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Opioid Precursor

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https://www.readbyqxmd.com/read/29124744/usefulness-of-knockout-mice-to-clarify-the-role-of-the-opioid-system-in-chronic-pain
#1
REVIEW
Rafael Maldonado, Josep Eladi Baños, David Cabañero
Several lines of knockout mice deficient in the genes encoding each component of the endogenous opioid system have been used for decades to clarify the specific role of the different opioid receptors and peptide precursors in multiple physiopathological conditions. The use of these genetically modified mice has improved our knowledge of the specific involvement of each endogenous opioid component in nociceptive transmission during acute and chronic pain conditions. The present review summarizes the recent advances obtained using these genetic tools in understanding the role of the opioid system in the pathophysiological mechanisms underlying chronic pain...
November 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29121571/high-throughput-%C3%AE-spe-based-elution-coupled-with-uplc-ms-ms-for-determination-of-eluxadoline-in-plasma-sample-application-in-pharmacokinetic-characterization-of-plga-nanoparticle-formulations-in-rats
#2
Muzaffar Iqbal, Essam Ezzeldin, Khalid A Al-Rashood, Ramadan Al-Shdefat, Md Khalid Anwer
Eluxadoline is a novel μ- and κ-opioid receptor (OR) agonist and δ-OR antagonist, recently approved as a first line therapy for the treatment of irritable bowel syndrome. Due to abuse potential, poor bioavailability and high intersubject variability, a sensitive and reliable assay is prerequisite for its determination in biological samples. This work first time report the development and validation of UPLC-MS/MS assay for determination of eluxadoline in rat plasma sample using risperidone as an internal standard (IS)...
October 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28991183/orexin-receptor-multimerization-versus-functional-interactions-neuropharmacological-implications-for-opioid-and-cannabinoid-signalling-and-pharmacogenetics
#3
Miles D Thompson, Takeshi Sakurai, Innocenzo Rainero, Mary C Maj, Jyrki P Kukkonen
Orexins/hypocretins are neuropeptides formed by proteolytic cleavage of a precursor peptide, which are produced by neurons found in the lateral hypothalamus. The G protein-coupled receptors (GPCRs) for these ligands, the OX₁ and OX₂ orexin receptors, are more widely expressed throughout the central nervous system. The orexin/hypocretin system has been implicated in many pathways, and its dysregulation is under investigation in a number of diseases. Disorders in which orexinergic mechanisms are being investigated include narcolepsy, idiopathic sleep disorders, cluster headache and migraine...
October 8, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28991118/truncated-%C3%AE-opioid-receptors-with-6-transmembrane-domains-are-essential-for-opioid-analgesia
#4
Zhigang Lu, Jin Xu, Mingming Xu, Grace C Rossi, Susruta Majumdar, Gavril W Pasternak, Ying-Xian Pan
BACKGROUND: Most clinical opioids act through μ-opioid receptors. They effectively relieve pain but are limited by side effects, such as constipation, respiratory depression, dependence, and addiction. Many efforts have been made toward developing potent analgesics that lack side effects. Three-iodobenzoyl-6β-naltrexamide (IBNtxA) is a novel class of opioid active against thermal, inflammatory, and neuropathic pain, without respiratory depression, physical dependence, and reward behavior...
October 4, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28923480/impact-of-morphine-on-the-expression-of-insulin-receptor-and-protein-levels-of-insulin-igfs-in-rat-neural-stem-cells
#5
Sadegh Salarinasab, AliReza Nourazarian, Masoud Nikanfar, Nima Abdyazdani, Masoumeh Kazemi, Navid Feizy, Reza Rahbarghazi
Alzheimer's disease is correlated with neuronal degeneration and loss of neuronal precursors in different parts of the brain. It has been found disturbance in the homeostasis neural stem cells (NSCs) can cause neurodegeneration. Morphine, an analgesic agent, can disrupt the dynamic and normal state of NSCs. However, more investigations are required to clearly address underlying mechanisms. The current experiment aimed to investigate the effects of morphine on the cell distribution of insulin factor and receptor and insulin-like growth factors (IGF1, IGF2) in NSCs...
November 1, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28802836/neocortical-prodynorphin-expression-is-transiently-increased-with-learning-implications-for-time-and-learning-dependent-neocortical-kappa-opioid-receptor-activation
#6
Ryan Loh, Sean Collins, Roberto Galvez
There are several lines of evidence that indicate a prominent role for the opioid system in the acquisition and consolidation of learned associations. Specifically, kappa opioid receptor (KOR) modulation has been demonstrated to alter various behavioral tasks including whisker trace eyeblink conditioning (WTEB). WTEB is an associative conditioning paradigm in which a neutral conditioned stimulus (CS; Whisker stimulation) is paired following a short stimulus free trace interval with a salient unconditioned stimulus that elicits a blink response (US; Eye shock)...
August 9, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28776309/morphine-withdrawal-increases-brain-derived-neurotrophic-factor-precursor
#7
Alessia Bachis, Lee A Campbell, Kierra Jenkins, Erin Wenzel, Italo Mocchetti
Morphine has been shown to increase the expression of brain-derived neurotrophic factor (BDNF) in the brain. However, little is known about the effect of morphine withdrawal on BDNF and its precursor protein, or proBDNF, which induces neuronal apoptosis. In this work, we examined whether BDNF and proBDNF levels change in rats chronically injected with escalating doses of morphine and those who undergo spontaneous withdrawal for 60 h. We observed, in the frontal cortex and striatum, that the ratio of BDNF to proBDNF changed depending upon the experimental paradigm...
August 3, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28747521/a-novel-18-f-labeled-kappa-opioid-receptor-antagonist-as-pet-radiotracer-synthesis-and-in-vivo-evaluation-of-18-f-ly2459989-in-non-human-primates
#8
Songye Li, Zhengxin Cai, Ming-Qiang Zheng, Daniel Holden, Mika Naganawa, Shu-Fei Lin, Jim Ropchan, David Labaree, Michael Kapinos, Teresa Lara-Jaime, Antonio Navarro, Yiyun Huang
The kappa opioid receptor (KOR) is implicated in depression, addictions, and other central nervous system (CNS) disorders and thus an important target for drug development. We have previously developed a number of (11)C-labeled PET radiotracers for KOR imaging in humans. Here we report the synthesis and evaluation of (18)F-LY2459989 as the first (18)F-labeled KOR antagonist radiotracer in non-human primates and its comparison with (11)C-LY2459989. Methods: The novel radioligand (18)F-LY2459989 was synthesized by (18)F-displacement of a nitro group or an iodonium ylide...
July 26, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28725181/impact-of-proestrus-on-gene-expression-in-the-medial-preoptic-area-of-mice
#9
Csaba Vastagh, Zsolt Liposits
The antero-ventral periventricular zone (AVPV) and medial preoptic area (MPOA) have been recognized as gonadal hormone receptive regions of the rodent brain that-via wiring to gonadotropin-releasing hormone (GnRH) neurons-contribute to orchestration of the preovulatory GnRH surge. We hypothesized that neural genes regulating the induction of GnRH surge show altered expression in proestrus. Therefore, we compared the expression of 48 genes obtained from intact proestrous and metestrous mice, respectively, by quantitative real-time PCR (qPCR) method...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28716934/sigma-1-receptors-control-immune-driven-peripheral-opioid-analgesia-during-inflammation-in-mice
#10
Miguel A Tejada, Angeles Montilla-García, Shane J Cronin, Domagoj Cikes, Cristina Sánchez-Fernández, Rafael González-Cano, M Carmen Ruiz-Cantero, Josef M Penninger, José M Vela, José M Baeyens, Enrique J Cobos
Sigma-1 antagonism potentiates the antinociceptive effects of opioid drugs, so sigma-1 receptors constitute a biological brake to opioid drug-induced analgesia. The pathophysiological role of this process is unknown. We aimed to investigate whether sigma-1 antagonism reduces inflammatory pain through the disinhibition of the endogenous opioidergic system in mice. The selective sigma-1 antagonists BD-1063 and S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute (3 h) inflammation...
August 1, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28708940/street-like-synthesis-of-krokodil-results-in-the-formation-of-an-enlarged-cluster-of-known-and-new-morphinans
#11
José Xavier Soares, Emanuele Amorim Alves, André M N Silva, Natália Guimarães de Figueiredo, João F Neves, Sara Manuela Cravo, Maria Rangel, Annibal Duarte Pereira Netto, Félix Carvalho, Ricardo Jorge Dinis-Oliveira, Carlos Manuel Afonso
"Krokodil" is the street name for a homemade injectable drug that has been used as a cheap substitute for heroin. Codeine is the opioid starting material for krokodil synthesis, and desomorphine is claimed to be the main opioid of krokodil and the main component responsible for its addictive and psychoactive characteristics. However, due to its peculiar manufacture, using cheap raw materials, krokodil is composed of a large and complex mixture of different substances. In order to shed some light upon the chemical complexity of krokodil, its profiling was conducted by reverse phase high performance liquid chromatography coupled to a photodiode array detector (RP-HPLC-DAD) and by liquid chromatography coupled to high resolution tandem mass spectrometry (LC-ESI-IT-Orbitrap-MS)...
August 21, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28609429/reciprocal-evolution-of-opiate-science-from-medical-and-cultural-perspectives
#12
George B Stefano, Nastazja Pilonis, Radek Ptacek, Richard M Kream
Over the course of human history, it has been common to use plants for medicinal purposes, such as for providing relief from particular maladies and self-medication. Opium represents one longstanding remedy that has been used to address a range of medical conditions, alleviating discomfort often in ways that have proven pleasurable. Opium is a combination of compounds obtained from the mature fruit of opium poppy, papaver somniferum. Morphine and its biosynthetic precursors thebaine and codeine constitute the main bioactive opiate alkaloids contained in opium...
June 13, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28419528/an-updated-synthesis-of-11-c-carfentanil-for-positron-emission-tomography-pet-imaging-of-the-%C3%AE-opioid-receptor
#13
Joseph E Blecha, Bradford D Henderson, Brian G Hockley, Henry F VanBrocklin, Jon-Kar Zubieta, Alexandre F DaSilva, Michael R Kilbourn, Robert A Koeppe, Peter J H Scott, Xia Shao
[(11) C]Carfentanil ([(11) C]CFN) is a selective radiotracer for in vivo positron emission tomography imaging studies of the μ-opioid system that, in our laboratories, is synthesized by methylation of the corresponding carboxylate precursor with [(11) C]MeOTf, and purified using a C2 solid-phase extraction cartridge. Changes in the commercial availability of common C2 cartridges have necessitated future proofing the synthesis of [(11) C]CFN to maintain reliable delivery of the radiotracer for clinical imaging studies...
April 17, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28242307/molecular-identification-of-the-dyn-kor-system-and-its-potential-role-in-the-reproductive-axis-of-goldfish
#14
Yali Liu, Shuisheng Li, Qing Wang, Yu Chen, Xin Qi, Yun Liu, Xiaochun Liu, Haoran Lin, Yong Zhang
To ascertain the significance of the dynorphin/kappa-opioid receptor (Dyn/Kor) system in fish reproduction, prodynorphin (pdyn) cDNA was cloned from goldfish. Two Dyn peptides (DynA and DynB) are present in the goldfish prodynorphin precursor. Both DynA and DynB are biologically active as they are able to functionally interact with the goldfish Kor expressed in cultured eukaryotic cells to suppress forskolin-induced CRE promoter activity. RT-PCR analysis showed that pdyn is widely expressed in brain regions, with the highest expression in hypothalamus...
February 24, 2017: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/28220108/adaptations-in-basal-and-hypothalamic-pituitary-adrenal-activated-deoxycorticosterone-responses-following-ethanol-self-administration-in-cynomolgus-monkeys
#15
Vanessa A Jimenez, Patrizia Porcu, A Leslie Morrow, Kathleen A Grant
Acute ethanol activates the hypothalamic-pituitary-adrenal (HPA) axis, while long-term exposure results in a blunted neuroendocrine state, particularly with regards to the primary endpoint, cortisol, the primary glucocorticoid produced in the adrenal cortex. However, it is unknown if this dampened neuroendocrine status also influences other adrenocortical steroids. Plasma concentration of the mineralocorticoid and neuroactive steroid precursor deoxycorticosterone (DOC) is altered by pharmacological challenges of the HPA axis in cynomolgus monkeys...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28105567/effects-of-oleuropein-on-pentylenetetrazol-induced-seizures-in-mice-involvement-of-opioidergic-and-nitrergic-systems
#16
Nastaran Rahimi, Bahram Delfan, Nazgol Motamed-Gorji, Ahmad R Dehpour
Oleuropein, a well-known olive polyphenol, has been shown to mediate neuroprotection in Alzheimer's disease and cerebral ischemia. We investigated the effects of oleuropein on pentylenetetrazole (PTZ)-induced seizures in male NMRI mice, with diazepam as the standard drug. We also examined the possible involvement of opioidergic/nitrergic pathways in the probable effects of oleuropein. Intraperitoneal (i.p.) administration of different doses of oleuropein (10, 20 and 30 mg/kg) significantly increased the seizure threshold 60 min prior to induction of seizure, in a dose-dependent manner...
April 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/27899097/antinociception-of-petroleum-ether-fraction-derived-from-crude-methanol-extract-of-melastoma-malabathricum-leaves-and-its-possible-mechanisms-of-action-in-animal-models
#17
Z A Zakaria, E S Jaios, M H Omar, S Abd Rahman, S S A Hamid, S M Ching, L K Teh, M Z Salleh, S Deny, M Taher
BACKGROUND: Melastoma malabathricum L. (family Melastomaceae) has been traditionally used as remedies against various ailments including those related to pain. The methanol extract of M. malabathricum leaves has been proven to show antinociceptive activity. Thus, the present study aimed to determine the most effective fraction among the petroleum ether- (PEMM), ethyl acetate- (EAMM) and aqueous- (AQMM) fractions obtained through successive fractionation of crude, dried methanol extract of M...
November 29, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27837406/b-lymphocytes-express-pomc-mrna-processing-enzymes-and-%C3%AE-endorphin-in-painful-inflammation
#18
Santhosh Chandar Maddila, Melanie Busch-Dienstfertig, Christoph Stein
Immune cell-derived beta-endorphin (END) and other opioid peptides elicit potent and clinically relevant inhibition of pain (analgesia) in inflamed tissue by activation of peripheral opioid receptors. Pro-opiomelanocortin (POMC) is the polypeptide precursor of END and is processed by prohormone convertases (PCs). This study aims to decipher the processing of POMC in lymphocyte subsets in a rat model of unilateral painful hindpaw inflammation. Lymphocytes, isolated from popliteal lymph nodes, were separated into B-cells, T-cells, T-helper cells and cytotoxic T-cells using magnetic cell sorting, and were examined by polymerase chain reaction, immunofluorescence and radioimmunoassay...
March 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/27779481/a-novel-non-opioid-binding-site-for-endomorphin-1
#19
I Lengyel, F Toth, D Biyashev, I Szatmari, K Monory, C Tomboly, G Toth, S Benyhe, A Borsodi
Endomorphins are natural amidated opioid tetrapeptides with the following structure: Tyr-Pro-Trp-Phe-NH2 (endomorphin-1), and Tyr-Pro-Phe-Phe-NH2 (endomorphin-2). Endomorphins interact selectively with the μ-opioid or MOP receptors and exhibit nanomolar or sub-nanomolar receptor binding affinities, therefore they suggested to be endogenous agonists for the μ-opioid receptors. Endomorphins mediate a number of characteristic opioid effects, such as antinociception, however there are several physiological functions in which endomorphins appear to act in a fashion that does not involve binding to and activation of the μ-opioid receptor...
August 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/27754186/sp-04-1-the-role-of-natriuretic-peptides-in-the-pathogenesis-of-cardiovascular-diseases
#20
Zhanna Kobalava
The burden of cardiovascular diseases (CVD) in general and heart failure (HF) in particular continues to increase worldwide. CVD are major contributors to death and morbidity and recognized as important drivers of healthcare expenditure. Chronic overactivity of the renin-angiotensin-aldosterone system (RAAS) plays a key role in human hypertension and HF pathophysiology. RAAS is fundamental in the overall regulation of cardiovascular homeostasis through the actions of hormones, which regulate vascular tone, and specifically blood pressure through vasoconstriction and renal sodium and water retention...
September 2016: Journal of Hypertension
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