Tiopinac (RS 40974) (RS 40974) 是一种二苯并噻吩,是一种具有口服活性的高效抗炎和解热剂。
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Tiopinac is a highly potent anti-inflammatory, analgesic and anti-pyretic agent.
Tiopinac (0.03-110 mg/kg) has 40 times the antiphlogistic potency of phenylbutazone. The dose required to reduce paw swelling by 30% is approximately 0.5 mg/kg. Tiopinac does not elicit overt side effects at the 20 mg/kg/day dose. Tiopinac causes a dose-related reversal of the decreases body weight caused by the adjuvant disease, the weight of those rats receiving 0.135 and 0.4 mg/kg/day being significantly greater than that of the positive controls. Tiopinac (0.3-30 mg/kg) is highly potent in inhibiting the pain evoked in the yeastinflamed hind paw of the rat[1].
[1]. Rooks WH 2nd, et al. The anti-inflammatory and analgesic profile of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid (tiopinac). Agents Actions. 1980 Jun;10(3):266-73.
Animal experiment: | Female rats, 160-180 g, receive 0.1 mL of a suspension in mineral oil of heatkilled M. butyricum (10 mg/mL) by means of two intradermal injections (0.05 mL each) into the proximal 1/4 of the tail on day 0. When the test agent is studied for its activity versus the development of the arthritic syndrome, it is administered p.o. (0.5 mL vehicle/dose) twice each day (at 9 a.m. and 4 p.m.) for 17 days, beginning on day 1. On day 18 the intensity of the swelling of the four foot pads and tail is determined blindly utilizing a scoring system in which the swelling in the four paws is scored 0-4 for each paw and the tail swelling is scored 0-3. The total maximum score is 19. The body weights and the weights of both hind paws are obtained. This procedure is a modification of a system initially described by PEARSON. |
参考文献: [1]. Rooks WH 2nd, et al. The anti-inflammatory and analgesic profile of 6,11-dihydrodibenzo-[b.e.]-thiepin-11-one-3-acetic acid (tiopinac). Agents Actions. 1980 Jun;10(3):266-73. |
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