Potentiation of 2-deoxy-D-glucose antinociception, but not hyperphagia by zolantidine, a histamine (H2) receptor antagonist.

Antagonism of the histamine (H2) receptor reduces antinociception induced by naloxone-resistant foot-shock, naloxone-sensitive foot-shock, and morphine with a rank-order potency similar to their H2 antagonism. The antimetabolic glucose analog 2-deoxy-D-glucose (2DG) produces antinociceptive and hyperphagic responses that dissociate from each other and are in part mediated by opioid systems. The present study determined the effects of the brain-penetrating H2 receptor antagonist zolantidine (ZOL) on 2DG antinociception on the tail-flick and jump tests, as well as on 2DG hyperphagia, in rats. ZOL (0.01-1 mg/kg) potentiated the antinociceptive responses induced by a moderate (450 mg/kg) dose of 2DG, but had lesser effects upon antinociception induced by a lower (100 mg/kg) 2DG dose. ZOL itself slightly increased jump thresholds, but not tail-flick latencies. Combinations of ZOL and 2DG produced supraadditive antinociception, even though ZOL failed to significantly shift the 2DG dose-response curve to the left. In contrast, ZOL failed to alter basal intake or 2DG hyperphagia, supporting previous evidence implicating the H1 but not the H2 receptor in these effects. These results further dissociate the antinociceptive and hyperphagic effects of 2DG, and also support previous results indicating both pro- and antinociceptive roles for H2 receptors.     

头孢克洛在健康人体内的药物动力学研究

采用ＨＰＬＣ测定健康志愿者血浆中头孢克洛的浓度。方法简便快速，结果准确。平均回收率为１０２．１８±４．０１％，日间及日内ＲＳＤ均小于６％。血药浓度－时间曲线符合一室模型。     

豨莶脂溶性成分的研究

从豨莶(Siegesbeckia orientalis L.)的地上部分,分离出八个化合物,其中I和I根据理化性质和光谱数据确定其结构为ent-17-acetoxy-18-isobutyryloxy-16(α)-kauran-19-oicacid(I)和ent-17-ethoxy-16(α)-kauran-19-oicacid(II),均为新化合物,分别被命为豨莶酯酸(siegesesteric acid,I)和豨莶醚酸(siegesetheric acid,I)。其余化合物分别鉴定为腺梗豨莶萜醇酸(ent-16β,17-dihydroxy-kauran-19-oicacid,II),奇任醇(kirenol,IV,β-谷甾醇葡萄糖甙(β-sitosterolglucoside,V),二十一醇(heneicosanol,VI),花生酸甲酯(methyl arachidate,VII)和β-谷甾醇(β-sitosterol,VII)。除奇任醇和β-谷甾醇外,均为首次从该植物中分得。