Analgesic combination of sodium channel blockers with opioid antagonists
A technology of opioid receptors and derivatives, which can be used in the treatment of various diseases - especially in the application field of pain, and can solve the problems of drug resistance of analgesia, adverse reactions of patients, and limited pain relief.
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Embodiment 1
[0117] pain test
[0118] After mice were anesthetized, the sciatic nerve was exposed by blunt dissection, freeing it from the surrounding tissue. Subsequently, 4 ligatures (5-0 chrome gut, 1-2 mm apart) were performed on the sciatic nerve (Bennett and Xie, 1998). In order to obtain a satisfactory clipping effect, the standard developed by Bennett and Xie (1988) was used for operation.
[0119] In mice with ligated sciatic nerves, the mechanical pain threshold (expressed in grams (g)) was determined by the method of Randall and Selitto (1957) by gradually applying pressure to the injured innervated hind paw until retraction Foot reflexes and hissing (vocalization).
[0120]Test rats were first given naloxone or normal saline, and 15 minutes later subcutaneously injected TTX at a dose of 3 μg / kg. The administration concentration of naloxone was 0.5 mg / kg, and the rats in the control group were treated with placebo (0.09% NaCl) at the same time and environment. Each test mou...
Embodiment 2
[0124] Pain Trials Using Opioid Agonists
[0125] The treatment of the test rats was as in Example 1.
[0126] Inject morphine or saline 15 minutes before TTX. Thirty minutes after TTX injection, pressure thresholds were recorded every 30 minutes until 2 hours. The data at each time point are the mean±S.E.M of the pressure threshold of the test rats (one stress threshold per rat), as indicated in parentheses.
[0127] The concentration of morphine used was 3 mg / kg, the dose of TTX was 3 μg / kg, and the rats in the control group were treated with placebo (0.09% NaCl) at the same time and environment. Each rat received only one treatment (one compound, single dose) and was administered only once.
[0128] Data are reported as mean ± S.E.M. Non-parametric Kruskal-Wallis (1952) one-way analysis of variance (ANOVA) was used for analysis, and Mann-Whitney test was used for comparison between groups. The area under the curve (AUC) was calculated using the trapezoidal method. The...
Embodiment 3
[0131] The effect of TTX on μ-opioid receptors, especially the effect of TTX chronic in vivo administration on μ-opioid receptor signaling
[0132] The aim of the trial was to examine the effect of TTX on altered opioid receptor modulation, which is associated with opioid resistance / dependence. The test model is: ligand binding test and functional evaluation of subcellular fractions on rat brain tissue (Szucs and Coscia, 1992; Fabian et al., 2002). The effects of the drug on intracellular mu opioid receptors are described in detail.
[0133] Materials and methods
[0134] animal
[0135] Female Wistar rats, weighing about 200 g, were randomly assigned to different experimental groups, with 5 rats in each group. Rats were individually housed in small wire cages during drug treatment and maintained on a 12-h diurnal cycle, with free access to food and water during the test period. All drug treatments were completed within the same time period on the same day (7:00-8:00, 17:0...
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