Search results for " Opioid"
showing 10 items of 218 documents
Nociceptin/orphanin FQ opioid receptor (NOP) selective ligand MCOPPB links anxiolytic and senolytic effects
2021
Accumulation of senescent cells may drive age-associated alterations and pathologies. Senolytics are promising therapeutics that can preferentially eliminate senescent cells. Here, we performed a high-throughput automatized screening (HTS) of the commercial LOPAC®Pfizer library on aphidicolin-induced senescent human fibroblasts, to identify novel senolytics. We discovered the nociceptin receptor FQ opioid receptor (NOP) selective ligand 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole (MCOPPB, a compound previously studied as potential anxiolytic) as the best scoring hit. The ability of MCOPPB to eliminate senescent cells in in vitro models was further tested…
Opiate-induced dopamine release is modulated by severity of alcohol dependence: an [(18)F]fallypride positron emission tomography study.
2011
Background Preclinical data implicate the reinforcing effects of alcohol to be mediated by interaction between the opioid and dopamine systems of the brain. Specifically, alcohol-induced release of β-endorphins stimulates μ-opioid receptors (MORs), which is believed to cause dopamine release in the brain reward system. Individual differences in opioid or dopamine neurotransmission have been suggested to be responsible for enhanced liability to abuse alcohol. In the present study, a single dose of the MOR agonist remifentanil was administered in detoxified alcohol-dependent patients and healthy control subjects to mimic the β-endorphin-releasing properties of ethanol and to assess the effect…
Intraventricular insulin decreases kappa opioid-mediated sucrose intake in rats.
2002
The hormone insulin acts in the central nervous system (CNS) as a regulator of body adiposity and food intake. Recent work from our laboratory has provided evidence that one way by which insulin may decrease food intake is by decreasing the rewarding properties of food. Evidence from others suggests that endogenous opioids may mediate the palatable properties of foods, and insulin may decrease nonfood-related reward via interaction with some CNS kappa opioid systems. In the present study we examined the ability of insulin to interact with exogenous or endogenous kappa opioids to modulate feeding of palatable sucrose pellets by nondeprived rats. Insulin (5 mU intracerebroventricular (i.c.v.)…
Synthetic studies of neoclerodane diterpenoids from Salvia splendens and evaluation of opioid receptor affinity
2008
Abstract Salvinorin A ( 1 ), a neoclerodane diterpene from the hallucinogenic mint Salvia divinorum , is the only known non-nitrogenous and specific κ-opioid agonist. Several structural congeners of 1 isolated from Salvia splendens ( 2 – 8 ) together with a series of semisynthetic derivatives ( 9 – 24 ), some of which possess a pyrazoline structural moiety ( 9 , 19 – 22 ), have been tested for affinity at human μ, δ, and κ opioid receptors. None of these compounds showed high affinity binding to these receptors. However, 10 showed modest affinity for κ receptors suggesting that other natural neoclerodanes from different Salvia species may possess opioid affinity.
TAP Block Prior to Open Ventral Hernia Repair Improves Surgical Outcome.
2022
Abstract Background Ventral hernias commonly affect patients after major abdominal surgery. To reduce postoperative pain, the effects of the transversus abdominis plane (TAP) block, epidural analgesia and medication-only protocol have been investigated. The primary outcome was the cumulative dosage of opioids (morphine milligram equivalents MME), of acetaminophen and diclofenac for postoperative pain control on postoperative day (POD) 0, 1, and 2. Secondary outcomes were length of stay (LOS) and the pain scale rating using the numeric rating scale (NRS) on POD 0, 1, and 2. Methods The data were retrospectively extracted from the charts of the patients admitted for a surgical operation for O…
Sympathetic blocks for visceral cancer pain management: A systematic review and EAPC recommendations.
2015
The neurolytic blocks of sympathetic pathways, including celiac plexus block (CPB) and superior hypogastric plexus block (SHPB) , have been used for years. The aim of this review was to assess the evidence to support the performance of sympathetic blocks in cancer patients with abdominal visceral pain. Only comparison studies were included. All data from the eligible trials were analyzed using the GRADE system. Twenty-seven controlled studies were considered. CPB, regardless of the technique used, improved analgesia and/or decrease opioid consumption, and decreased opioid-induced adverse effects in comparison with a conventional analgesic treatment. In one study patients treated with superi…
Maddalena Opioid Switching Score in patients with cancer pain
2021
Evaluation of opioid switching (OS) for cancer pain has not been properly assessed. The aim of this study was to assess an integrated score (Maddalena Opioid Switching Score) as a simple and repeatable tool to evaluate the outcomes of OS, facilitating the interpretation and comparison of studies, and information exchange among researchers. The integrated score took into account pain intensity, intensity of opioid-related symptoms, and cognitive function by using an author's formula. Physical and psychological symptoms were evaluated by the Edmonton Symptom Assessment Scale and Patient Global Impression (PGI) by the minimal clinically important difference. One hundred six patients were analy…
Methadone as First-line Opioid for the Management of Cancer Pain
2022
Abstract Aim The aim of this study was to assess the efficacy and adverse effects of methadone when used as first-line therapy in patients that are either receiving low doses of opioids or none. Methods Patients with advanced cancer were prospectively assessed. Opioid-naive patients (L-group) were started with methadone at 6 mg/day. Patients receiving weak or other opioids in doses of <60 mg/day of OME (H-group) were started with methadone at 9 mg/day. Methadone doses were changed according to the clinical needs to obtain the most favorable balance between analgesia and adverse effects. Edmonton Symptom Asssement Score (ESAS), Memorial Delirium Assessment Score (MDAS), doses of metha…
On the opioid receptor subtype inhibiting the evoked release of 3H-noradrenaline from guinea-pig atria in vitro
1986
1. Guinea-pig isolated atria were incubated and loaded with 3H-(−)-noradrenaline. The intrinsic nerves were stimulated with trains of 5 or 35 field pulses (4 Hz), and the evoked efflux of 3H-noradrenaline and of total tritium was determined in the presence of atropine, corticosterone, desipramine, and phentolamine by liquid scintillation spectrometry. 2. Ethylketocyclazocine (1.4 nmol/l, IC50), MR 2033 (9.1 nmol/l), dynorphin A (1–13) (25 nmol/l, peptidase inhibitors present), etorphine (71 nmol/l), and [d-Ala2, d-Leu5]-enkephalin (>10 μmol/l, peptidase inhibitors present) inhibited the stimulation-evoked efflux of 3H-noradrenaline in a concentration-dependent manner, but not morphine up to…
Strengths and Weaknesses of Cancer Pain Management in Italy: Findings from a Nationwide SIAARTI Survey
2022
Objectives: Despite guidelines, a large percentage of cancer patients continue to suffer from ineffectively treated pain. The authors undertook this survey to assess the strengths and weaknesses of cancer pain management in Italy. Design: This was a prospectively administered survey. Participants: The participants were anesthesiologists of the Italian Society of Anesthesia, Analgesia, Resuscitation and Intensive Care (SIAARTI). Intervention: A 58-item questionnaire covered the demographics and features of cancer pain management in the Italian context. Results: The authors received responses from 611 pain therapists of 279 centers. Only 22% of physicians are exclusively pain therapists. Seve…