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https://www.readbyqxmd.com/read/27908790/mpp-inhibits-mglur1-5-mediated-long-term-depression-in-mouse-hippocampus-by-calpain-activation
#1
Junyao Li, Hui Chen, Shengbing Wu, Yuefa Cheng, Qinglin Li, Jing Wang, Guoqi Zhu
Neurotoxins are harmful to nervous system and cause either neuronal cell death or impairment of synaptic activity, which contributes to Parkinson's disease or other neuronal disorders. Hippocampal synaptic plasticity was proposed as a cellular model for memory processing. In this study, we reported a novel effect of neurotoxin, 1-methyl-4-phenylpyridinium (MPP(+)), on metabotropic glutamate receptor 1/5 agonist, 3,5-dihydroxyphenylglycine (DHPG)-induced hippocampal synaptic plasticity, and MPP(+) incubation blocked DHPG-induced hippocampal long-term depression (LTD) in Schaffer collateral-CA1 synapses...
November 28, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27903101/d-cycloserine-an-nmda-glutamate-receptor-glycine-site-partial-agonist-induces-acute-increases-in-brain-glutamate-plus-glutamine-and-gaba-comparable-to-ketamine
#2
Joshua T Kantrowitz, Matthew S Milak, Xiangling Mao, Dikoma C Shungu, J John Mann
No abstract text is available yet for this article.
December 1, 2016: American Journal of Psychiatry
https://www.readbyqxmd.com/read/27900462/effects-of-a-trpv1-agonist-capsaicin-on-respiratory-rhythm-generation-in-brainstem-spinal-cord-preparation-from-newborn-rats
#3
Mariho Tani, Sayumi Kotani, Chikara Hayakawa, Shih-Tien Lin, Saki Irie, Keiko Ikeda, Kiyoshi Kawakami, Hiroshi Onimaru
The heat-sensitive transient receptor potential vanilloid 1 (TRPV1) channels are expressed in the peripheral and central nervous systems. However, there is no report on how the activation of TRPV1 causes the modulation of neuronal activity in the medullary respiratory center. We examined effects of capsaicin, a specific agonist of TRPV1 channels, on respiratory rhythm generation in brainstem-spinal cord preparation from newborn rats. Capsaicin induced a biphasic response in the respiratory rhythm (a transient decrease followed by an increase in the C4 rate)...
November 29, 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27898948/%C3%AE-and-%C3%AE-adrenergic-receptors-stimulation-relaxes-porcine-myometrium-in-the-peri-implantation-period
#4
W Markiewicz, J J Jaroszewski
These studies were to demonstrate whether the β-receptor is involved in regulating the contractility of the swine myometrium in the peri-implantation period and to compare a relaxing activity of selective β- and β-adrenergic agonists (salbutamol and BRL 37344, respectively). Myometrial strips were collected form the gilts ( = 8) on d 12 to 14 of pregnancy. Changes in the contractility of myometrial strips were assessed further to the administration of increasing concentrations of the agonists (10 to 10 ) with and without β-adrenergic receptor antagonists: butoxamine, propranolol, and bupranolol at 10 ...
November 2016: Journal of Animal Science
https://www.readbyqxmd.com/read/27897273/a-novel-therapeutic-peptide-as-a-partial-agonist-of-rankl-in-ischemic-stroke
#5
Hitomi Kurinami, Munehisa Shimamura, Hironori Nakagami, Hideo Shimizu, Hiroshi Koriyama, Tomohiro Kawano, Kouji Wakayama, Hideki Mochizuki, Hiromi Rakugi, Ryuichi Morishita
The enhanced receptor activator of nuclear factor-κB (NFκB) ligand (RANKL) and its receptor (RANK) signal have been reported to attenuate ischemic brain injury through inhibition of Toll-like receptor (TLR) 4-mediated inflammation. However, augmentation of the RANKL/RANK signal also accelerates osteoporosis, which is a potential problem in clinical use of RANKL. Therefore, we developed novel peptides, microglial healing peptides (MHPs), which were based on the DE and/or EF loop of RANKL. Among them, MHP1 was the most effective inhibitor of TLR4-induced inflammations in microglia/macrophages...
November 29, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27896372/opioid-receptor-agonists-may-favorably-affect-bone-mechanical-properties-in-rats-with-estrogen-deficiency-induced-osteoporosis
#6
Aleksandra Janas, Joanna Folwarczna
The results of epidemiological, clinical, and in vivo and in vitro experimental studies on the effect of opioid analgesics on bone are inconsistent. The aim of the present study was to investigate the effect of morphine (an agonist of opioid receptors), buprenorphine (a partial μ opioid receptor agonist and κ opioid receptor antagonist), and naloxone (an antagonist of opioid receptors) on the skeletal system of female rats in vivo. The experiments were carried out on 3-month-old Wistar rats, divided into two groups: nonovariectomized (intact; NOVX) rats and ovariectomized (OVX) rats...
November 28, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27895119/partial-agonist-and-biased-signaling-properties-of-the-synthetic-enantiomers-j113863-ucb35625-at-chemokine-receptors-ccr2-and-ccr5
#7
Jenny Corbisier, Alexandre Huszagh, Céline Galés, Marc Parmentier, Jean-Yves Springael
Biased agonism at G protein coupled receptors constitutes a promising area of research for the identification of new therapeutic molecules. In this study, we identified two novel biased ligands for the chemokine receptors CCR2 and CCR5 and characterized their functional properties. We showed that J113863 and its enantiomer UCB35625, initially identified as high-affinity antagonists for CCR1 and CCR3, also bind with low affinity to the closely related receptors CCR2 and CCR5. Binding of J113863 and UCB35625 to CCR2 or CCR5 resulted in the full or partial activation of the three Gi proteins and the two Go isoforms...
November 28, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27894797/roles-of-the-serotonin-5-ht4-receptor-in-dendrite-formation-of-the-rat-hippocampal-neurons-in-vitro
#8
Naoki Kozono, Akiko Ohtani, Takashi Shiga
Serotonin (5-HT) is involved in various aspects of hippocampal development, although the specific roles of 5-HT receptors are poorly understood. We investigated the roles of 5-HT receptors in the dendrite formation of hippocampal neurons. We focused on the 5-HT4 receptor, which is coupled with Gs protein, and compared the effects with those of the Gi-coupled 5-HT1A receptor. Neurons from rat hippocampi at embryonic day 18 were dissociated and treated for 4 days with the 5-HT4 receptor agonist BIMU8 or the 5-HT1A receptor agonist 8-OH DPAT...
November 25, 2016: Brain Research
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#9
Jocelien D A Olivier, Diana C Esquivel Franco, Ronald Oosting, Marcel Waldinger, Zoltan Sarnyai, Berend Olivier
Tramadol is a well-known and effective analgesic. Recently it was shown that tramadol is also effective in human premature ejaculation. The inhibitory effect of tramadol on the ejaculation latency is probably due to its mechanism of action as a μ-opioid receptor agonist and noradrenaline/serotonin (5-HT) reuptake inhibitor. In order to test this speculation, we tested several doses of tramadol in a rat model of male sexual behavior and investigated two types of drugs interfering with the μ-opioid and the 5-HT system...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27890450/src2-3-binds-to-vitamin-d-receptor-with-high-sensitivity-and-strong-affinity
#10
Daichi Egawa, Toshimasa Itoh, Akira Kato, Saori Kataoka, Yasuaki Anami, Keiko Yamamoto
Vitamin D receptor (VDR) is a member of the nuclear receptor superfamily and regulates the expression of target genes through ligand binding. To express the target gene, coactivator binding to the VDR/ligand complex is essential. Although there are many coactivators in living cells, precise interactions between coactivators and VDR have not been clarified. Here, we synthesized two coactivator peptides, DRIP205-2 and SRC2-3, evaluated their affinity for the ligand-binding domain (LBD) of VDR using 1α,25-dihydroxyvitamin D3, partial agonist 1, and antagonist 2 by surface plasmon resonance (SPR), and assessed their interaction modes with VDR-LBD using X-ray crystallographic analysis...
November 14, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27886063/d-lysergic-acid-diethylamide-lsd-as-a-model-of-psychosis-mechanism-of-action-and-pharmacology
#11
REVIEW
Danilo De Gregorio, Stefano Comai, Luca Posa, Gabriella Gobbi
d-Lysergic Acid Diethylamide (LSD) is known for its hallucinogenic properties and psychotic-like symptoms, especially at high doses. It is indeed used as a pharmacological model of psychosis in preclinical research. The goal of this review was to understand the mechanism of action of psychotic-like effects of LSD. We searched Pubmed, Web of Science, Scopus, Google Scholar and articles' reference lists for preclinical studies regarding the mechanism of action involved in the psychotic-like effects induced by LSD...
November 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27882537/neurochemical-and-behavioral-effects-of-hypidone-hydrochloride-yl-0919-a-novel-combined-selective-serotonin-reuptake-inhibitor-and-partial-5-ht1a-agonist
#12
Li-Ming Zhang, Xiao-Yun Wang, Nan Zhao, Yu-Lu Wang, Xiao-Xu Hu, Yu-Hua Ran, Yan-Qin Liu, You-Zhi Zhang, Ri-Fang Yang, Yun-Feng Li
The purpose of the present study was to investigate the pharmacology of hypidone hydrochloride (YL-0919), a novel selective serotonin reuptake inhibitor (SSRI) and 5-hydroxytryptamine (5-HT)1A receptor agonist with high affinity for serotonin transporter (SERT) and 5-HT1A receptors. YL-0919 promoted [(35) S]GTPγ S binding at 85% of the magnitude of the full 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), suggesting that YL-0919 is a high-efficacy partial agonist of 5-HT1A receptors...
November 24, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27880981/a-novel-glucagon-like-peptide-1-glucagon-receptor-dual-agonist-improves-steatohepatitis-and-liver-regeneration-in-mice
#13
M Pilar Valdecantos, Virginia Pardo, Laura Ruiz, Luis Castro-Sánchez, Borja Lanzón, Elisa Fernández-Millán, Carmelo García-Monzón, Ana I Arroba, Águeda González-Rodríguez, Fernando Escrivá, Álvarez Carmen, Francisco J Rupérez, Coral Barbas, Anish Konkar, Jacqui Naylor, David Hornigold, Ana Dos Santos, Maria Bednarek, Joseph Grimsby, Cristina M Rondinone, Ángela M Valverde
BACKGROUND AND AIMS: Since non-alcoholic steatohepatitis (NASH) is associated with impaired liver regeneration, we investigated the effects of G49, a dual glucagon-like peptide-1(GLP-1)/glucagon (GCG) receptor agonist, on NASH and hepatic regeneration. METHODS: C57Bl/6 mice fed chow or methionine and choline-deficient (MCD) diet for one week were divided into 4 groups: C (chow diet), MCD (MCD diet), C+G49 (chow diet plus G49) and M+G49 (MCD diet plus G49). Mice fed high fat diet (HFD) for 10 weeks were divided in groups: HFD and H+G49 (HFD plus G49)...
November 23, 2016: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/27880803/wdr68-mediates-dorsal-and-ventral-patterning-events-for-craniofacial-development
#14
Estibaliz Alvarado, Mina Yousefelahiyeh, Greg Alvarado, Robin Shang, Taryn Whitman, Andrew Martinez, Yang Yu, Annie Pham, Anish Bhandari, Bingyan Wang, Robert M Nissen
Birth defects are among the leading causes of infant mortality and contribute substantially to illness and long-term disability. Defects in Bone Morphogenetic Protein (BMP) signaling are associated with cleft lip/palate. Many craniofacial syndromes are caused by defects in signaling pathways that pattern the cranial neural crest cells (CNCCs) along the dorsal-ventral axis. For example, auriculocondylar syndrome is caused by impaired Endothelin-1 (Edn1) signaling, and Alagille syndrome is caused by defects in Jagged-Notch signaling...
2016: PloS One
https://www.readbyqxmd.com/read/27879191/replacement-of-sfc-dpi-with-sfc-mdi-exhaled-through-the-nose-improved-eosinophilic-chronic-rhinosinusitis-with-bronchial-asthma%C3%A2
#15
Yoshiki Kobayashi, Mikiya Asako, Takahisa Yamamoto, Hirotaka Yasuba, Koichi Tomoda, Akira Kanda
OBJECTIVE: Eosinophilic chronic rhinosinusitis (ECRS), a subgroup of chronic rhinosinusitis with nasal polyps, is a refractory disease closely associated with bronchial asthma. We recently reported on the efficacy of ultra-fine particle inhaled corticosteroids (ICS) (hydrofluoroalkane-134a-beclomethasone dipropionate: HFA-BDP) exhalation through the nose (ETN) treatment for mild-to-moderate asthmatics with ECRS. However, the effect of HFA-BDP ETN was found to be transient in some cases with severe ECRS and asthma, requiring treatment with higher-dose ICS and long-acting β2-agonists (LABA)...
November 23, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27876620/the-gabab-positive-allosteric-modulators-cgp7930-and-gs39783-stimulate-erk1-2-signalling-in-cells-lacking-functional-gabab-receptors
#16
Maria C Olianas, Simona Dedoni, Pierluigi Onali
The present study shows that the GABAB positive allosteric modulators (PAMs) CGP7930 and GS39783 stimulate extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) signalling in cells that do not express functional GABAB receptors. In human SH-SY5Y neuroblastoma cells, CGP7930 and GS39783 induced a time- and concentration-dependent increase in ERK1/2 phosphorylation with potencies similar to those displayed as GABAB PAMs. Conversely, γ-aminobutyric acid and the GABAB receptor agonists (-)baclofen and SKF97541 were completely inactive...
November 19, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27873143/regulation-of-rac1-gtpase-activity-by-quinine-through-g-protein-and-bitter-taste-receptor-t2r4
#17
Crystal Sidhu, Appalaraju Jaggupilli, Prashen Chelikani, Rajinder P Bhullar
Rac1 belongs to the Rho family of small GTPases and regulates actin cytoskeleton reorganization. T2R4 is a bitter taste receptor belonging to the G protein-coupled receptor family of proteins. In addition to mediating bitter taste perception from the tongue, T2R4s are found in extra-oral tissues, e.g., nasal epithelium, airways, brain, testis suggesting a much broader physiological function for these receptors. Anti-malarial drug and a bitter tasting compound, quinine, is a known agonist for T2R4, whereas BCML (Nα,Nα-Bis(carboxymethyl)-L-lysine) acts as an inverse agonist...
November 22, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27867511/is-tapentadol-different-from-classical-opioids-a-review-of-the-evidence
#18
Richard M Langford, Roger Knaggs, Paul Farquhar-Smith, Anthony H Dickenson
Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain...
November 2016: British Journal of Pain
https://www.readbyqxmd.com/read/27865645/discovery-of-smp-304-a-novel-benzylpiperidine-derivative-with-serotonin-transporter-inhibitory-activity-and-5-ht1a-weak-partial-agonistic-activity-showing-the-antidepressant-like-effect
#19
Hidefumi Yoshinaga, Shuji Masumoto, Koji Koyama, Naoya Kinomura, Yuji Matsumoto, Taro Kato, Satoko Baba, Kenji Matsumoto, Tomoko Horisawa, Hitomi Oki, Kazuki Yabuuchi, Toru Kodo
We report the discovery of a novel benzylpiperidine derivative with serotonin transporter (SERT) inhibitory activity and 5-HT1A receptor weak partial agonistic activity showing the antidepressant-like effect. The 3-methoxyphenyl group and the phenethyl group of compound 1, which has weak SERT binding activity, but potent 5-HT1A binding activity, were optimized, leading to compound 35 with potent and balanced dual SERT and 5-HT1A binding activity, but also potent CYP2D6 inhibitory activity. Replacement of the methoxy group in the left part of compound 35 with a larger alkoxy group, such as ethoxy, isopropoxy or methoxy-ethoxy group ameliorated CYP2D6 inhibition, giving SMP-304 as a candidate...
October 29, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27859267/human-motoneurone-excitability-is-depressed-by-activation-of-5ht1a-receptors-with-buspirone
#20
Jessica M D'Amico, Annie A Butler, Martin E Héroux, Florence Cotel, Jean-François M Perrier, Jane E Butler, Simon C Gandevia, Janet L Taylor
Intense serotonergic drive in the turtle spinal cord results in serotonin spillover to the axon initial segment of the motoneurones where it activates 5HT1A receptors and inhibits generation of action potentials. We examined whether activation of 5HT1A receptors decreases motoneurone excitability in humans by determining the effects of a 5HT1A receptor partial agonist, buspirone, on F waves and cervicomedullary motor evoked potentials (CMEPs). In a placebo-controlled double-blind study, 10 participants were tested on two occasions where either placebo or 20 mg buspirone was administered orally...
November 17, 2016: Journal of Physiology
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