Objectives: Crocin, a constituent of saffron and yellow gardenia, possesses anti-nociceptive effects. In the present study, we investigated the effects of intra-fourth ventricle injection of crocin in a rat model of orofacial pain. The contribution of opioid system was assessed using intra-fourth ventricle injection of naloxone, an opioid receptor antagonist. Materials and Methods: A guide cann...

INTRODUCTION Opioids are needed for postoperative pain in spine surgery patients, but opioid-induced constipation is a harmful adverse event. The aim of this clinical trial was to compare the use of a controlled-release oxycodone-naloxone combination product with oxycodone controlled-release tablets in these patients. The main outcome measure was the prevalence of constipation at 7 days postope...

Rationale: Cinnamoylquinides are formed from the corresponding chlorogenic acids during coffee roasting. Instant coffee has been shown to displace binding of the mu opioid receptor antagonist, [H]naloxone, but the putative active agent, feruloylquinide, has not been characterized. Objectives: The goal was to identify the active agent(s) in coffee by measuring the binding affinity of individual ...

Opioids are broad-spectrum analgesics with potent pain-relieving qualities but also with potential adverse effects related to both short-term and long-term therapy. Researchers have attempted to alter existing opioid analgesics, utilize different routes/formulations, or combine opioid analgesics with other compounds in efforts to improve analgesia while minimizing adverse effects. Exogenous opi...

The most highly abused prescription drugs are opioids used for the treatment of pain. Physician-reported drug-seeking behavior has resulted in a significant health concern among doctors trying to adequately treat pain while limiting the misuse or diversion of pain medications. In addition to abuse liability, opioid use is associated with unwanted side effects that complicate pain management, in...

Novel bioactive opioid mimetic agonists containing 2',6'-dimethyl-l-tyrosine (Dmt) and a pyrazinone ring interact with mu- and delta-opioid receptors. Compound 1 [3-(4' -Dmt-aminobutyl)-6-(3'-Dmt-aminopropyl)-5-methyl-2(1H)pyrazinone] exhibited high mu-opioid receptor affinity and selectivity (K(i)mu = 0.021 nM and K(i)delta/K(i)mu = 1,519, respectively), and agonist activity on guinea pig ileu...

opioids are widely used for the treatment of malignant and non-malignant pains. these medications are accompanied by adverse effects, in particular gastrointestinal symptoms known as opioid bowel dysfunction (obd). the most common symptom of obd is refractory constipation that is usually stable regardless of the use of laxatives. narcotic bowel syndrome (nbs) is a subset of obd described as amb...

objective: in this study, the current literatures on the use of herbs and herbal preparations of traditional chinese and indian medicine for the treatment of opioid addiction were reviewed. methods: search was done in databases such as pub med, science direct, scopus, springer link, and google scholar. results: among 18 retrieved studies, 3 studies were about asafetida extract, an approved prep...

Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African sleeping sickness, resulted in the identification of a number of compounds with selective antiproliferative activity over mammalian cells. These included (+)-(1R,2R)-U50488, a weak opioid agonist with an EC(50) value of 59 nM as determined in o...

Bioactivity-guided fractionation of the leaves of Salvia divinorum has resulted in the isolation of three new neoclerodane diterpenoids: divinatorin D (1), divinatorin E (2), and salvinorin G (3), together with 10 known terpenoids, divinatorin C (4), hardwickiic acid (5), salvinorin-A (6), -B (7), -C (8), -D (9), -E (10), and -F (11), presqualene alcohol (12), and (E)-phytol (13). The structure...