In earlier studies, it was shown that male rats were considerably more sensitive to the antinociceptive properties of morphine than females in several antinociceptive assays. The purpose of our studies was to examine whether these male-female differences might be due to differences in the blood and brain levels of morphine attained after its s.c. injection rather than to intrinsic differences i...

Forty patients were allocated randomly to receive one of four premedications i.m.: placebo only, morphine 10 mg plus placebo, morphine 10 mg plus cisapride 10 mg and morphine 10 mg plus cisapride 4 mg. Gastric emptying after each premedication was assessed using the oral paracetamol absorption model. The morphine only group and the morphine and cisapride 4 mg group showed delayed gastric emptyi...

A new, pharmacologically active morphine derivative, 6-succinylmorphine, was synthesized. The properties of this compound and evidence for its structure are presented. Succinylmorphine was covalently coupled to ethylamino-Sepharose. Morphine-Sepharose containing up to 40 mug of morphine did not block the electrically stimulated contraction of isolated guinea pig ileum, but after alkaline hydrol...

In our previous study, we reported that chronic morphine exposure changes neuronal response properties in rat somatosensory cortex. In this study, we investigated the effect of chronic morphine treatment on tactile learning behavior in rats. Morphine sulfate was dissolved in tap water, and was administered for 21 days. Tactile learning was assessed using the novel object recognition test (NORT)...

Morphine is a schedule II-controlled substance that used to allow the diminution of intra-operative, post-operative or chronic pain. However, its usage limited due addiction and overdose liabilities. was observed cause tolerance, dependence withdrawal in human. Justification: date lack scientific evidence morphine carried out by using specific single human neuroblastoma cell-line (SK-N-SH). The...

In a rat model of morphine tolerance, we examined the hypotheses that thermal hyperalgesia to radiant heat develops in association with the development of morphine tolerance and that both the development and expression of thermal hyperalgesia in morphine-tolerant rats are mediated by central NMDA and non-NMDA receptors and subsequent protein kinase C (PKC) activation. Tolerance to the analgesic...

BACKGROUND AND PURPOSE Opioids, such as morphine, are the most effective treatment for pain but their efficacy is diminished with the development of tolerance following repeated administration. Recently, we found that morphine activated ERK in opioid-tolerant but not in naïve rats, suggesting that morphine activation of μ-opioid receptors is altered following repeated morphine administration. H...

Repeated administration of opioids produces long-lasting changes in micro-opioid receptor (MOR) signaling that underlie behavioral changes such as tolerance. Mitogen-activated protein kinase (MAPK) pathways, including MAPK extracellular signal-regulated kinases (ERK1/2), are modulated by opioids and are known to produce long-lasting changes in cell signaling. Thus, we tested the hypothesis that...

BACKGROUND This study examined the opioid-sparing effectiveness, analgesic efficacy, and tolerability of postoperative administration of the parenteral cyclooxygenase 2 selective inhibitor, parecoxib sodium, in total hip arthroplasty patients. METHODS This was a multicenter, multiple-dose, randomized, double-blind, placebo-controlled study to compare the opioid-sparing effects, analgesic effi...

Morphine exhibits important pharmacological effects for which it has been used in medical practice for quite a long time. However, it has a high addictive potential and can be abused. Long-term use of this drug can be connected with some pathological consequences including neurotoxicity and neuronal dysfunction, hepatotoxicity, kidney dysfunction, oxidative stress and apoptosis. Therefore, most...