双氯芬酸钠-β-环糊精包合物制备工艺的研究

本文采用正交试验法研究了β-环糊精对双氯芬酸的包合作用。以包合物的收率、含量作为考察指标，筛选出最佳包合条件为A1B3C3D2，即β-环糊精与双氯苯酸钠的摩尔比为1：1，包合温度为80℃，包合时间为5h，搅拌强度为中等。用IR、DSC证明包合物的形成。     

ACUTE LITHIUM ADMINISTRATION IMPAIRS THE ACTION OF PARATHYROID HORMONE ON RAT RENAL CALCIUM,MAGNESIUM AND PHOSPHATE TRANSPORT*

1. Chronic lithium (Li⁺) treatment commonly produces a state of hyperparathyroidism in humans and rat although the mechanism is unknown. 2. The present study evaluated the acute effect of Li⁺ on renal electrolyte transport, particularly Ca²⁺ and Mg²⁺ in thyroparathyroidectomized (TPTX) and intact rats. 3. The acute administration of Li⁺ significantly increased water, sodium, potassium and phosphate excretion in both TPTX and intact animals; however, Ca²⁺ and Mg²⁺ excretion was only increased in the intact group. Fractional excretion (FE) of Ca²⁺ and Mg²⁺ increased from 2.2±0.2 to 3.5±0.3% and 12±2 to 18±2%, respectively (P<0.01). 4. In further experiments in TPTX rats, Li⁺ administration inhibited the usual reduction in urine Ca²⁺ and Mg²⁺ excretion following parathyroid hormone (PTH) administration and inhibited the phosphaturia. However, supramaximal concentrations of PTH overcame this inhibitory effect. For example, an FE_Ca of 3.8±0.2% was reduced to 1.4±0.2% and 1.7±0.2% with maximal and supramaximal PTH concentrations, respectively, while in the presence of Li⁺ an FE_ca of 4.0±0.2 was decreased to 2.8±0.2 and then 1.9±0.3% with the same PTH concentrations. 5. The inhibitory effect of Li⁺ was reduced with a lower plasma Li⁺ concentration (0.7±0.2 vs 1.6–1.8 mmol/L). The FE_Mg results were comparable. 6. These results demonstrate that Li⁺ directly inhibits PTH-mediated renal reabsorption of Ca²⁺ and Mg²⁺ and also blunts PTH-mediated phosphaturia. Therefore, the hyperparathyroidism in humans following Li⁺ treatment may be a consequence of reduced renal Ca²⁺ reabsorption.     

Interactions between sodium balance, intrarenal dopamine synthesis, and sympathetic activity in HLA-identical kidney donors and recipients

Intrarenal dopamine (DA) synthesis, sympathetic activity andsodium homeostasis were studied in eight HLA-identical kidneyrecipient and donor pairs at 50, 150, and 300 mmol sodium intake.Trimethaphan was given intravenously (i.v.), to mimic acutedenervation, tyramine i.v. to induce noradrenaline (NE) release,and the DA precursor DOPA i.v. to study DOPA to DA conversion.Blood pressure was higher in the recipients (P<0.05) andwas not influenced by sodium intake. Cumulative sodium balanceswere not different between the groups. Sodium intake did notaffect DA excretion in either group. The recipients had higherDA (P<0.05) and DOPA (P<0.01) excretions and lower urinaryDA over DOPA ratio (U_DA/DOPA, P<0.01) and lower NE excretion(P<0.05) during the whole study. High sodium intake suppressedthe U_DA/DOPA in both groups (P<0.05). Trimetaphan decreasedrenal vascular resistance (RVR) and increased sodium excretiononly in the donors (P<0.05), while GFR increased in bothgroups. During HiSo tyramine increased RVR in the recipients(P<0.01) and U_DA/DOPA in the donors (P<0.05). DOPA infusionincreased DA excretion four to fivefold but did not change sodiumexcretion in either group. It is concluded that the recipientsmaintained sodium homeostasis well but seem to have an impairedfunctional innervation of the transplanted kidney. NE releaseseem to stimulate intrarenal DOPA to DA conversion. In bothgroups a direct relation between DA and sodium excretion waslacking.     

阿托品对兔局部脑缺血Ca2+积累和细胞水肿的作用

阿托品对兔局部脑缺血Ｃａ２＋积累和细胞水肿的作用吕爱刚胡香杰贾丹辉张贵卿可君（河南医科大学药理学教研室，郑州４５００５２）阿托品（ａｔｒｏｐｉｎｅ，Ａｔｒ）为一典型的Ｍ受体阻断剂，近年研究表明它可以选择性对抗ＫＣｌ和ＣａＣｌ２对兔基底动脉收缩作用，其...     

Increased human erythrocyte sodium-Iithium countertransport in hyperlipidaemic patients may indicate increased membrane lipid fluidity

Abstract. Erythrocyte sodium-lithium countertransport (SLC) activity, membrane fluidity, plasma trigly-ceride and cholesterol were measured in hyperlipidaemic patients and normal subjects. Fluidity was assessed by the fluorescence anisotropy (inversely related to fluidity) of the probes 1,6-diphenyl-1,3,5-hexatriene (DPH) and 1,4-trimethylammonium-3,5-hexatriene (TMA-DPH). In a second group of patients the maximum velocity (Vmax) and external sodium affinity constant (k_m) of SLC was also measured.
In the first group of patients, SLC activity was increased compared with the controls (0.279 ± 0.019 vs. 0.213 ± 0.013, P = 0.006) as was membrane fluidity in the deep hydrophobic regions (DPH anisotropy 0.211 ± 0.0007 vs. 0.215 ± 0.0011, P = 0.007). There was a strong correlation between SLC and DPH anisotropy (Rs= -0.72, P= < 0.001) which was due to the correlation between Vmax and DPH anisotropy (Rs=-0.90, P= < 0.001).
Increases in Vmax of SLC in hyperlipidaemic patients may be due to differences in lipid organisation in the deep hydrophobic regions of the membrane which may affect the turnover rate of the transporter.     

ANTEROVENTRAL WALL OF THE THIRD VENTRICLE AND DORSAL LAMINA TERMINALIS: HEADQUARTERS FOR CONTROL OF BODY FLUID HOMEOSTASIS?

1. The subfornical organ, median preoptic nucleus and the organum vasculosum of the lamina terminalis (OVLT) are a series of structures situated in the anterior wall of the third ventricle and form the lamina terminalis. The OVLT and ventral part of the median preoptic nucleus are part of a region known as the anteroventral third ventricle region.
2. Data from many laboratories, using techniques ranging from lesions, electrophysiology, neuropharmacology, Fos expression, immunohistochemistry and receptor localization, indicate that the tissue in the lamina terminalis plays a major role in many aspects of body fluid and electrolyte balance.
3. The subfornical organ and OVLT lack the blood-brain barrier and detect alterations in plasma tonicity and the concentrations of circulating hormones such as angiotensin II and possibly atrial natriuretic peptide and relaxin.
4. This information is then integrated within the lamina terminalis (probably in the median preoptic nucleus) with neural signals from other brain regions. The neural output from the lamina terminalis is distributed to a number of effector sites including the paraventricular (both parvo- and magno-cellular parts) and supraoptic nuclei and influences vasopressin secretion, water drinking, salt intake, renin secretion, renal sodium excretion and cardiovascular regulation.     

Effects of tetrodotoxin monoclonal antibody on the blocking action of tetrodotoxin on sodium channels

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DL-酒石酸的诱导拆分

将(±)-酒石酸制成其钠铵盐,在27℃以下进行诱导拆分,得(+)-和(-)-酒石酸钠铵,经转化为钙盐,再处理精制可得合格的(+)-和(-)-酒石酸。总收率为91%以上。