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https://www.readbyqxmd.com/read/28647729/analgesic-effects-of-diluted-bee-venom-acupuncture-mediated-by-%C3%AE-opioid-and-%C3%AE-2-adrenergic-receptors-in-osteoarthritic-rats
#1
Jeong-Eun Huh, Byung-Kwan Seo, Jung-Woo Lee, Yeon-Cheol Park, Yong-Hyeon Baek
Context • Pain from osteoarthritis is associated with peripheral nociception and central pain processing. Given the unmet need for innovative, effective, and well-tolerated therapies, many patients, after looking for more satisfactory alternatives, decide to use complementary and alternative modalities. The analgesic mechanism of subcutaneous injections of diluted bee venom into an acupoint is thought to be part of an anti-inflammatory effect and the central modulation of pain processing. Objectives • Using the rat model of collagenase-induced osteoarthritis (CIOA), the study intended to investigate the analgesic effects of bee venom acupuncture (BVA) as they are related to the acupuncture points and dosage used and to determine whether the analgesic mechanisms of BVA for pain were mediated by opioid or adrenergic receptors...
June 23, 2017: Alternative Therapies in Health and Medicine
https://www.readbyqxmd.com/read/28647677/buprenorphine-augmentation-improved-symptoms-of-ocd-compared-to-placebo-results-from-a-randomized-double-blind-and-placebo-controlled-clinical-trial
#2
Mohammad Ahmadpanah, Amin Reihani, Ali Ghaleiha, Alireza Soltanian, Mohammad Haghighi, Leila Jahangard, Dena Sadeghi Bahmani, Edith Holsboer-Trachsler, Serge Brand
BACKGROUND: In the search for new psychopharmacologic options in the treatment of obsessive-compulsive disorders (OCD), some findings suggested that augmentation with buprenorphine, a partial-opioid agonist used to treat opioid addiction, moderate acute pain and moderate chronic pain, is worthy of consideration. Accordingly, to explore this possibility further, a double-blinded, placebo-controlled clinical trial was performed. METHOD: A total of 43 patients (mean age: 34...
June 13, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28645860/gper-agonist-dilates-mesenteric-arteries-via-pi3k-akt-enos-and-potassium-channels-in-both-sexes
#3
Pollyana Peixoto, Rosária Dias Aires, Virgínia Soares Lemos, Nazaré Souza Bissoli, Roger Lyrio Dos Santos
AIM: The action of oestrogen has traditionally been attributed to the activation of nuclear receptors (ERα and ERβ). A third receptor, the G protein-coupled oestrogen receptor (GPER), has been described as mediator of the rapid action of oestrogen. Based on the possible protective role of oestrogen in the cardiovascular system, the present study was designed to determine whether selective GPER activation induces relaxation of mesenteric resistance arteries in both sexes and which signalling pathways are involved...
June 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28644418/new-mt%C3%A2-melatonin-receptor-selective-ligands-agonists-and-partial-agonists
#4
Jean A Boutin, Anne Bonnaud, Chantal Brasseur, Olivier Bruno, Nolwenn Lepretre, Peter Oosting, Sophie Coumailleau, Philippe Delagrange, Olivier Nosjean, Céline Legros
The search for melatonin receptor agonists and antagonists specific towards one of the receptor subtypes will extend our understanding of the role of this system in relaying circadian information to the body. A series of compounds derived from a hit compound discovered in a screening process led to powerful agonists specific for one of the isoform of the melatonin receptor namely, MT₂. The compounds are based on a poorly explored skeleton in the molecular pharmacology of melatonin. By changing the steric hindrance of one substituent (i...
June 23, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28641524/the-bio-psycho-social-dimension-in-women-s-sexual-desire-argumentum-ad-novitatem
#5
Nur Syazwani Roslan, Nik Ruzyanei Nik Jaafar, Hatta Sidi, Najwa Baharuddin, Jaya Kumar, Srijit Das, Nik Hazlina Nik Hussein
Sexual desire includes complex motivation and drive. In the context of biological and cognitive-emotive state art of science, it is often a neglected field in medicine. With regard to the treatment, study on women's sexual function received less attention compared to the men's sexuality. In the past, this endeavor was relatively not well disseminated in the scientific community. Recently, there was a revolutionized surge of drug targets available to treat women with low sexual desire. It is timely to review the relevant biological approach, especially in the context of pharmacotherapy to understand this interesting clinical entity which was modulated by numerous interactive psychosocial inter-play and factors...
June 21, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28641517/the-case-for-cannabinoid-cb1-receptors-as-a-target-for-bronchodilator-therapy-for-%C3%AE-agonist-resistant-asthma
#6
John Ashton, Robert J Hancox
Although b2-receceptor agonists are powerful bronchodilators and are at the forefront of asthma symptom relief, patients who use them frequently develop partial resistance to them. This can be a particularly serious problem during severe attacks, where high dose b2-agonist treatment is the front line therapy. Alternative bronchodilators are urgently needed. In this article we review the evidence for the bronchodilator effects of the cannabinoid CB1 receptor tetrahydrocannabinol (THC) and suggest that the mechanism of action for these effects are sufficiently independent of the mechanisms of standard bronchodilators to warrant clinical investigation...
June 15, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28637021/dectin-1-signaling-inhibits-osteoclastogenesis-via-il-33-induced-inhibition-of-nfatc1
#7
Xiaoqing Zhu, Yinghua Zhao, Yuxue Jiang, Tianxue Qin, Jintong Chen, Xiao Chu, Qing Yi, Sujun Gao, Siqing Wang
Abnormal osteoclast activation contributes to osteolytic bone diseases (OBDs). It was reported that curdlan, an agonist of dectin-1, inhibits osteoclastogenesis. However, the underlying mechanisms are not fully elucidated. In this study, we found that curdlan potently inhibited RANKL-induced osteoclast differentiation and the resultant bone resorption. Curdlan inhibited the expression of nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1), the key transcriptional factor for osteoclastogenesis. Notably, dectin-1 activation increased the expression of MafB, an inhibitor of NFATc1, and IL-33 in osteoclast precursors...
June 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28634283/phase-ib-study-of-utomilumab-pf-05082566-a-4-1bb-cd137-agonist-in-combination-with-pembrolizumab-mk-3475-in-patients-with-advanced-solid-tumors
#8
Anthony W Tolcher, Mario Sznol, Siwen Hu-Lieskovan, Kyriakos P Papadopoulos, Amita Patnaik, Drew Rasco, Donna Di Gravio, Bo Huang, Dhiraj Gambhire, Ying Chen, Aron Thall, Nuzhat Pathan, Emmett V Schmidt, Laura Q M Chow
Purpose:  This phase Ib study (NCT02179918) evaluated the safety, antitumor activity, pharmacokinetics, and pharmacodynamics of utomilumab, a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137 in combination with the humanized, PD-1-blocking IgG4 mAb pembrolizumab in patients with advanced solid tumors. <p>Experimental Design:  Utomilumab (0.45-5.0 mg/kg) and pembrolizumab (2 mg/kg) were administered intravenously every 3 weeks. Utomilumab dose escalation was conducted using the time-to-event-continual reassessment method...
June 20, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28632301/regulation-of-kindling-epileptogenesis-by-hippocampal-toll-like-receptors-2
#9
Jesús-Servando Medel-Matus, Ashley Reynolds, Don Shin, Raman Sankar, Andrey Mazarati
This study examined whether Toll-like receptors 2 (TLR2) contribute to rapid kindling epileptogenesis. A TLR2 agonist, lipoteichoic acid (LTA), LTA antibody (LTA-A), or normal saline (control) was administered daily over 3 consecutive days, unilaterally into ventral hippocampus of adult male Wistar rats. Thirty minutes after the last injection, the animals were subjected to a rapid kindling procedure. The ictogenesis was gauged by comparing afterdischarge threshold (ADT) and afterdischarge duration (ADD) before the treatments, after the treatments prior to kindling, and 24 h after kindling...
June 20, 2017: Epilepsia
https://www.readbyqxmd.com/read/28632204/successful-pharmacotherapy-for-the-treatment-of-severe-feeding-aversion-with-mechanistic-insights-from-cross-species-neuronal-remodeling
#10
W G Sharp, A G Allen, K H Stubbs, K K Criado, R Sanders, C E McCracken, R G Parsons, L Scahill, S L Gourley
Pediatric feeding disorders affect up to 5% of children, causing severe food intake problems that can result in serious medical and developmental outcomes. Behavioral intervention (BI) is effective in extinguishing feeding aversions, and also expert-dependent, time/labor-intensive and not well understood at a neurobiological level. Here we first conducted a double-blind, placebo-controlled trial comparing BI with BI plus d-cycloserine (DCS). DCS is a partial N-methyl-d-aspartate (NMDA) receptor agonist shown to augment extinction therapies in multiple anxiety disorders...
June 20, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#11
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28629518/analysis-of-the-asymmetry-of-activated-epo-receptor-enables-designing-small-molecule-agonists
#12
Frank Guarnieri
Amgen solved the high-resolution cocrystal structure of erythropoietin (EPO) bound to the extracellular part of the receptor (EPOR) in 1998, which reveals that the EPO-EPOR interaction surface is formed by 11 salt bridges, 17 H-bonds, and 2 hydrophobic clusters centered at a pair of crucial phenylalanines (F93). The EPOR has two domains, one that penetrates the membrane and a second extracellular domain that forms one arm of the binding site for the EPO ligand. The complete competent receptor-binding site is a homodimer of EPOR with the two arms forming a funnel-shaped cup where EPO binds...
2017: Vitamins and Hormones
https://www.readbyqxmd.com/read/28623169/mutation-of-the-inhibitory-ethanol-site-in-gabaa-%C3%AF-1-receptors-promotes-tolerance-to-ethanol-induced-motor-incoordination
#13
Yuri A Blednov, Cecilia M Borghese, Carlos I Ruiz, Madeline A Cullins, Adriana Da Costa, Elizabeth A Osterndorff-Kahanek, Gregg E Homanics, R Adron Harris
Genes encoding the ρ1/2 subunits of GABAA receptors have been associated with alcohol (ethanol) dependence in humans, and ρ1 was also shown to regulate some of the behavioral effects of ethanol in animal models. Ethanol inhibits GABA-mediated responses in wild-type (WT) ρ1, but not ρ1(T6'Y) mutant receptors expressed in Xenopus laevis oocytes, indicating the presence of an inhibitory site for ethanol in the second transmembrane helix. In this study, we found that ρ1(T6'Y) receptors expressed in oocytes display overall normal responses to GABA, the endogenous GABA modulator (zinc), and partial agonists (β-alanine and taurine)...
June 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28619359/postpartum-estrogen-withdrawal-impairs-gabaergic-inhibition-and-ltd-induction-in-basolateral-amygdala-complex-via-down-regulation-of-gpr30
#14
Rong Yang, Baofeng Zhang, Tingting Chen, Suyun Zhang, Ling Chen
Postpartum estrogen (E2) withdrawal is known to be a particularly vulnerable time for depressive symptoms. In this study, ovariectomized (OVX) mice were treated with co-administration of estradiol benzoate and progesterone (E2/P4) followed by administration of E2 alone (E2) and a subsequent E2 withdrawal (EW) to mimic the hormonal changes during pregnancy and postpartum. The objective of this study was to investigate the influence of E2 withdrawal after hormone-simulated pregnancy on synaptic function and plasticity in basolateral amygdala complex (BLA)...
June 13, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28610629/the-use-of-imepitoin-pexion%C3%A2-on-fear-and-anxiety-related-problems-in-dogs-a-case-series
#15
Kevin J McPeake, Daniel S Mills
BACKGROUND: Fear and anxiety based problems are common in dogs. Alongside behaviour modification programmes, a range of psychopharmacological agents may be recommended to treat such problems, but few are licensed for use in dogs and the onset of action of some can be delayed. The low affinity partial benzodiazepine receptor agonist imepitoin (Pexion™, Boehringer Ingelheim) is licensed for treating canine epilepsy, has a fast onset of action in dogs and has demonstrated anxiolytic properties in rodent models...
June 13, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/28607487/single-molecule-analysis-of-ligand-efficacy-in-%C3%AE-2ar-g-protein-activation
#16
G Glenn Gregorio, Matthieu Masureel, Daniel Hilger, Daniel S Terry, Manuel Juette, Hong Zhao, Zhou Zhou, Jose Manuel Perez-Aguilar, Maria Hauge, Signe Mathiasen, Jonathan A Javitch, Harel Weinstein, Brian K Kobilka, Scott C Blanchard
G-protein-coupled receptor (GPCR)-mediated signal transduction is central to human physiology and disease intervention, yet the molecular mechanisms responsible for ligand-dependent signalling responses remain poorly understood. In class A GPCRs, receptor activation and G-protein coupling entail outward movements of transmembrane helix 6 (TM6). Here, using single-molecule fluorescence resonance energy transfer imaging, we examine TM6 movements in the β2 adrenergic receptor (β2AR) upon exposure to orthosteric ligands with different efficacies, in the absence and presence of the Gs heterotrimer...
June 7, 2017: Nature
https://www.readbyqxmd.com/read/28604329/report-on-the-first-government-funded-opioid-substitution-programme-for-heroin-users-in-the-western-cape-province-south-africa
#17
Graeme Michie, Shuaib Hoosain, Muiruri Macharia, Lize Weich
BACKGROUND: Although pharmacological opioid substitution treatment (OST) is a well-established treatment modality for heroin addiction, it is a relatively recent introduction in low- and middle-income countries. OBJECTIVE: To report on a pilot OST programme initiated in 2013 that was the only public-funded programme in South Africa (SA) at the time. Participants were offered standard care only (n=68) or, for the OST group (n=67), standard care plus Suboxone (Reckitt Benckiser), a synthetic partial opioid agonist, in a 12-week clinician-monitored programme...
May 24, 2017: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
https://www.readbyqxmd.com/read/28603630/a-three-parameter-two-state-model-of-receptor-function-that-incorporates-affinity-efficacy-and-signal-amplification
#18
Peter Buchwald
A generalized model of receptor function is proposed that relies on the essential assumptions of the minimal two-state receptor theory (i.e., ligand binding followed by receptor activation), but uses a different parametrization and allows nonlinear response (transduction) for possible signal amplification. For the most general case, three parameters are used: Kd, the classic equilibrium dissociation constant to characterize binding affinity; ε, an intrinsic efficacy to characterize the ability of the bound ligand to activate the receptor (ranging from 0 for an antagonist to 1 for a full agonist); and γ, a gain (amplification) parameter to characterize the nonlinearity of postactivation signal transduction (ranging from 1 for no amplification to infinity)...
June 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28602099/zerumbone-regulates-dna-repair-responding-to-ionizing-radiation-and-enhances-radiosensitivity-of-human-prostatic-cancer-cells
#19
Pai-Kai Chiang, Wei-Kung Tsai, Marcelo Chen, Wun-Rong Lin, Yung-Chiong Chow, Chih-Chiao Lee, Jong-Ming Hsu, Yu-Jen Chen
INTRODUCTION: Radiation therapy using ionizing radiation is widely used for the treatment of prostate cancer. The intrinsic radiation sensitivity of cancer cells could be enhanced by modulating multiple factors including the capacity to repair DNA damage, especially double-strand breaks (DSBs). We aimed to examine the effect of zerumbone on radiation sensitivity and its protective effects against ionizing radiation-induced DSB in human prostate cancer cells. MATERIALS AND METHODS: The human prostate cancer PC3 and DU145 cell lines were used...
June 1, 2017: Integrative Cancer Therapies
https://www.readbyqxmd.com/read/28600049/intravenous-leiomyomatosis-of-the-uterus-a-clinicopathological-analysis-of-nine-cases-and-literature-review
#20
Hui-Ying Low, Yu Zhao, Kuo-Shu Huang, Huang-Pin Shen, Pei-Ju Wu, Chih-Jen Tseng
OBJECTIVE: Intravenous/intravascular leiomyomatosis is characterized by intravenous proliferation of a histologically benign smooth muscle cell tumor mass that is non-tissue-invasive. Although benign, intravenous leiomyomatosis may cause remarkable systematic complications, presents significant diagnostic difficulties, and also is characterized by a relatively increased possibility of recurrence. We determine patients' characteristics, and recurrence and treatment of intravenous leiomyomatosis...
June 2017: Taiwanese Journal of Obstetrics & Gynecology
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