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https://www.readbyqxmd.com/read/28213593/randomised-double-blind-parallel-group-placebo-controlled-study-to-evaluate-the-analgesic-efficacy-and-safety-of-vvz-149-injections-for-postoperative-pain-following-laparoscopic-colorectal-surgery
#1
Srdjan S Nedeljkovic, Darin J Correll, Xiaodong Bao, Natacha Zamor, Jose L Zeballos, Yi Zhang, Mark J Young, Johanna Ledley, Jessica Sorace, Kristen Eng, Carlyle P Hamsher, Rajivan Maniam, Jonathan W Chin, Becky Tsui, Sunyoung Cho, Doo H Lee
INTRODUCTION: In spite of advances in understanding and technology, postoperative pain remains poorly treated for a significant number of patients. In colorectal surgery, the need for developing novel analgesics is especially important. Patients after bowel surgery are assessed for rapid return of bowel function and opioids worsen ileus, nausea and constipation. We describe a prospective, double-blind, parallel group, placebo-controlled randomised controlled trial testing the hypothesis that a novel analgesic drug, VVZ -149, is safe and effective in improving pain compared with providing opioid analgesia alone among adults undergoing laparoscopic colorectal surgery...
February 17, 2017: BMJ Open
https://www.readbyqxmd.com/read/28212204/1-2-4-dibromophenyl-3-6-6-trimethyl-1-5-6-7-tetrahydro-4h-indazol-4-one-a-novel-opioid-receptor-agonist-with-less-accompanying-gastrointestinal-dysfunction-than-morphine
#2
Po-Kuan Chao, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Ming-Fu Cheng, Jian-Ying Chuang, Chiung-Tong Chen, Chuan Shih, Shiu-Hwa Yeh
BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5)...
February 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28211895/electroacupuncture-attenuates-cfa-induced-inflammatory-pain-by-suppressing-nav1-8-through-s100b-trpv1-opioid-and-adenosine-pathways-in-mice
#3
Hsien-Yin Liao, Ching-Liang Hsieh, Chun-Ping Huang, Yi-Wen Lin
Pain is associated with several conditions, such as inflammation, that result from altered peripheral nerve properties. Electroacupuncture (EA) is a common Chinese clinical medical technology used for pain management. Using an inflammatory pain mouse model, we investigated the effects of EA on the regulation of neurons, microglia, and related molecules. Complete Freund's adjuvant (CFA) injections produced a significant mechanical and thermal hyperalgesia that was reversed by EA or a transient receptor potential V1 (TRPV1) gene deletion...
February 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28206989/il-4-mediated-by-hsv-vector-suppresses-morphine-withdrawal-response-through-decreasing-tnf%C3%AE-nr2b-and-pc-ebp%C3%AE-in-the-periaqueductal-gray-in-rats
#4
H Yi, T Iida, S Liu, D Ikegami, Q Liu, A Iida, D A Lubarsky, S Hao
Chronic opiates induce the development of physical dependence. Opioid physical dependence characterized by withdrawal symptoms, may have very long-lasting effects on the motivation for reward, including the incubation of cue-induced drug-seeking behavior. Elucidation of the mechanisms involved in physical dependence is crucial to developing more effective treatment strategies for opioid dependence. Chronic morphine induces production of proinflammatory cytokines in regional-specific sites of the brain. Interleukin-4 (IL-4) is a prototypical anti-inflammatory cytokine that globally suppresses proinflammatory cytokines...
February 16, 2017: Gene Therapy
https://www.readbyqxmd.com/read/28203347/killing-two-birds-with-one-stone-successful-opioid-monotherapy-in-intractable-migraine-triggered-epilepsy-a-case-series
#5
REVIEW
Iraj Derakhshan
The novel concept explored in this case series is the primacy of headaches in generating seizures in those patients who suffer from migraine-triggered epilepsy. In this series, once the migraine headaches were fully suppressed, via daily scheduled opioid therapy, the seizures also stopped. Seizures returned, however, after the patients stopped the opiate regimen for any reason. The above pharmacological scenario is reminiscent of a similar but naturalistic course of events reported on the salutary effects of ketogenic diet, or changes in life style, in similar cases of migraine-triggered epilepsy...
January 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/28199982/n-acetyl-cysteine-attenuates-remifentanil-induced-postoperative-hyperalgesia-via-inhibiting-matrix-metalloproteinase-9-in-dorsal-root-ganglia
#6
Yue Liu, Yuan Ni, Wei Zhang, Yu-E Sun, Zhengliang Ma, Xiaoping Gu
Treatment of remifentanil-induced postoperative hyperalgesia (RIH) remains a clinical challenge because the mechanisms are not fully understood. Matrix metalloproteinase-9 (MMP-9) is a key component in neuroinflammation because of its facilitation of pro-inflammatory cytokine maturation. Therefore, inhibition of MMP-9 may represent a novel therapeutic approach to the treatment of RIH. Sprague-Dawley rats were randomly divided into three groups: Control, Incision and Remifentanil. A right plantar surgical incision was performed in Group Incision, and intraoperative remifentanil (0...
February 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28190898/synthesis-and-opioid-receptor-binding-of-indium-iii-and-111-in-labeled-macrocyclic-conjugates-of-diprenorphine-novel-ligands-designed-for-imaging-studies-of-peripheral-opioid-receptors
#7
Shefali Srivastava, Emily A Fergason-Cantrell, Roger I Nahas, John R Lever
Radiolabeled diprenorphine (DPN) and analogs are widely used ligands for non-invasive brain imaging of opioid receptors. To develop complementary radioligands optimized for studies of the peripheral opioid receptors, we prepared a pair of hydrophilic DPN derivatives, conjugated to the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), for complexation with trivalent metals. The non-radioactive indium (III) complexes, tethered to the C6-oxygen position of the DPN scaffold by 6- to 9-atom spacers, displayed high affinities for binding to μ, δ and κ opioid receptors in vitro...
October 6, 2016: Tetrahedron
https://www.readbyqxmd.com/read/28190392/pi3k-akt-pathway-a-potential-therapeutic-target-for-chronic-pain
#8
Shu-Ping Chen, Ya-Qun Zhou, Dai-Qiang Liu, Wen Zhang, Anne Manyande, Xue-Hai Guan, Yu-Ke Tian, Da-Wei Ye, Deeq Mohamed Omar
Chronic pain is among the most disabling and costly disorders, with prevalence ranging from 10% to 55%. However, current therapeutic strategies for chronic pain are unsatisfactory due to our poor understanding of its mechanisms. Thus, novel therapeutic targets need to be found in order to improve these patients' quality of life. PI3K and its downstream Akt are widely expressed in the spinal cord, particularly in the laminae I-IV of the dorsal horn, where nociceptive C and Aδ fibers of primary afferents principally terminate...
February 10, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28188777/enhanced-ability-of-trpv1-channels-in-regulating-glutamatergic-transmission-after-repeated-morphine-exposure-in-the-nucleus-accumbens-of-rat
#9
Haitao Zhang, Dong Jia, Yuan Wang, Liang Qu, Xuelian Wang, Jian Song, Lijun Heng, Guodong Gao
Glutamatergic projections to nucleus accumbens (NAc) drive drug-seeking behaviors during opioids withdrawal. Modulating glutamatergic neurotransmission provides a novel pharmacotherapeutic avenue for treatment of opioids dependence. Great deals of researches have verified that transient receptor potential vanilloid 1 (TRPV1) channels alters synaptic transmitter release and regulate neural plasticity. In the present study, whole-cell patch clamp recordings were adopted to examine the activity of TRPV1 Channels in regulating glutamate-mediated excitatory postsynaptic currents (EPSCs) in NAc of rat during morphine withdrawal for 3 days and 3 weeks...
February 7, 2017: Brain Research
https://www.readbyqxmd.com/read/28182123/long-term-safety-and-analgesic-efficacy-of-buprenorphine-buccal-film-in-patients-with-moderate-to-severe-chronic-pain-requiring-around-the-clock-opioids
#10
Martin Hale, Veronica Urdaneta, M Todd Kirby, Qinfang Xiang, Richard Rauck
BACKGROUND: This open-label, single-arm study was conducted to evaluate the long-term safety and efficacy of a novel buprenorphine formulation, buprenorphine buccal film, in the treatment of moderate-to-severe chronic pain requiring around-the-clock opioids. METHODS: The primary purpose of this study was to evaluate the long-term safety and tolerability of buprenorphine buccal film. Five hundred and six patients who completed previous studies with buprenorphine buccal film (n=445; rollover patients) or were recruited de novo for this study (n=61) were enrolled in this study...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28166793/cytotoxic-t-cells-modulate-inflammation-and-endogenous-opioid-analgesia-in-chronic-arthritis
#11
Uta Baddack-Werncke, Melanie Busch-Dienstfertig, Sara González-Rodríguez, Santhosh Chandar Maddila, Jenny Grobe, Martin Lipp, Christoph Stein, Gerd Müller
BACKGROUND: This study examined the development of chronic pain, a cardinal symptom of rheumatoid arthritis (RA), in mice with antigen- and collagen-induced arthritis (ACIA). Since the role of CD8(+) T cells in arthritis is controversial, we investigated the consequences of CD8-depletion on arthritis development and opioid modulation of pain in this novel model of chronic autoimmune arthritis. METHODS: Disease severity in control and CD8-depleted animals was determined by histological assessment of knee-joint sections and measurement of autoantibody formation...
February 6, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28163104/age-dependent-regulation-of-gaba-transmission-by-kappa-opioid-receptors-in-the-basolateral-amygdala-of-sprague-dawley-rats
#12
K R Przybysz, D F Werner, M R Diaz
Anxiety disorders are one of the most common and debilitating mental illnesses worldwide. Growing evidence indicates an age-dependent rise in the incidence of anxiety disorders from adolescence through adulthood, suggestive of underlying neurodevelopmental mechanisms. Kappa opioid receptors (KORs) are known to contribute to the development and expression of anxiety; however, the functional role of KORs in the basolateral amygdala (BLA), a brain structure critical in mediating anxiety, particularly across ontogeny, are unknown...
February 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28162693/-442-pharmacodynamic-data-assessing-the-abuse-potential-of-a-novel-abuse-deterrent-oxycodone-formulation-eli-200-compared-to-oxycodone-immediate-release-oral-intact-eli-200-and-placebo-in-healthy-non-dependent-recreational-opioid-users-following-intranasal
#13
B Setnik, K Schoedel, C Bartlett, C Dick, N Hakim, P Geoffroy
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28162663/-421-a-novel-non-opioid-conesnail-peptide-based-analgesic-as-a-therapeutic-alternative-for-the-treatment-of-chronic-pain
#14
J Mercado, M Xu, K Norton, D Peckham, J Posakony, E Tarcha, J Bartron, M Brown, K Lustig, L Manelli, C Ghelardini, B Cheppudira, M Fowler, S Christensen, J McIntosh, S Iadonato
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28162601/-361-a-novel-g-protein-biased-kappa-opioid-that-displays-analgesic-but-not-dysphoric-actions-in-the-rat
#15
T Martin, S Kim, J Rose, S Jones, J Aubé, L Bohn
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28158929/the-analgesic-and-anti-inflammatory-effects-of-salvinorin-a-analogue-%C3%AE-tetrahydropyran-salvinorin-b-in-mice
#16
K F Paton, N Kumar, R S Crowley, J L Harper, T E Prisinzano, B M Kivell
BACKGROUND: Drugs activating the mu opioid receptor are routinely used to treat severe acute and chronic pain. Unfortunately, side effects including nausea, constipation, respiratory depression, addiction and tolerance can limit clinical utility. In contrast, kappa opioid receptor (KOPr) agonists, such as Salvinorin A (SalA), have analgesic properties with little potential for abuse. METHODS: We evaluated SalA and the novel analogue β-tetrahydropyran Salvinorin B (β-THP SalB) for the ability to modulate pain and inflammation in vivo...
February 3, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28156579/snapshot-of-an-outpatient-supportive-care-center-at-a-comprehensive-cancer-center
#17
Maxine Grace De la Cruz, Angelique Wong, Debra Castro, Eduardo Bruera
: 145 Background: Integration of Palliative Care (PC) in oncology has been found to improve symptom distress, quality of life and survival in patients with advanced cancer. Early integration is most appropriate in the outpatient (OP) setting. However, most PC services in the U.S. do not have an OP component. Our study aims to provide a snapshot of the type of patients that are referred to this novel setting for the delivery of early PC. METHODS: We reviewed a day in the SCC to illustrate the structure and process involved in the delivery of outpatient PC...
October 9, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28146271/liposomal-bupivacaine-infiltration-at-the-surgical-site-for-the-management-of-postoperative-pain
#18
REVIEW
Thomas W Hamilton, Vassilis Athanassoglou, Stephen Mellon, Louise H Strickland, Marialena Trivella, David Murray, Hemant G Pandit
BACKGROUND: Despite multi-modal analgesic techniques, acute postoperative pain remains an unmet health need, with up to three quarters of people undergoing surgery reporting significant pain. Liposomal bupivacaine is an analgesic consisting of bupivacaine hydrochloride encapsulated within multiple, non-concentric lipid bi-layers offering a novel method of sustained-release analgesia. OBJECTIVES: To assess the analgesic efficacy and adverse effects of liposomal bupivacaine infiltration at the surgical site for the management of postoperative pain...
February 1, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28144772/a-combined-opiate-agonist-and-antagonist-treatment-reduces-prolactin-secreting-pituitary-tumor-growth
#19
George Maglakelidze, Olivia Wynne, Dipak K Sarkar
Prolactin secreting pituitary adenomas (prolactinomas) is the most common pituitary tumors in humans. Animal studies have identified aggressive prolactinoma development in fetal alcohol exposed rats. We have recently identified a combination treatment of a μ opioid receptor antagonist naltrexone and a δ opioid receptor agonist D-Ala2-,N-Me-Phe4,Gly-ol Enkephalin (DPDPE) increases innate immune function. In this study, we tested whether naltrexone and DPDPE combination therapy is useful to control pituitary tumor growth...
January 31, 2017: Journal of Cell Communication and Signaling
https://www.readbyqxmd.com/read/28142305/effects-of-acute-and-repeated-treatment-with-the-biased-mu-opioid-receptor-agonist-trv130-oliceridine-on-measures-of-antinociception-gastrointestinal-function-and-abuse-liability-in-rodents
#20
Ahmad A Altarifi, Bethany David, Karan H Muchhala, Bruce E Blough, Hamid Akbarali, S Stevens Negus
RATIONALE: TRV130 (oliceridine; N-[(3-methoxythiophen-2-yl)methyl]-2-[(9 R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethanamine) is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs. Prevailing evidence suggests that TRV130 and other G-protein-biased MOR agonists may produce therapeutic analgesic effects with reduced adverse effects compared to existing MOR agonists. OBJECTIVES: This study compared the effects of acute and repeated TRV130 administration on measures of antinociception, gastrointestinal function, and abuse liability in rodents...
January 1, 2017: Journal of Psychopharmacology
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