keyword
MENU ▼
Read by QxMD icon Read
search

Opioid Precursor

keyword
https://www.readbyqxmd.com/read/28609429/reciprocal-evolution-of-opiate-science-from-medical-and-cultural-perspectives
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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...
November 11, 2016: 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
#8
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
#9
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
https://www.readbyqxmd.com/read/27688945/kappa-opioid-receptors-differentially-regulate-low-and-high-levels-of-ethanol-intake-in-female-mice
#10
Ashlee Van't Veer, Karen L Smith, Bruce M Cohen, William A Carlezon, Anita J Bechtholt
INTRODUCTION: Studies in laboratory animals and humans indicate that endogenous opioids play an important role in regulating the rewarding value of various drugs, including ethanol (EtOH). Indeed, opioid antagonists are currently a front-line treatment for alcoholism in humans. Although roles for mu- and delta-opioid receptors have been characterized, the contribution of kappa-opioid receptors (KORs) is less clear. There is evidence that changes in KOR system function can decrease or increase EtOH drinking, depending on test conditions...
September 2016: Brain and Behavior
https://www.readbyqxmd.com/read/27643143/sp-04-1-the-role-of-natriuretic-peptides-in-the-pathogenesis-of-cardiovascular-diseases
#11
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
https://www.readbyqxmd.com/read/27566575/peptidome-analysis-of-human-milk-from-women-delivering-macrosomic-fetuses-reveals-multiple-means-of-protection-for-infants
#12
Xianwei Cui, Yun Li, Lei Yang, Lianghui You, Xing Wang, Chunmei Shi, Chenbo Ji, Xirong Guo
Breastfeeding is associated with a lower incidence of obesity, diabetes, and cardiovascular disease later in life. While macrosomic infants have a higher risk of developing obesity and other metabolic disorders. Breast milk may contain special nutrients to meet the different growth needs of different infants. Whether mothers make breast milk different to meet the requirement of macrosomic infants is still unknown. Here, we conducted a comparison between mothers delivering macrosomic and non-macrosomic infants in colostrum endogenous peptides...
September 27, 2016: Oncotarget
https://www.readbyqxmd.com/read/27560775/fentanyl-law-enforcement-submissions-and-increases-in-synthetic-opioid-involved-overdose-deaths-27-states-2013-2014
#13
R Matthew Gladden, Pedro Martinez, Puja Seth
In March and October 2015, the Drug Enforcement Administration (DEA) and CDC, respectively, issued nationwide alerts identifying illicitly manufactured fentanyl (IMF) as a threat to public health and safety (1,2). IMF is unlawfully produced fentanyl, obtained through illicit drug markets, includes fentanyl analogs, and is commonly mixed with or sold as heroin (1,3,4). Starting in 2013, the production and distribution of IMF increased to unprecedented levels, fueled by increases in the global supply, processing, and distribution of fentanyl and fentanyl-precursor chemicals by criminal organizations (3)...
August 26, 2016: MMWR. Morbidity and Mortality Weekly Report
https://www.readbyqxmd.com/read/27476446/identification-of-a-new-psychoactive-substance-in-seized-material-the-synthetic-opioid-n-phenyl-n-1-2-phenethyl-piperidin-4-yl-prop-2-enamide-acrylfentanyl
#14
Torben Breindahl, Andreas Kimergård, Mette Findal Andreasen, Daniel Sejer Pedersen
Among the new psychoactive substances (NPS) that have recently emerged on the market, many of the new synthetic opioids have shown to be particularly harmful. A new synthetic analogue of fentanyl, N-phenyl-N-[1-(2-phenethyl)piperidin-4-yl]prop-2-enamide (acrylfentanyl), was identified in powder from a seized capsule found at a forensic psychiatric ward in Denmark. Gas chromatography with mass spectrometry (GC-MS) identified a precursor to synthetic fentanyls, N-phenyl-1-(2-phenylethyl)piperidin-4-amine; however, the precursor 1-(2-phenethyl)piperidin-4-one, was not detected...
March 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27466337/identification-of-the-kappa-opioid-receptor-as-a-therapeutic-target-for-oligodendrocyte-remyelination
#15
Feng Mei, Sonia R Mayoral, Hiroko Nobuta, Fei Wang, Caroline Desponts, Daniel S Lorrain, Lan Xiao, Ari J Green, David Rowitch, Jennifer Whistler, Jonah R Chan
UNLABELLED: Remyelinating therapies seek to promote restoration of function and normal cellular architecture following demyelination in diseases, such as multiple sclerosis (MS). Functional screening for small molecules or novel targets for remyelination is a major hurdle to the identification and development of rational therapeutics for MS. Recent findings and technical advances provide us with a unique opportunity to provide insight into the cell autonomous mechanisms for remyelination and address this unmet need...
July 27, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27260403/altered-secondary-structure-of-dynorphin-a-associates-with-loss-of-opioid-signalling-and-nmda-mediated-excitotoxicity-in-sca23
#16
Cleo J L M Smeets, Justyna Zmorzyńska, Manuel N Melo, Anita Stargardt, Colette Dooley, Georgy Bakalkin, Jay McLaughlin, Richard J Sinke, Siewert-Jan Marrink, Eric Reits, Dineke S Verbeek
Spinocerebellar ataxia type 23 (SCA23) is caused by missense mutations in prodynorphin, encoding the precursor protein for the opioid neuropeptides α-neoendorphin, Dynorphin (Dyn) A and Dyn B, leading to neurotoxic elevated mutant Dyn A levels. Dyn A acts on opioid receptors to reduce pain in the spinal cord, but its cerebellar function remains largely unknown. Increased concentration of or prolonged exposure to Dyn A is neurotoxic and these deleterious effects are very likely caused by an N-methyl-d-aspartate-mediated non-opioid mechanism as Dyn A peptides were shown to bind NMDA receptors and potentiate their glutamate-evoked currents...
June 3, 2016: Human Molecular Genetics
https://www.readbyqxmd.com/read/27190528/methanolic-extract-of-clinacanthus-nutans-exerts-antinociceptive-activity-via-the-opioid-nitric-oxide-mediated-but-cgmp-independent-pathways
#17
Mohammad Hafiz Abdul Rahim, Zainul Amiruddin Zakaria, Mohd Hijaz Mohd Sani, Maizatul Hasyima Omar, Yusnita Yakob, Manraj Singh Cheema, Siew Mooi Ching, Zuraini Ahmad, Arifah Abdul Kadir
The objectives of the present study were to determine the mechanisms of antinociceptive effect of methanol extract of Clinacanthus nutans (Acanthaceae) leaves (MECN) using various animal nociceptive models. The antinociceptive activity of orally administered 10% DMSO, 100 mg/kg acetylsalicylic acid (ASA), 5 mg/kg morphine, or MECN (100, 250, and 500 mg/kg) was determined using the acetic acid-induced abdominal constriction (ACT), formalin-induced paw licking (FT), and hot plate tests (HPT). The role of opioid and nitric oxide/cyclic guanosine monophosphate (NO/cGMP) systems was also investigated...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27172347/batch-and-continuous-flow-aerobic-oxidation-of-14-hydroxy-opioids-to-1-3-oxazolidines-a-concise-synthesis-of-noroxymorphone
#18
Bernhard Gutmann, Ulrich Weigl, D Phillip Cox, C Oliver Kappe
14-Hydroxymorphinone is converted to noroxymorphone, the immediate precursor of important opioid antagonists, such as naltrexone and naloxone, in a three-step reaction sequence. The initial oxidation of the N-methyl group in 14-hydroxymorphinone with in situ generated colloidal palladium(0) as the catalyst and molecular oxygen as the terminal oxidant constitutes the key transformation in this new route. This oxidation results in the formation of an unexpected oxazolidine ring structure. Subsequent hydrolysis of the oxazolidine under reduced pressure followed by hydrogenation in a packed-bed flow reactor using palladium(0) as the catalyst provides noroxymorphone in high purity and good overall yield...
July 18, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27081466/%C3%AE-terpineol-attenuates-morphine-induced-physical-dependence-and-tolerance-in-mice-role-of-nitric-oxide
#19
Siavash Parvardeh, Mahsa Moghimi, Pegah Eslami, Alireza Masoudi
OBJECTIVES: Dependence and tolerance to opioid analgesics are major problems limiting their clinical application. α-Terpineol is a monoterpenoid alcohol with neuroprotective effects which is found in several medicinal plants such as Myrtus communis, Laurus nobilis, and Stachys byzantina. It has been shown that some of these medicinal plants such as S. byzantina attenuate dependence and tolerance to morphine. Since α-terpineol is one of the bioactive phytochemical constituent of these medicinal plants, the present study was conducted to investigate the effects of α-terpineol on morphine-induced dependence and tolerance in mice...
February 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27013974/dynorphin-dependent-reduction-of-excitability-and-attenuation-of-inhibitory-afferents-of-nps-neurons-in-the-pericoerulear-region-of-mice
#20
Kay Jüngling, Peter Blaesse, Lena Goedecke, Hans-Christian Pape
The Neuropeptide S system, consisting of the 20-amino acid peptide neuropeptide S (NPS) and its G-protein coupled receptor (NPSR), modulates arousal, wakefulness, anxiety, and fear-extinction in mice. In addition, recent evidence indicates that the NPS system attenuates stress-dependent impairment of fear extinction, and that NPS-expressing neurons in close proximity to the locus coeruleus region (LC; pericoerulear, periLC) are activated by stress. Furthermore, periLC NPS neurons receive afferents from neurons of the centrolateral nucleus of the amygdala (CeL), of which a substantial population expresses the kappa opioid receptor (KOR) ligand precursor prodynorphin...
2016: Frontiers in Cellular Neuroscience
keyword
keyword
73735
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"