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Opioid receptors

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https://www.readbyqxmd.com/read/28635314/fluorescent-labeled-bioconjugates-of-the-opioid-peptides-biphalin-and-dpdpe-incorporating-fluorescein-maleimide-linkers
#1
Azzurra Stefanucci, Wei Lei, Victor J Hruby, Giorgia Macedonio, Grazia Luisi, Simone Carradori, John M Streicher, Adriano Mollica
AIM: The conjugation of fluorescent labels to opioid peptides is an extremely challenging task, which needs to be overcome to create new classes of probes for biological assays. MATERIALS & METHODS: Three opioid peptide analogs of biphalin and [D-Pen2,5]-Enkephalin (DPDPE) containing a fluorescein-maleimide motif were synthesized. RESULTS & DISCUSSION: The biphalin analog 17 binds to opioid receptors with Ki(μ) = 530 ± 90 nM and Ki(δ) = 69...
June 21, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28635181/buprenorphine-requires-concomitant-activation-of-nop-and-mop-receptors-to-reduce-cocaine-consumption
#2
Marsida Kallupi, Qianwei Shen, Giordano de Guglielmo, Dennis Yasuda, V Blair Journigan, Nurulain T Zaveri, Roberto Ciccocioppo
Buprenorphine's clinical use is approved for the treatment of heroin addiction; however, evidence supporting its efficacy in cocaine abuse also exists. While for heroin it has been demonstrated that the effect of buprenorphine is mediated by its ability to activate μ-opioid peptide receptor (MOP) receptors, the mechanism through which it attenuates cocaine intake remains elusive. We explored this mechanism using operant models where rodents were trained to chronically self-administer cocaine for 2 hours daily...
June 21, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28632076/association-of-oprd1-gene-variants-with-opioid-dependence-in-addicted-male-individuals-undergoing-methadone-treatment-in-the-north-of-iran
#3
Alireza Sharafshah, Hedyeh Fazel, Ali Albonaim, Vahid Omarmeli, Sajjad Rezaei, Ebrahim Mirzajani, Farzam Ajamian, Parvaneh Keshavarz
Genetic association of rs678849 along with neuroimaging and biomarker phenotypes, parallel with the known involvements of the OPRD1 in drug abuse, provided additional support for targeting these receptors as potential therapeutic targets in both neurodegenerative diseases and neuropsychiactric disorders such as Alzheimer's disease. Samples were selected among 202 opium-addicted participants undergoing methadone treatment and 202 healthy controls. Genomic DNA of all subjects was extracted from whole blood samples through a Salting Out procedure...
March 1, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28629227/chemical-and-biological-studies-on-cichorium-intybus-l
#4
Dinara Satmbekova, Radhakrishnan Srivedavyasasri, Yerkebulan Orazbekov, Roza Omarova, Ubaidilla Datkhayev, Samir A Ross
Cichorium intybus L. (Asteraceae family) is a world-wide grown plant known as chicory. In traditional medicine, this plant is used as diuretic, anti-inflammatory, digestive, cardiotonic and liver tonic. Chromatographic purification of the supercritical fluid extract of aerial parts of C. intybus on silica gel column led to isolation of three compounds: new compound, 28β-hydroxytaraxasterol (I), and two known compounds usnic acid (II) and β-sitosterol (III). Purification of the ethanolic extract of aerial parts of this plant on silica gel column chromatography yielded four compounds: 1,3-dioleylglycerate (IV), sitoindoside II (V), 11β-13-dihydrolactucin (VI) and β-sitosterol-3-O-glucoside (VII)...
June 19, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28627589/effect-of-the-spinal-apelin%C3%A2-apj-system-on-the-pathogenesis-of-chronic-constriction-injury%C3%A2-induced-neuropathic-pain-in-rats
#5
Qingming Xiong, Wanyou He, Hanbing Wang, Jun Zhou, Yajun Zhang, Jian He, Chengxiang Yang, Bin Zhang
Apelin is hypothesized to serve a dual function in pain processing. Spinal administration of apelin induces hyperalgesia, while opioid receptors are implicated in the antinociceptive effects of apelin in acute nociceptive models. However, whether the apelin‑apelin receptor (APJ) system is involved in neuropathic pain remains to be elucidated. The present study aimed to evaluate the impact and mechanism of the spinal apelin‑APJ system in neuropathic pain. Chronic constriction injury (CCI) of the sciatic nerve produced sustained spinal apelin and APJ upregulation, which was associated with mechanical allodynia and heat hyperalgesia development in the hind‑paw plantar surface...
June 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28626808/attenuation-of-opioid-tolerance-by-etb-receptor-agonist-irl-1620-is-independent-of-an-accompanied-decrease-in-nerve-growth-factor-in-mice
#6
Shruti Gulati, Seema Briyal, Shantel Jones, Shaifali Bhalla, Anil Gulati
AIM: ETA receptor antagonists reverse opioid tolerance but the involvement of ETB receptors is unknown. In morphine or oxycodone tolerant mice we investigated (1) the effect of ETB receptor agonist, IRL-1620, on analgesic tolerance; (2) changes in expression of the brain ETA and ETB receptors; and (3) alterations in the brain VEGF, NGF, PI3K and notch-1 expression. MAIN METHODS: Body weight, body temperature, and tail-flick latency were assessed before and after a challenge dose of morphine or oxycodone in vehicle or IRL-1620 treated mice...
June 2017: Heliyon
https://www.readbyqxmd.com/read/28626482/the-possible-mechanisms-of-analgesia-produced-by-microinjection-of-morphine-into-the-lateral-habenula-in-the-acute-model-of-trigeminal-pain-in-rats
#7
Emad Khalilzadeh, Gholamreza Vafaei Saiah
This study aimed to assess the effect of intra-habenular injection of morphine on acute trigeminal pain in rats. Also here, we examined the involvement of raphe nucleus opioid and 5HT3 receptors on the antinociceptive activity of intra habenular morphine to explore the possibility of existence of descending antinociceptive relay between the habenula and raphe nucleus. The numbers of eye wiping response elicited by applying a drop (40 μL) of NaCl (5 M) solution on the corneal surface were taken as an index of acute trigeminal nociception...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28625549/the-long-term-effects-of-stress-and-kappa-opioid-receptor-activation-on-conditioned-place-aversion-in-male-and-female-california-mice
#8
Abigail R Laman-Maharg, Tiffany Copeland, Evelyn Ordoñes Sanchez, Katharine L Campi, Brian C Trainor
Psychosocial stress leads to the activation of kappa opioid receptors (KORs), which induce dysphoria and facilitate depression-like behaviors. However, less is known about the long-term effects of stress and KORs in females. We examined the long-term effects of social defeat stress on the aversive properties of KOR activation in male and female California mice (Peromyscus californicus) using a conditioned place aversion paradigm. Female California mice naïve to social defeat, formed a place aversion following treatment with 2...
June 15, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28625456/the-effect-of-ondansetron-on-analgesic-efficacy-of-acetaminophen-after-hysterectomy-a-randomized-double-blinded-placebo-controlled-trial
#9
Onur Koyuncu, Steve Leung, Jing You, Menekse Oksar, Selim Turhanoglu, Cagla Akkurt, Kenan Dolapcioglu, Hanifi Sahin, Daniel I Sessler, Alparslan Turan
OBJECTIVES: To determine that perioperative ondansetron reduces the analgesic efficacy of acetaminophen. DESIGN: Randomized, double-blinded study. PATIENTS: 120 patients ASA I-II who underwent abdominal hysterectomy. INTERVENTIONS: All the patients were given 1g acetaminophen at skin closure. Patients were divided into two groups; ondansetron HCl (8mg, 2ml IV) (Group I, N=60) and saline (2ml IV) (Group II, N=60) at the skin closure...
August 2017: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/28623508/clinical-pharmacokinetic-characteristics-of-cebranopadol-a-novel-first-in-class-analgesic
#10
Elke Kleideiter, Chiara Piana, Shaonan Wang, Robert Nemeth, Michael Gautrois
BACKGROUND AND OBJECTIVES: Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clinical development for the treatment of chronic pain conditions. This trial focuses on the clinical pharmacokinetic (PK) properties of cebranopadol after oral single- and multiple-dose administration. METHODS: The basic PK properties of cebranopadol were assessed by means of noncompartmental methods in six phase I clinical trials in healthy subjects and patients...
June 16, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28621702/short-duration-physical-activity-prevents-the-development-of-activity-induced-hyperalgesia-through-opioid-and-serotoninergic-mechanisms
#11
Lucas V Lima, Josimari M DeSantana, Lynn A Rasmussen, Kathleen A Sluka, Lucas Vasconcelos Lima
Regular physical activity prevents development of chronic muscle pain through modulation of central mechanisms that involve rostral ventromedial medulla (RVM). We tested if pharmacological blockade or genetic deletion of mu-opioid receptors in physically active mice modulates excitatory and inhibitory systems in the RVM in an activity-induced hyperalgesia model. We examined response frequency to mechanical stimulation of the paw, muscle withdrawal thresholds, and expression of phosphorylation of the NR1 subunit of the NMDA receptor (p-NR1) and serotonin transporter (SERT) in the RVM...
June 8, 2017: Pain
https://www.readbyqxmd.com/read/28620922/supraspinal-inhibitory-effects-of-chimeric-peptide-mcrt-on-gastrointestinal-motility-in-mice
#12
Chunbo He, Hailan Li, Jing Zhang, Yanping Kang, Fang Jia, Shouliang Dong, Lanxia Zhou
OBJECTIVES: Chimeric peptide MCRT, based on morphiceptin and PFRTic-NH2 , was a bifunctional ligand of μ- and δ-opioid receptors (MOR-DOR) and produced potent analgesia in tail-withdrawal test. The study focused on the supraspinal effects of morphiceptin, PFRTic-NH2 and MCRT on gastrointestinal motility. Moreover, opioid receptor antagonists, naloxone (non-selective), cyprodime (MOR selective) and naltrindole (DOR selective) were utilized to explore the mechanisms. METHODS: Intracerebroventricular administration was achieved via the implanted cannula...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620391/toll-like-receptor-dependent-negative-effects-of-opioids-a-battle-between-analgesia-and-hyperalgesia
#13
REVIEW
Masaud Shah, Sangdun Choi
Our understanding of the pathophysiology of the pathological pain and the pharmacology of analgesic treatments has progressed tremendously over the past two decades. Among the well-documented pro-algesic factors, glia and other toll-like receptors (TLRs)-expressing cells in the neuroimmune interface have been recognized for their role in the development of neuropathic pain and for compromising the analgesic effects of opioids. Here, we comprehensively review the molecular mechanisms of pain initiation and progression, the role of TLRs in these processes, and the molecular mechanisms of morphine and morphine-3-glucuronide in TLR-dependent central immune signaling...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28618070/morin-suppresses-astrocyte-activation-and-regulates-cytokine-release-in-bone-cancer-pain-rat-models
#14
Wei Jiang, Ying Wang, Wei Sun, Mengyuan Zhang
As inflammatory and immune responses are involved in pathophysiology of debilitating neuropathic pain, reagents that can modulate these two responses may have therapeutic potential. Morin, derived from the moraceae family of plants, benefits inflammation-related diseases, but its antinociceptive effects on cancer pain remain elusive. In the present study, we investigated antinociceptive effects of morin on bone cancer pain using a rat model, where rats were subject to implantation of Walker 256 mammary gland carcinoma cells into the tibia...
June 15, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28609429/reciprocal-evolution-of-opiate-science-from-medical-and-cultural-perspectives
#15
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/28608532/%C3%AE-opioid-receptor-dopamine-d1-receptor-heteromers-modulate-opioid-induced-locomotor-sensitization-in-a-dopamine-independent-manner
#16
Yi-Min Tao, Chuan Yu, Wei-Sheng Wang, Yuan-Yuan Hou, Xue-Jun Xu, Zhi-Qiang Chi, Yu-Qiang Ding, Yu-Jun Wang, Jing-Gen Liu
BACKGROUND AND PURPOSE: Exposure to opiates induces locomotor sensitization in rodents, which has been proposed to correspond to the compulsive drug-seeking behavior. Numerous studies have demonstrated that locomotor sensitization can occur in a dopamine transmission-independent manner, however, the underlying mechanisms are unclear. EXPERIMENTAL APPROACH: The coimmunoprecipitation, BRET and cross-antagonism assays were used to demonstrating the existence of receptor heterodimers...
June 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28606851/cardiorespiratory-action-of-opioid-tachykinin-agonist-peptide-hybrid-in-anaesthetized-rats-transduction-pathways
#17
Piotr Wojciechowski, Małgorzata Szereda-Przestaszewska, Andrzej Wojciech Lipkowski
AWL3106 composed of opioid (dermorphin) and tachykinin (substance P7-11) pharmacophores is a new compound with high analgesic potency and markedly reduced ability to induce tolerance and dependence. The present study aimed to determine the respiratory and cardiovascular responses evoked by this peptide in urethane-chloralose anaesthetized, spontaneously breathing rats in the presence or absence of vagal connection. Intravenous injection of AWL3106 at a dose of 0.3μmol/kg in intact rats resulted in apnoea lasting 5...
June 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28606631/restraint-stress-enhances-alcohol-intake-in-adolescent-female-rats-but-reduces-alcohol-intake-in-adolescent-male-and-adult-female-rats
#18
Aranza Wille-Bille, Ana Ferreyra, Martina Sciangula, Florencia Chiner, Michael E Nizhnikov, Ricardo Marcos Pautassi
Adolescents may be more sensitive to stress-induced alcohol drinking than adults, which would explain the higher prevalence of alcohol abuse and dependence in late adolescence than in adulthood. The present study analyzed the impact of restraint stress on the initiation of alcohol intake across 2 weeks of intermittent, two-bottle choice intake in male and female adolescent rats and adult female rats. Restraint stress significantly increased alcohol intake and preference in female adolescent rats but decreased alcohol intake and preference in male adolescent and female adult rats...
June 10, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28604788/long-term-efficacy-and-safety-of-nalfurafine-hydrochloride-on-pruritus-in-chronic-liver-disease-patients-patient-reported-outcome-based-analyses
#19
Kenya Kamimura, Takeshi Yokoo, Hiroteru Kamimura, Akira Sakamaki, Satoshi Abe, Atsunori Tsuchiya, Masaaki Takamura, Hirokazu Kawai, Satoshi Yamagiwa, Shuji Terai
BACKGROUND AND AIM: Among various symptoms accompanied with chronic liver disease, pruritus affects the quality of life of patients, causing physical and mental stress, and worsens hepatic function. Recently, κ-opioid receptor agonist, nalfurafine hydrochloride was approved to treat central pruritus in patients with liver disease in Japan. This study aimed to assess the long-term efficacy and safety of nalfurafine hydrochloride on pruritus in chronic liver disease patients. METHODS: A patient-reported outcome using questionnaire-based methods was used for 41 liver disease patients with or without pruritus symptoms...
2017: PloS One
https://www.readbyqxmd.com/read/28603962/novel-opioid-analgesics-and-side-effects
#20
Giovanna Del Vecchio, Viola Spahn, Christoph Stein
Conventional opioids mediate analgesia as well as severe adverse effects via G-protein coupled opioid receptors (OR) in both inflamed (peripheral injured tissue) and healthy (brain, intestinal wall) environments. To exclude side effects, OR activation can be selectively achieved in damaged tissue by lowering the pKa of an opioid ligand to the acidic pH of inflammation. As a result, protonation of the ligand and consequent OR binding and activation of G-proteins is pH- and injury-specific. A novel compound (NFEPP) demonstrates the feasibility of this approach and displays blockade of pain transmission only at the peripheral site of injury, but with lack of central and gastrointestinal adverse effects...
June 12, 2017: ACS Chemical Neuroscience
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