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• 产品描述： Meptazinol Hcl, a unique centrally opioid analgesic, is used as a narcotic antagonist with analgesic properties.

• 靶点： Opioid Receptor

• 体内研究： Naloxonazine treatment 24 hr earlier attenuates Meptazinol (10 mg/kg i.v.) analgesia in both the mouse writhing and rat tail-flick assays. Meptazinol administered with morphine does not reverse the respiratory depressant actions seen with morphine alone, distinguishing meptazinol from other mixed agonist/antagonists. The absorption of Meptazinol (8 mg/kg i.v.) from nasal cavity to systemic circulation is rapid and complete in male Sprague-Dawley rats. The maximum observed concentration is achieved at 15 min after administration and the absolute bioavailability is 96.06%. The cerebrospinal fluid level of Meptazinol (8 mg/kg i.v.) attains a high concentration of 2.71 μg/mL and then is followed by an exponential decline. The concentration of intravenous Meptazinol (8 mg/kg i.v.) achieves a peak at 10 min followed by a steep decline in the cortex dialysate. Inclusion of Meptazinol (2 mg/kg) reduces the total dose of anaesthetic required, allows a more rapid recovery and is associated with less movement in response to surgery in cystoscopy patients. The patients in the control group tends to hyperventilate, and has lower end-tidal CO2 tension, and also higher pulse rates during surgery than the Meptazinol group. Meptazinol (25 mg/kg) evokes larger increases in nociceptive thresholds in the mouse than in the rat, whereas morphine induces large increases in both species. Antinociceptive responses to Meptazinol are consistently inhibited in animals pretreated with naloxone, whereas scopolamine attenuates th

• 参考文献：
  1. Hargreaves J, et al. Anaesthesia, 1985, 40(5), 490-493. 2. Fagbemi O, et al. Br J Pharmacol, 1983, 78(3), 455-460. 3. Spiegel K, et al. J Pharmacol Exp Ther, 1984, 228(2), 414-419. 4. Shi Z, et al. Life Sci, 2005, 77(20), 2574-2583. 5. Bill DJ, et al. Br J Pharmacol, 1983, 79(1), 191-199.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.706 ml	18.532 ml	37.063 ml
  5 mM	0.741 ml	3.706 ml	7.413 ml
  10 mM	0.371 ml	1.853 ml	3.706 ml
  50 mM	0.074 ml	0.371 ml	0.741 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *