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Opioid Precursor

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https://www.readbyqxmd.com/read/29757600/dark-classics-in-chemical-neuroscience-morphine
#1
Andrea L Devereaux, Susan L Mercer, Christopher W Cunningham
As the major psychoactive agent in opium and direct precursor for heroin, morphine is a historically critical molecule in chemical neuroscience. A structurally complex phenanthrene alkaloid produced by Papaver somniferum, morphine has fascinated chemists seeking to disentangle pharmacologically beneficial analgesic effects from addiction, tolerance, and dependence liabilities. In this review, we will detail the history of morphine, from the first extraction and isolation by Sertürner in 1804 to the illicit use of morphine and proliferation of opioid use and abuse disorders currently ravaging the United States...
May 14, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29738766/development-of-a-novel-photoaffinity-probe-for-labeling-nocistatin-receptor
#2
Masashi Harada, Toshiaki Minami, Seiji Ito, Emiko Okuda-Ashitaka
Nocistatin (NST) is a neuropeptide produced from the same precursor protein of opioid peptide nociceptin/orphanin FQ (N/OFQ), and it is involved in a broad range of central functions including pain transmission in the nervous system. However, the composition and structure of the receptor(s) for NST remain unclear. Here, we developed NST photoaffinity probe to identify NST-binding receptor. The NST photoaffinity probe contains an azide moiety for the tagging of the binding protein as well as biotin for protein detection...
May 5, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29679289/cross-state-dependency-of-learning-between-tramadol-and-mk-801-in-the-mouse-dorsal-hippocampus-involvement-of-nitric-oxide-no-signaling-pathway
#3
Majid Jafari-Sabet, Shiva Amiri, Ramin Ataee
RATIONALE: Tramadol, an atypical μ-opioid receptor agonist, as a psychoactive drug, is frequently abused by human beings. Understanding the neurobiological mechanisms of drug-associated learning and memory formation may help prevent drug addiction and relapse. Previous study revealed that dorsal hippocampus (CA1) plays a crucial role in the retrieval of tramadol-associated memory and that its role depends on the expression of CA1 N-methyl-D-aspartate (NMDA) receptors (Jafari-Sabet et al...
April 21, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29678771/prenatal-ethanol-induces-an-anxiety-phenotype-and-alters-expression-of-dynorphin-nociceptin-orphanin-fq-genes
#4
Aranza Wille-Bille, Roberto Sebastián Miranda-Morales, Mariangela Pucci, Fabio Bellia, Claudio D'Addario, Ricardo Marcos Pautassi
Animal models have suggested that prenatal ethanol exposure (PEE) alters the κ opioid receptor system. The present study investigated the brain expression of dynorphin and nociceptin/orphanin FQ related genes and assessed anxiety-like behavior in the light-dark box (LDB), shelter-seeking and risk-taking behaviors in the concentric square field (CSF) test, and ethanol-induced locomotion in the open field (OF), in infant or adolescent Wistar rats that were exposed to PEE (0.0 or 2.0 g/kg, intragastrically, gestational days 17-20)...
April 17, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29571287/chronic-oxycodone-induces-axonal-degeneration-in-rat-brain
#5
Ruping Fan, Lisa M Schrott, Thomas Arnold, Stephen Snelling, Meghana Rao, Derrel Graham, Angela Cornelius, Nadejda L Korneeva
BACKGROUND: Chronic opioid therapy for non-malignant pain conditions has significantly increased over the last 15 years. Recently, the correlation between opioid analgesics and alternations in brain structure, such as leukoencephalopathy, axon demyelination, and white matter lesions, has been demonstrated in patients with a history of long-term use of prescription opioids. The exact mechanisms underlying the neurotoxic effect of opioids on the central nervous system are still not fully understood...
March 23, 2018: BMC Neuroscience
https://www.readbyqxmd.com/read/29476270/cognitive-behavioral-therapy-cbt-for-subacute-low-back-pain-a-systematic-review
#6
REVIEW
Timothy Y Mariano, Richard D Urman, Catherine A Hutchison, Robert N Jamison, Robert R Edwards
PURPOSE OF REVIEW: Chronic low back pain (CLBP) is a major source of physical and psychiatric morbidity and mortality, and the current overreliance on opioid analgesics has contributed to a burgeoning epidemic in the USA. Cognitive behavioral therapy (CBT) is an empirically supported treatment for CLBP, but little information exists regarding its potential efficacy for CLBP's precursor condition, subacute low back pain (sALBP), defined here as having a 7-12-week duration. Earlier intervention with CBT at the sALBP stage could produce larger clinical benefits...
February 23, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29453978/venlafaxine-prevents-morphine-antinociceptive-tolerance-the-role-of-neuroinflammation-and-the-l-arginine-nitric-oxide-pathway
#7
Mohammad Taghi Mansouri, Bahareh Naghizadeh, Behnam Ghorbanzadeh, Soheila Alboghobeish, Neda Amirgholami, Gholamreza Houshmand, Omar Cauli
Opioid-induced neuroinflammation and the nitric oxide (NO) signal-transduction pathway are involved in the development of opioid analgesic tolerance. The antidepressant venlafaxine (VLF) modulates NO in nervous tissues, and so we investigated its effect on induced tolerance to morphine, neuroinflammation, and oxidative stress in mice. Tolerance to the analgesic effects of morphine were induced by injecting mice with morphine (50 mg/kg) once a day for three consecutive days; the effect of co-administration of VLF (5 or 40 mg/kg) with morphine was similarly tested in a separate group...
May 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29330135/apbb2-is-associated-with-amphetamine-use-and-plasma-beta-amyloids-in-patients-receiving-methadone-maintenance-treatment
#8
Chia-Chen Liu, Chiu-Ping Fang, Tung-Hsia Liu, Hsiang-Wei Kuo, Shu Chi Liu, Sheng-Chang Wang, Andrew C H Chen, Yu-Li Liu
APBB2, amyloid beta (A4) precursor protein-binding family B member 2, has been reported to be associated with opioid dependence. In this study, we reported the first time that the genetic variants in the APBB2 gene were associated with use of amphetamine in opioid dependent patients undergoing methadone maintenance treatment (MMT). 344 heroin-dependent patients undergoing MMT were recruited and assessed for use of amphetamine and opioids by urine toxicology, withdrawal severity, and side effects. DNAs were genome-widely genotyped for all patients...
April 20, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29275265/anesthetic-and-pharmacologic-considerations-in-perioperative-care-of-obese-children
#9
REVIEW
Vidya Chidambaran, Anurag Tewari, Mohamed Mahmoud
PURPOSE: Anesthetic management of obese pediatric patients is challenging. With increasing prevalence of childhood obesity, more severely obese children with comorbidities present for surgery every day. The purpose of this review is to provide an up-to-date comprehensive narrative review on the impact of pathophysiological changes imposed by pediatric obesity on the perioperative management of obese children, especially drug dosing. This knowledge is necessary to provide safe delivery of anesthesia for severely obese children...
March 2018: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/29193080/the-non-peptidic-%C3%AE-opioid-receptor-agonist-tan-67-mediates-neuroprotection-post-ischemically-and-is-associated-with-altered-amyloid-precursor-protein-expression-maturation-and-processing-in-mice
#10
Jia-Wei Min, Yanying Liu, David Wang, Fangfang Qiao, Hongmin Wang
Tan-67 is a selective non-peptidic δ-opioid receptor (DOR) agonist that confers neuroprotection against cerebral ischemia/reperfusion (I/R)-caused neuronal injury in pre-treated animals. In this study, we examined whether post-ischemic administration of Tan-67 in stroke mice is also neuroprotective and whether the treatment affects expression, maturation and processing of the amyloid precursor protein (APP). A focal cerebral I/R model in mice was induced by middle cerebral artery occlusion for 1 h and Tan-67 (1...
February 2018: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29186585/fatality-following-ingestion-of-tetrahydrofuranylfentanyl-u-49900-and-methoxy-phencyclidine
#11
Alex J Krotulski, Donna M Papsun, Melissa Friscia, Jennifer L Swartz, Brian D Holsey, Barry K Logan
Novel psychoactive substances (NPS), and specifically novel opioids, continue to cause adverse events, including death, within drug-using populations. As the number of opioid-related overdoses continues to increase, laboratories have identified the emergence of new fentanyl analogues and other synthetic opioid-related drugs. Tetrahydrofuranylfentanyl (THFF) has been identified in Europe and the United States as an emerging novel opioid, causing death in at least 15 drug-using individuals to date. THFF is structurally similar to furanylfentanyl, a previously characterized novel opioid responsible for numerous adverse events, including death...
November 24, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29124744/usefulness-of-knockout-mice-to-clarify-the-role-of-the-opioid-system-in-chronic-pain
#12
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 many 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
#13
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)...
February 5, 2018: 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
#14
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
#15
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...
March 2018: 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
#16
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
#17
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
#18
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...
October 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28747521/novel-18-f-labeled-%C3%AE%C2%BA-opioid-receptor-antagonist-as-pet-radiotracer-synthesis-and-in-vivo-evaluation-of-18-f-ly2459989-in-nonhuman-primates
#19
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 κ-opioid receptor (KOR) has been implicated in depression, addictions, and other central nervous system disorders and, thus, is an important target for drug development. We previously developed several11 C-labeled PET radiotracers for KOR imaging in humans. Here we report the synthesis and evaluation of18 F-LY2459989 as the first18 F-labeled KOR antagonist radiotracer in nonhuman primates and its comparison with11 C-LY2459989. Methods: The novel radioligand18 F-LY2459989 was synthesized by18 F displacement of a nitro group or an iodonium ylide...
January 2018: 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
#20
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
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