Objective: In this study, it was aimed to investigate the antinociceptive activity potential of Tofisopam and elucidate possible involvement opioid system in effect.Material Method: The efficacy (25 50 mg/kg) evaluated by hot-plate acetic acid-induced writhing tests; while effects drug on motor coordination mice were with Rota-rod tests.Result Discussion: at a dose mg/kg significantly prolonged...

Opioids, acting at μ opioid receptors, are commonly used for pain management. Chronic opioid treatment induces cellular adaptations, which trigger long-term side effects, including constipation mediated by enteric neurons. We tested the hypothesis that chronic opioid treatment induces alterations of μ opioid receptor signaling in enteric neurons, which are likely to serve as mechanisms underlyi...

Opioid analgesics are clinically used to relieve severe pain in acute postoperative and cancer pain, also the long term chronic pain. The analgesic action is mediated by μ-, δ-, κ-receptors, but currently, with few exceptions for k-agonists, μ-agonists only ones therapy. Previously synthesized compounds diazotricyclodecane cores (DTDs) have shown their effectiveness binding opioid receptors. Fo...

We have previously shown that the balance of electrically evoked descending brainstem control of spinal nociceptive reflexes undergoes a switch from excitation to inhibition in preadolescent rats. Here we show that the same developmental switch occurs when μ-opioid receptor agonists are microinjected into the rostroventral medulla (RVM). Microinjections of the μ-opioid receptor agonist [D-Ala(2...

Acute challenges with psychostimulants such as amphetamine affect impulsive behavior in both animals and humans. With regard to amphetamine, it is important to unravel how this drug affects impulsivity since it is not only a widely abused recreational drug but also regularly prescribed to ameliorate maladaptive impulsivity. Therefore, we studied the effects of amphetamine in two rat models of i...

The discovery of the opioid receptors began in the 1970s and three (μ, δ and κ) are now recognised. Most current opioid analgesics interact preferentially with μ receptors, although some have actions at δ and κ receptors. The revelation that opioid receptors are present on peripheral sensory neurones and immune system cells, has led to the realisation that the opioid system is involved in a hos...

Opioid-induced constipation (OIC), a prevalent and distressing side effect of opioid therapy, does not reliably respond to treatment with conventional laxatives. OIC can be a treatment-limiting adverse event. Recent advances in medications with peripherally acting μ-opioid receptor antagonists, such as methylnaltrexone, naloxegol, and alvimopan, hold promise for treating OIC and thus extending ...

Placebo analgesia is one of the most robust and best-studied placebo effects. Recent researches suggest that placebo analgesia activated the μ-opioid receptor signalling in the human brain. However, whether other opioid receptors are involved in the placebo analgesia remains unclear. We have previously evoked placebo responses in mice (Guo et al. 2010, 2011) and these mice may serve as a model ...

Bupivacaine is a widely used, local anesthetic agent that blocks voltage-gated Na(+) channels when used for neuro-axial blockades. Much lower concentrations of bupivacaine than in normal clinical use, < 10(-8)  m, evoked Ca(2+) transients in astrocytes from rat cerebral cortex, that were inositol trisphosphate receptor-dependent. We investigated whether bupivacaine exerts an influence on the Ca...