determination of buprenorphine hydrochloride and naloxone hydrochloride in tablets. The measurements were carried out at wavelengths of 257...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28496430/cholinergic-nociceptive-mechanisms-in-rat-meninges-and-trigeminal-ganglia-potential-implications-for-migraine-pain
#10
Irina Shelukhina, Nikita Mikhailov, Polina Abushik, Leniz Nurullin, Evgeny E Nikolsky, Rashid Giniatullin
BACKGROUND: Parasympathetic innervation of meninges and ability of carbachol, acetylcholine (ACh) receptor (AChR) agonist, to induce headaches suggests contribution of cholinergic mechanisms to primary headaches. However, neurochemical mechanisms of cholinergic regulation of peripheral nociception in meninges, origin place for headache, are almost unknown. METHODS: Using electrophysiology, calcium imaging, immunohistochemistry, and staining of meningeal mast cells, we studied effects of cholinergic agents on peripheral nociception in rat hemiskulls and isolated trigeminal neurons...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28494312/anagyrine-desensitization-of-peripheral-nicotinic-acetylcholine-receptors-a-potential-biomarker-of-quinolizidine-alkaloid-teratogenesis-in-cattle
#11
Benedict T Green, Stephen T Lee, Kevin D Welch, Daniel Cook
Anagyrine, a teratogenic quinolizidine alkaloid found in Lupinus spp., is proposed to undergo metabolism by pregnant cattle to a piperidine alkaloid which inhibits fetal movement, the putative mechanism behind crooked calf syndrome. The objective of this study was to test the hypothesis that anagyrine but not lupanine or sparteine can directly, without metabolism, desensitize nicotinic acetylcholine receptors (nAChR) in a cell culture model. SH-SY5Y cells expressing autonomic nAChR, and TE-671 cells expressing fetal muscle-type nAChR were exposed to lupine alkaloids or Dimethylphenylpiperazinium (DMPP) in log10 molar increments from 10nM to 100μM and then to a fixed concentration of acetylcholine (ACh) (10μM for SH-SY5Y cells and 1μM for TE-671 cells) and the responses measured with a membrane potential sensing dye to assess nAChR activation and desensitization...
May 2, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28494108/selective-%C3%AE%C2%BA-opioid-receptor-partial-agonist-hs666-produces-potent-antinociception-without-inducing-aversion-after-i-c-v-administration-in-mice
#12
Mariana Spetea, Shainnel O Eans, Michelle L Ganno, Aquilino Lantero, Michael Mairegger, Lawrence Toll, Helmut Schmidhammer, Jay P McLaughlin
BACKGROUND AND PURPOSE: The κ opioid (KOP) receptor has a central role in modulating neurotransmission in central and peripheral neuronal circuits that subserve pain and other behavioural responses. Although KOP agonists do not produce euphoria or lead to respiratory suppression, they induce dysphoria and sedation. We hypothesized that brain-penetrant KOP receptor ligands possessing biased agonism towards G protein signalling over β-arrestin2 recruitment would produce robust antinociception with fewer liabilities of use...
May 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28493341/design-and-validation-of-the-first-cell-impermeant-melatonin-receptor-agonist
#13
Florence Gbahou, Erika Cecon, Guillaume Viault, Romain Gerbier, Frederic Jean-Alphonse, Angeliki Karamitri, Gérald Guillaumet, Philippe Delagrange, Robert M Friedlander, Jean-Pierre Vilardaga, Franck Suzenet, Ralf Jockers
BACKGROUND AND PURPOSE: The paradigm that G protein-coupled receptors are able to prolong or initiate cellular signaling through intracellular receptors recently emerged. Melatonin binds to G protein-coupled MT1 and MT2 receptors. Different from most other hormones targeting GPCRs, melatonin and its synthetic analogs are amphiphilic molecules easily penetrating into cells, but the existence of intracellular receptors is still unclear mainly due to a lack of appropriate tools. EXPERIMENTAL APPROACH: We therefore designed and synthesized a series of hydrophilic melatonin receptor ligands coupled to the Cy3 cyanin fluorophore to reliably monitor its inability of cellular penetration...
May 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28492810/rimonabant-improves-metabolic-parameters-partially-attributed-to-restoration-of-high-voltage-activated-ca2-channels-in-skeletal-muscle-in-hfd-fed-mice
#14
B Chen, N Hu
Cannabinoid type 1 receptor (CB1R) inhibition tends to be one of the promising strategies for the treatment of obesity and other related metabolic disorders. Although CB1R inhibition may cause adverse psychiatric effects including depression and anxiety, the investigation of the role of peripheral CB1R on weight loss and related metabolic parameters are urgently needed. We first explored the effect of rimonabant, a selective CB1R antagonist/inverse agonist, on some metabolic parameters in high fat-diet (HFD)-induced obesity in mice...
May 4, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28489770/degeneration-of-corticofugal-fibers-in-a-patient-with-primary-progressive-freezing-gait-a-case-report
#15
Jeong Pyo Seo, Min Cheol Chang
RATIONALE: To report a patient with primary progressive freezing gait (PPFG) whose degeneration of corticofugal tract (CFT) from the supplementary motor area (SMA) was demonstrated using diffusion tensor tractography (DTT). PATIENT CONCERNS: A 66-year-old woman presented with a solitary symptom of a sudden transient break on walking (i.e., freezing gait), which slowly progressed for 4 years. DIAGNOSES: Imaging evidence using magnetic resonance imaging and F-florinated-N-3-fluoropropyl-2-β-carboxymethoxy-3-β-(4-lodophenyl) nortropane positron emission tomography scanning was unremarkable, and our patient's symptom was not affected by dopamine agonist medication...
May 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28488817/neladenoson-bialanate-hydrochloride-a-prodrug-of-a-partial-adenosine%C3%A2-a1-receptor-agonist-for-the-chronic-treatment-of-heart-diseases
#16
Daniel Meibom, Barbara Albrecht-Küpper, Nicole Diedrichs, Walter Hübsch, Raimund Kast, Thomas Krämer, Ursula Krenz, Hans-Georg Lerchen, Joachim Mittendorf, Peter G Nell, Frank Süssmeier, Alexandros Vakalopoulos, Katja Zimmermann
Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A1 receptors (A1 Rs) has been shown to inhibit myocardial pathologies associated with ischemia and reperfusion injury, suggesting several options for new cardiovascular therapies. When full A1 R agonists are used, the desired protective and regenerative cardiovascular effects are usually overshadowed by unintended pharmacological effects such as induction of bradycardia, atrioventricular (AV) blocks, and sedation...
May 10, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28485590/structure-activity-relationship-of-2-4-dichloro-n-3-5-dichloro-4-quinolin-3-yloxy-phenyl-benzenesulfonamide-int131-analogs-for-ppar%C3%AE-targeted-antidiabetics
#17
Rebecca L Frkic, Beatriz B Rodriguez, Mi Ra Chang, Dana Kuruvilla, Anthony Ciesla, Andrew D Abell, Theodore M Kamenecka, Patrick R Griffin, John B Bruning
Peroxisome Proliferator-Activated Receptor γ (PPARγ) is a nuclear receptor central to fatty acid and glucose homeostasis. PPARγ is the molecular target for type 2 diabetes mellitus (T2DM) therapeutics TZDs (thiazolidinediones), full agonists of PPARγ with robust antidiabetic properties, which are confounded with significant side effects. Partial agonists of PPARγ such as INT131 (1), have displayed similar insulin-sensitizing efficacy as TZDs, but lack many side-effects. To probe the structure-activity relationship (SAR) of the scaffold 1, we synthesized 14 analogs of compound 1 which revealed compounds with higher transcriptional potency for PPARγ and identification of moieties of the scaffold 1 key to high transcriptional potency...
May 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28478994/emerging-paradigms-of-g-protein-coupled-receptor-dephosphorylation
#18
REVIEW
Andrea Kliewer, Rainer K Reinscheid, Stefan Schulz
Elucidation of the molecular mechanisms underlying G protein-coupled receptor (GPCR) dephosphorylation remains a major challenge. While specific GPCR phosphatases (GRPs) have eluded identification, prevailing models propose that receptors must first internalize into acidic endosomes to become dephosphorylated in a housekeeping-like process. Recently, phosphosite-specific antibodies, combined with siRNAs targeting specific phosphatase transcripts, have facilitated the identification of distinct protein phosphatase 1 (PP1) and PP2 catalytic subunits as bona fide GRPs...
May 4, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28478801/involvement-of-trpc1-in-nampt-induced-cardiomyocyte-hypertrophy-through-the-activation-of-er-stress
#19
J Li, W Wu, M Zhao, X Liu
Nicotinamide phosphoribosyltransferase (Nampt) is involved in the development of cardiac hypertrophy. Transient receptor potential canonical channel 1 (TRPC1) and endoplasmic reticulum stress (ER stress) are regarded as critical pathways in cardiac hypertrophy. Therefore, we hypothesizedthat TRPC1 might be associated with ER stress in Nampt-induced cardiac hypertrophy. CulturedH9c2cardiomyocyteswereexposed to Namptfor different timesand the expression of markers of cardiomyocyte hypertrophy and ER stress, as well as TRPC1 were detected...
April 29, 2017: Cellular and Molecular Biology
https://www.readbyqxmd.com/read/28478771/evaluation-of-the-long-term-safety-and-tolerability-of-cariprazine-in-patients-with-schizophrenia-results-from-a-1-year-open-label-study
#20
Andrew J Cutler, Suresh Durgam, Yao Wang, Raffaele Migliore, Kaifeng Lu, István Laszlovszky, György Németh
OBJECTIVE: Cariprazine, a dopamine D3/D2 partial agonist atypical antipsychotic with preferential binding to D3 receptors, is approved for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder. The efficacy and safety of cariprazine was established in three randomized, double-blind, placebo-controlled, 6-week trials in patients with acute exacerbation of schizophrenia. This 53-week study evaluated the long-term safety and tolerability of cariprazine in patients with schizophrenia...
May 8, 2017: CNS Spectrums
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