Pharmaceutical composition for treating withdrawal syndrome
A composition and syndrome technology, applied in the field of indole derivatives or their salts, can solve the problems of general effect of treating withdrawal syndrome and the like, and achieve the effects of no adverse reactions, low toxicity and convenient medication
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Embodiment 1
[0022] Example 1: Synthesis of 2-bromo-N-acetyl-5-methoxytryptamine
[0023] N-bromosuccinimide (NBS, 0.89g, 5mM) was slowly added to anhydrous acetic acid solution of melatonin (1.16g, 5mM) under stirring, stirred at room temperature for 3 hours under nitrogen, and ice water Cool and neutralize to neutral with 50% sodium hydroxide to obtain an oily suspension product. After the aqueous phase was extracted four times with chloroform, the organic phases were combined, treated with saturated sodium chloride solution, and then dried by adding anhydrous sodium sulfate. The solvent was distilled off under reduced pressure to obtain a tan oily crude product. The crude product was subjected to column chromatography on a silica gel column (mobile phase: ethyl acetate-cyclohexane=8:2) to obtain the product, which was recrystallized from ethyl acetate-cyclohexane solution to obtain the product, mp: 145-149°C.
Embodiment 2
[0024] Embodiment two: acute toxicity test
[0025] 1 Acute toxicity test in mice
[0026] The Experimental Animal Center of the Academy of Military Medical Sciences produced Kunming mice, 35-40 days old, half male and half female, female mice weighing 19.8±0.7g, and male mice weighing 21.0±0.6g. Administration method: The route of administration is intragastric administration. The experimental animals were fasted for 12 hours, and the test drugs were administered once by intragastric administration according to the same volume and different administration concentrations, and the volume was 0.5ml / animal.
[0027] After the drug, the animal moved lazily, did not eat, and became drunk after 20 minutes, and then lay still in the cage until death or recovery. The higher the dose, the more obvious it is. Surviving animals returned to normal within 1-3 days after administration.
[0028] Mice were fed with 2-bromo-N-acetyl-5-methoxytryptamine once, and the LD50 of female animals...
Embodiment 3
[0033] Example 3: Therapeutic effect on urging withdrawal symptoms in morphine-dependent mice
[0034] Kunming mice were bred by the Experimental Animal Center of the Academy of Military Medical Sciences, Grade II. Male and female are half and half, body weight is 20±2g. Morphine hydrochloride injection (manufactured by Shenyang No. 1 Pharmaceutical Factory, batch number: 040102, specification: 1ml: 10mg), naloxone hydrochloride injection (produced by Beijing Sihuan Pharmaceutical Technology Co., Ltd., batch number: 0403251, specification: 1ml: 0.4mg ), 2-bromo-N-acetyl-5-methoxytryptamine, synthesized by the Medicinal Chemistry Laboratory, Institute of Radiation and Radiation Medicine, Academy of Military Medical Sciences. Experimental equipment includes syringes, beakers, balances, gavage devices, timers and counters.
[0035] The experiment was divided into model control group, 2-bromo-N-acetyl-5-methoxytryptamine low-dose 2.5mg / kg group, middle-dose 5mg / kg group and high...
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