Sharma Sunita, Lata S, Kumar A, Srivastava V K
Department of Pharmacology, L.L.R.M. Medical College, Meerut-250 004.
Indian J Physiol Pharmacol. 2002 Apr;46(2):235-40.
Analgesic, antipyretic and anti-inflammatory activities of newly synthesized spirobarbitunylphenothiazines viz 10-[7, 11-Di(4-4' dimethoxphenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5.5] undecane 1, 5 dione] acetylphenothiazine (test drug A) and 10-[7, 11-Di (N.N-dimethylaminophenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5, 5] undecane-1, 5 dione] acetylphenothiazine (test drug B) have been screened in Swiss mice and Wistar rats. The peripheral analgesic activity of test drugs A and B was investigated by acetic acid induced writhing test in Swiss mice while the central analgesic action was assessed by hot-wire (tail flick test) of the analgesiometer and tail-clip test in Wistar rats. Antipyretic activity was assessed on Brewer's yeast induced pyrexic model while antiinflammatory activity was seen on carrageenan induced hind paw oedema. Analgesic activity was found to be only of peripheral type as there was reduction of 66% in writhing responses by test drugs A and B in dose of 80 mg/kg in mice. No change in the tail flick responses was observed on analgesiometer or by tail clip by both the test drugs. Reduction of 1.5 to 2.0 degrees C in rectal temperature was observed in pyretic rats by test drugs A and B in dose of 80 mg/kg. 80% reduction in paw volume was noted in 80 mg/kg dose of both the test drugs which was comparable to the anti-inflammatory activity of 300 mg/kg, p.o. of phenylbutazone.
新合成的螺巴比妥基吩噻嗪类药物,即10-[7,11-二(4,4'-二甲氧基苯基)-3-氧代-9-甲基氨基亚氨基-2,4-二氮杂螺[5.5]十一烷-1,5-二酮]乙酰吩噻嗪(受试药物A)和10-[7,11-二(N,N-二甲基氨基苯基)-3-氧代-9-甲基氨基亚氨基-2,4-二氮杂螺[5,5]十一烷-1,5-二酮]乙酰吩噻嗪(受试药物B)的镇痛、解热和抗炎活性已在瑞士小鼠和Wistar大鼠中进行了筛选。受试药物A和B的外周镇痛活性通过瑞士小鼠的醋酸诱导扭体试验进行研究,而中枢镇痛作用则通过Wistar大鼠的热丝(甩尾试验)和镇痛仪以及尾夹试验进行评估。解热活性在啤酒酵母诱导的发热模型上进行评估,抗炎活性则在角叉菜胶诱导的后爪水肿模型上观察。发现镇痛活性仅为外周型,因为受试药物A和B在小鼠中80mg/kg剂量时扭体反应减少了66%。两种受试药物在镇痛仪上或通过尾夹试验均未观察到甩尾反应的变化。受试药物A和B在80mg/kg剂量时使发热大鼠的直肠温度降低了1.5至2.0摄氏度。两种受试药物在80mg/kg剂量时爪体积减少了80%,这与口服300mg/kg苯基丁氮酮的抗炎活性相当。