Nakazawa M, Yoshimura T, Naito J, Azuma H
Nihon Yakurigaku Zasshi. 1978 May;74(4):467-72.
N-5' shows a potent inhibitory action on the homologous passive cutaneous anaphylaxis (PCA) in rats mainly through the inhibition of histamine release from mast cells. The present experiment was an attempt to clarify in detail the pharmacological properties of N-5'. Inhibition of PCA was most potent at 30 or 60 min pretreatment with N-5', and negligible at 240 min pretreatment. Given p.o., N-5' produced a dose-dependent, potent inhibitory action at 30-min pretreatment. On the other hand, disodium cromoglycate (DSCG) had little effect on PCA when given orally. On the case of i.v. administration, N-5' (20 mg/kg) and DSCG (5 mg/kg) showed a most potent inhibition of PCA at 5 min pretreatment. The inhibitory action of DSCG was, however, shorter lasting than that of N-5'. Median effective doses (ED50) of DSCG and N-5' on the PCA were estimated to be 0.79 and 8.8 mg/kg i.v., respectively. Inhibitory activity of N-5' in the adrenalectomized rat did not differ from that in sham operated animals. N-5' had a more potent inhibitory action on the PCA in infant rats than in adults. Inhibitory activity of N-5' in the case of 1, 2, 3 and 4 weeks of successive administration was equipotent to that with a single administration.
N - 5’对大鼠同种被动皮肤过敏反应(PCA)显示出强大的抑制作用,主要是通过抑制肥大细胞释放组胺。本实验旨在详细阐明N - 5’的药理特性。在N - 5’预处理30或60分钟时,对PCA的抑制作用最强,而在预处理240分钟时可忽略不计。口服给药时,在预处理30分钟时,N - 5’产生剂量依赖性的强大抑制作用。另一方面,口服色甘酸钠(DSCG)对PCA几乎没有影响。静脉注射时,N - 5’(20mg/kg)和DSCG(5mg/kg)在预处理5分钟时对PCA显示出最强的抑制作用。然而,DSCG的抑制作用持续时间比N - 5’短。DSCG和N - 5’对PCA的半数有效剂量(ED50)经估计分别为静脉注射0.79和8.8mg/kg。N - 5’在肾上腺切除大鼠中的抑制活性与假手术动物中的无差异。N - 5’对幼鼠PCA的抑制作用比对成年大鼠更强。连续给药1、2、3和4周时,N - 5’的抑制活性与单次给药时相当。