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Opiod receptor

Xinxin Song, Shan Zhu, Yangchun Xie, Jiao Liu, Lingyi Sun, Dexing Zeng, Pengcheng Wang, Xiaochao Ma, Guido Kroemer, David L Bartlett, Timothy R Billiar, Michael T Lotze, Herbert J Zeh, Rui Kang, Daolin Tang
BACKGROUND & AIMS: Maintenance of acid-base homeostasis is required for normal physiology, metabolism, and development. It is not clear how cell death is activated in response to changes in pH. We performed a screen to identify agents that induce cell death in a pH-dependent manner (we call this alkaliptosis) in pancreatic ductal adenocarcinoma cancer (PDAC) cells and tested their effects in mice. METHODS: We screened a library of 254 compounds that interact with G-protein-coupled receptors (GPCRs) to identify those with cytotoxic activity against a human PDAC cell line (PANC1)...
April 2018: Gastroenterology
Jens Engel-Andreasen, Isabelle Wellhöfer, Kathrine Wich, Christian A Olsen
The 1,2,3-triazole moiety can be incorporated as a peptide bond bioisostere to provide protease resistance in peptidomimetics. Herein, we report the synthesis of peptidomimetic building blocks containing backbone-fluorinated 1,4-disubstituted 1,2,3-triazole moieties. Synthetic protocols for the preparation of various Xaa-Gly dipeptide surrogates in the form of Xaa-ψ[triazole]-F2Gly building blocks were established, and selected examples were introduced into the endogenous peptide opioid receptor ligand Leu-enkephalin as a model compound...
October 16, 2017: Journal of Organic Chemistry
Ismaliza Ismail, Suzaily Wahab, Hatta Sidi, Srijit Das, Loo Jiann Lin, Rosdinom Razali
Kratom (Mitragynaspeciosa), a natural existing plant found in South-East Asia, is tradi-tionally used as an herb to help to elevate a person's energy and also to treat numerous medical ailments. Other than the analgesic property, kratom has been used as an agent to overcome opioid withdrawal as it contains natural alkaloids, i.e. mitragynine, 7-hydroxymitragynine, and MGM-9, which has agonist affinity on the opioid receptors, including mu (μ) and kappa (κ). The role of neural reward pathway linked to μ-opioid receptors and both dopaminergic and GABA-ergic interneurons that express μ-opioid receptors were deliberated...
April 25, 2017: Current Drug Targets
E Scarpellini, A Pauwels, R Vos, N Rommel, J Tack
BACKGROUND: Endogenous opioids (EO) acting on μ-opiod receptors in central and enteric nervous system (ENS) control gastrointestinal motility but it is still unclear whether EO in ENS may control esophageal function in man, thus we will study the effects of methylnaltrexone (MNTX), a peripherally selective, and naloxone (NA), a non-selective μ-opiod receptor antagonist, on esophageal motility in healthy subjects. METHODS: Fifteen HV (6 M; 34.1 ± 0.6 years; BMI: 22...
March 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
Andreas Link, Christa E Müller
Together forever? Functional selection was applied to finally achieve separation of the analgesic properties of opiods from serious side effects such as potentially lethal respiratory depression. A Gi-biased μ-opioid-receptor agonist (PZM21) was identified that stabilizes previously unexplored receptor conformations. This compound relieves pain in mice without causing hypoventilation or addiction.
December 23, 2016: Angewandte Chemie
Renato Leonardo de Freitas, Priscila Medeiros, Juliana Almeida da Silva, Rithiele Cristina de Oliveira, Ricardo de Oliveira, Farhad Ullah, Asmat Ullah Khan, Norberto Cysne Coimbra
It has been proposed that the post-ictal state is associated with the expression of hypoalgesia. It is clear that the projections among the periaqueductal gray matter (PAG), dorsal raphe nucleus (DRN) and locus coeruleus (LC) play a role in pain management. These mesencephalic structures have direct reciprocal opioid and monoaminergic projections to the LC that can possibly modulate post-ictal hypoalgesia. The goal of this study was to examine if LC-opioid and serotonergic/noradrenergic mechanisms signal the post-ictal hypoalgesic responses to tonic-clonic seizures produced by intraperitoneal administration of pentylenetetrazole (PTZ at 64mg/kg), causing an ionophore γ-aminobutyric acid (GABA)-mediated Cl- influx antagonism...
November 12, 2016: Neuroscience
Nunzio Vicario, Rosalba Parenti, Giuseppina Arico', Rita Turnaturi, Giovanna Maria Scoto, Santina Chiechio, Carmela Parenti
No abstract text is available yet for this article.
2016: Molecular Pain
George E Woody, Evgeny Krupitsky, Edwin Zvartau
Naltrexone is an antagonist that binds tightly to μ-opioid receptors and blocks the subjective and analgesic effects of opioids. It does not produce physiologic dependence and precipitates withdrawal if administered to an opioid dependent person, thus starting it must begin with detoxification. It was first available in the mid-1970s as a 50 mg tablet that blocked opioids for 24-36 h if taken daily, or every 2-3 days at higher doses - for example: 100 mg Monday and Wednesday, 150 mg on Friday. From a pharmacological perspective it worked very well and was hoped to be an effective treatment but results were disappointing due to low patient interest and high dropout followed by relapse...
September 2016: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
Neel Mehta, Kelli O'Connell, Gregory P Giambrone, Aisha Baqai, Sudhir Diwan
OBJECTIVE: Constipation is a common adverse effect in patients requiring long-term opioid therapy for pain control. Methylnaltrexone, a quaternary peripheral mu-opioid receptor antagonist, is an effective treatment of opioid induced constipation (OIC) without affecting centrally mediated analgesia. Our objective was to conduct a review and meta-analysis to evaluate the efficacy of methylnaltrexone for treatment of OIC, as well as to provide a clinical discussion regarding newly developed alternatives and provide the current treatment algorithm utilized at our institution...
2016: Postgraduate Medicine
Pierre-Eric Lutz, Yi Zhou, Aurélie Labbe, Naguib Mechawar, Gustavo Turecki
The nociceptin/orphanin FQ (N/OFQ)-Nociceptin Opiod-like Peptide (NOP) receptor system is a critical mediator of physiological and pathological processes involved in emotional regulation and drug addiction. As such, this system may be an important biological substrate underlying psychiatric conditions that contribute to the risk of suicide. Thus, the goal of the present study was to characterize changes in human N/OFQ and NOP signaling as a function of depression, addiction and suicide. We quantified the expression of N/OFQ and NOP by RT-PCR in the anterior insula, the mediodorsal thalamus, and the dorsal anterior cingulate cortex (dACC) from a large sample of individuals who died by suicide and matched psychiatrically-healthy controls...
November 2015: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Iraia Muñoa, Itziar Urizar, Luis Casis, Jon Irazusta, Nerea Subirán
The most well-known physiological effect associated with opiod system is their efficacy in pain reduction or analgesia, although their effect on a variety of other physiological and physiophological functions has become apparent in recent years. This review is an attempt to clarify in more detail the epigenetic regulation of opioid system to understand with more precision their transcriptional and posttranscriptional regulation in multiple pyisiological and pharmacological contexts. The opioid receptors show an epigenetic regulation and opioid peptide precursors by methylation, chromatin remodeling and microRNA...
November 2015: Journal of Cellular Biochemistry
Amanda S Mota, Anderson B de Lima, Thayana Lucy F Albuquerque, Tiago S Silveira, José Luiz M do Nascimento, Joyce Kelly R da Silva, Alcy F Ribeiro, José Guilherme S Maia, Gilmara N T Bastos
Seed oil (Pp-oil) of Plukenetia polyadenia is used by native people of the Brazilian Amazon against arthritis and rheumatism, spreading it on the arms and legs to reduce the pain and inflammation. Pp-oil was obtained by pressing dried seeds at room temperature to give a 47.0% yield of oil. It was then subjected to fatty acid composition analysis. The principal fatty acids were linoleic acid (46.5%), α-linolenic acid (34.4%) and oleic acid (13.9%). Then, it was evaluated for its antinociceptive activity in mice, using the acetic acid-induced abdominal writhing, hot plate and formalin test models...
2015: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Shaima Salman, Josef Buttigieg, Colin A Nurse
The adrenal medulla plays a key role in the physiological responses of developing and mature mammals by releasing catecholamines (CAT) during stress. In rodents and humans, the innervation of CAT-producing, adrenomedullary chromaffin cells (AMCs) is immature or absent during early postnatal life, when these cells possess 'direct' hypoxia- and CO2/H(+)-chemosensing mechanisms. During asphyxial stressors at birth, these mechanisms contribute to a CAT surge that is critical for adaptation to extra-uterine life...
March 1, 2014: Journal of Experimental Biology
Zaher Radi, Phillip Bartholomew, Michael Elwell, W Mark Vogel
In humans, hibernoma is a very rare, benign neoplasm of brown adipose tissue (BAT) that typically occurs at subcutaneous locations and is successfully treated by surgical excision. No single cause has been accepted to explain these very rare human tumors. In contrast, spontaneous hibernoma in rats is rare, often malignant, usually occurs in the thoracic or abdominal cavity, and metastases are common. In recent years, there has been an increased incidence of spontaneous hibernomas in rat carcinogenicity studies, but overall the occurrence remains relatively low and highly variable across studies...
December 15, 2013: Toxicology and Applied Pharmacology
Gina Games, Amber Hutchison
With the prevalence of diabetes mellitus (DM) increasing, pathologic complications such as diabetic peripheral neuropathy (DPN) are also becoming more common. Of those diagnosed with DM, 10% to 20% of patients suffer from painful DPN. Until recently, only pregabalin and duloxetine possessed Food and Drug Administration (FDA) approval for this condition. However, FDA recently approved tapentadol-ER [extended release] (Nucynta ER) for painful DPN. Tapentadol-ER is an opioid analgesic commonly used for the treatment of moderate-to-severe chronic pain that contains a unique dual mechanism acting as both a weak mu-opiod receptor agonist and norepinephine-reuptake inhibitor...
October 2013: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
Nawaz Ahmed Shaik, Surisetty Sreenivasa Rao, Sunil Chiruvella, Manduri Sreenivasa Rao, Siddareddigari Velayudha Reddy
BACKGROUND: The peripheral nerve endings carrying pain contains opiod receptors. Blocking these receptors during haematoma block or periosteal block may provide better analgesia. AIM: Evaluation of effectiveness and safety of butorphanol as an adjuvant to lidocaine for haematoma block. SETTINGS AND DESIGN: This is a two centre, prospective, individually randomised, two group, parallel, double-blind clinical trial. METHODS: In this study, 115 American society of anaesthesiologist grade I and II adult patients scheduled for closed reduction of fractures were randomly allocated into two groups; Group A received 1% lidocaine (2 mg/kg) where as Group B received 1% lidocaine (2 mg/kg) with butorphanol (0...
March 2013: Indian Journal of Anaesthesia
Elzbieta P Wala, Joseph R Holtman, Paul A Sloan
BACKGROUND: Opioids may cause progressive enhancement of pain sensitivity (opioid-induced hyperalgesia [OIH]) and thus, exacerbate existing pain. Animal studies also demonstrate paradoxical OIH with an ultralow dose (ULD, subanalgesic) of opioid; eg, the μ-opioid, morphine. Repeated administration of ULD-morphine resulted in tolerance to ULD-OIH. Prior exposure to ULD-morphine prolonged subsequent morphine antinociception in intact rats (delay of tolerance) and blocked neuropathic pain in nerve-injured rats (no hyperalgesia)...
March 2013: Journal of Opioid Management
Shanna L Resendez, Brandon J Aragona
Social bonds are important for human health and well-being, and a crucial component of these bonds is the ability to maintain a bond once it has been formed. Importantly, although bond maintenance is required for social attachments, very little is known about the neural mechanisms that mediate this behavior. Recently, laboratory studies utilizing the socially monogamous prairie vole (an excellent animal model for the neurobiology of selective social attachment), have allowed the neural correlates of selective social attachment to begin to unfold...
2013: Reviews in the Neurosciences
Peck Y Ong
Various new agents are in the research pipeline for atopic dermatitis. These include IL-4 receptor antagonist, cis-urocanic acid, κ-opiod receptor agonist, neurokinin receptor antagonist and antimicrobial peptide. The current review updates the status of these clinical trials and provides insight into other potential molecular targets including IL-22 and TLR-2.
June 2012: Expert Opinion on Emerging Drugs
Jo Lynne Herzog, James A Solomon, Zoe Draelos, Alan Fleischer, Dow Stough, David I Wolf, William Abramovits, William Werschler, Emma Green, Maeve Duffy, Alan Rothaul, Robert Tansley
OBJECTIVE: To investigate the efficacy, safety and tolerability of topical nalmefene (SRD174), a long acting opioid antagonist for the management of pruritus associated with atopic dermatitis (AD). DESIGN: Double-blind, vehicle-controlled, randomized, cross-over trial. SETTING: Eleven dermatology outpatient clinics in the U.S. PATIENTS: Sixty-two out of 136 screened adult subjects with confirmed AD affecting is less than or equal to 20% of body surface area and with moderate-to-severe pruritus...
August 2011: Journal of Drugs in Dermatology: JDD
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