Yanagi Y, Kurokawa H, Koga Y, Awata H, Inukai T
Nihon Yakurigaku Zasshi. 1978 Sep;74(6):735-47. doi: 10.1254/fpj.74.735.
Potency of analgetic activity of SL-573 was between that of indomethacin and aminopyrine in chemical stimulation tests. The analgetic activity of SL-573 was 3.2 times as potent as that of aminopyrine in the phenylquinone writhing test, 4.1 times as potent as aminopyrine in the acetic acid writhing test and 6.3 times as potent as aminopyrine in the Randall and Selitto test. Thus the analgetic activity of SL-573 appears to be comparable etic to that of codeine. SL-573, unlike narcotic analgesics, showed common properties to known antipyretic analgesics and anti-inflammatory agents in the following points. (1) Analgetic activity was not evident in the mechanical stimulation or in the heat stimulation tests. (2) The analgetic activity was not antagonized by naloxone. (3) SL-573 showed no antagonistic effect to morphine. (4) Tolerance to the analgetic activity of SL-573 was not observed after a one week pretreatment with this compound. (5) SL-573 had no effect on the evoked potentials recorded from cells in the pain pathway of CNS and the site of action of analgetic effect was considered to be in peripheral sites of the sensory neurons. The antipyretic activity of SL-573 was equal to that of aminopyrine in febrile rabbits and 4 times as potent as that of aminopyrine in febrile rats. This compound did not affect normal body temperature of rabbits and rats, this observation being similar to that noted with antipyretic analgesics and nonsteroidal anti-inflammatory agents.
在化学刺激试验中，SL - 573的镇痛活性强度介于吲哚美辛和氨基比林之间。在苯醌扭体试验中，SL - 573的镇痛活性是氨基比林的3.2倍；在醋酸扭体试验中，是氨基比林的4.1倍；在Randall和Selitto试验中，是氨基比林的6.3倍。因此，SL - 573的镇痛活性似乎与可待因相当。与麻醉性镇痛药不同，SL - 573在以下方面表现出与已知解热镇痛药和抗炎药的共同特性。(1)在机械刺激或热刺激试验中，镇痛活性不明显。(2)镇痛活性不受纳洛酮拮抗。(3)SL - 573对吗啡无拮抗作用。(4)用该化合物预处理一周后，未观察到对SL - 573镇痛活性的耐受性。(5)SL - 573对中枢神经系统疼痛通路中细胞记录的诱发电位无影响，镇痛作用的作用部位被认为是感觉神经元的外周部位。在发热兔中，SL - 573的解热活性与氨基比林相当；在发热大鼠中，是氨基比林的4倍。该化合物不影响兔和大鼠的正常体温，这一观察结果与解热镇痛药和非甾体抗炎药相似。
