AN-132 block of cardiac sodium channels: A gate-related receptor analysis

Summary Based on the gate-related receptor hypothesis, an analysis of kinetics of AN-132, a new antiarrhythmic agent, blockade of cardiac sodium channels and the gate-related receptor which is bound by the drug was performed by computer simulation. Model-predicted apparent rates of onset of AN-132 (30 μmol/L) blocking were 0.051, 0.038, and 0.034 AF⁻¹ at stimulation frequencies of 1.0, 2.0 and 3.0 Hz, respectively. The time constant of recovery from block by AN-132 at resting potential -90 mV was 39.5 s. These findings are in agreement with those experimental data documented. The analysis of gate-related receptor shows that AN-132 binds the inactivation gate-related receptor, and the binding and unbinding are modulated by the inactivation process.     

Spinal cholinergic and monoamine receptors mediate the antinociceptive effect of morphine microinjected in the periaqueductal gray on the rat tail, but not the feet

The antinociceptive effects of morphine (5 μg) microinjected into the ventrolateral periaqueductal gray were determined using both the tail flick and the foot withdrawal responses to noxious radiant heating in lightly anesthetized rats. Intrathecal injection of appropriate antagonists was used to determine whether the antinociceptive effects of morphine were mediated byα₂-noradrenergic, serotonergic, opioid, or cholinergic muscarinic receptors. The increase in the foot withdrawal response latency produced by microinjection of morphine in the ventrolateral periaqueductal gray was reversed by intrathecal injection of the cholinergic muscarinic receptor antagonist atropine, but was not affected by the a2-adrenoceptor antagonist yohimbine, the serotonergic receptor antagonist methysergide, or the opioid receptor antagonist naloxone. In contrast, the increase in the tail flick response latency produced by morphine was reduced by either yohimbine, methysergide or atropine. These results indicate that microinjection of morphine in the ventrolateral periaqueductal gray inhibits nociceptive responses to noxious heating of the tail by activating descending neuronal systems that are different from those that inhibit the nociceptive responses to noxious heating of the feet. More specifically, serotonergic, muscarinic cholinergic andα₂-noradrenergic receptors appear to mediate the antinociception produced by morphine using the tail flick test. In contrast, muscarinic cholinergic, but not monoamine receptors appear to mediate the antinociceptive effects of morphine using the foot withdrawal response.     

Comparative study of three fluorescent dyes for angiography: sodium fluorescein, carboxyfluorescein, and calcein

To compare the characteristics of carboxyfluorescein (CF) and calcein (Calc) with those of sodium fluorescein (Naf), the only fluorescent dye currently in clinical use, we performed angiography in rabbits and primates using these three dyes. The circulation decay time of all dyes was longer in primates than in rabbits. In primates, CF and Calc had longer decay times than Naf. Calc produced the greatest contrast between the choroidal and retinal vasculature. Tissue staining and dye leakage into the vitreous immediately after retinal photocoagulation were minimal with Calc, moderate with CF, and marked with Naf. The limited leakage and longer circulation time of Calc may permit simultaneous angiography and photocoagulation therapy without obscuring the fundus view with leaking dye from the photocoagulated structure.     

聚对苯乙炔（PPV）及其衍生物的研究进展

评价了ＰＰＶ系列衍生物的电学性质、非线性光学性质及其应用。     

手术治疗胫腓骨远端骨折36例

目的 :探讨胫腓骨远端骨折治疗术式的选择、术中术后应注意的问题及其疗效。方法 :对不同类型的胫腓骨远端骨折 36例进行 8～ 18个月的随访 ,并结合临床及影像学资料 ,对其诊断、手术方法及治疗效果进行分析总结。结果 :本组术后 2 5～ 3 5个月骨折均愈合。踝关节功能优良率 77 7%。结论 :熟悉骨折的分型及相应内固定术式的选择 ;注重踝穴骨折的解剖复位及固定和踝关节的功能位固定及早期功能锻炼。     

抗真菌剂三氮唑含硫化合物的合成

合成了１３个三氮唑含硫化合物，均为未见文献报道的新化合物，对所合成的化合物，选择三种常见真菌进行体外最低抑菌浓度（ＭＩＣ）的测定，结果表明它们均有较好的抗真菌活性，有些化合物抑菌活性极高，有进一步研究和开发前景。     

Extraction, purification and ascertainment of anti-hepatoma active principles for targeted preparation of radix Aconiti Kusnezoffii]

The extraction, purification, pharmacological experiments and chemical analysis of anti-hepatoma active principles of Radix Aconiti Kusnezoffii have been studied. The results show that the medicinal material Radix Aconiti Kusnezoffii is efficacious in inhibiting hepatoma, and the active principles are mainly made up of poisonous ester alkaloids. The liver targeting delivery system will be the first choice for its anti-hepatoma preparation, and the effective component AY3a is fit for the preparation of targeted microspheres.     

Acute psychotropic effects of bilateral subthalamic nucleus stimulation and levodopa in Parkinson's disease.

High-frequency deep brain stimulation (DBS) of the subthalamic nucleus (STN) improves the motor symptoms of Parkinson's disease (PD). Opposite changes in mood, such as mania or depression, have been reported after surgery, but it is not known whether these side effects are specifically related to STN DBS. To learn whether STN DBS also influences the limbic loop, we investigated acute subjective psychotropic effects related to levodopa or bilateral STN DBS. After a median postoperative follow-up of 12 months, 50 PD patients completed the Addiction Research Center Inventory (ARCI), assessing subjective psychotropic effects in four conditions: off-drug/on-stimulation; off-drug/off-stimulation; on-drug/off-stimulation; and on-drug/on-stimulation. Both levodopa and STN DBS improved all the ARCI subscales, indicating subjective feelings of well being, euphoria, increase in motivation, and decrease in fatigue, anxiety, and tension. A suprathreshold dose of levodopa was significantly more effective than STN DBS, using the same electrical parameters as for chronic stimulation, on four of the five ARCI subscales. We concluded that 1) both STN DBS and levodopa have synergistic acute beneficial psychotropic effects in PD, 2) the psychotropic effects of both treatments need to be considered in the long-term management of chronic STN DBS, and 3) the results indicate an involvement of the limbic STN in mood disorders of PD.     

In vitro evaluation of ablation parameters of normal and fibrous aorta using smooth excimer laser coronary angioplasty

A modified exeimer laser energy delivery system was used to irradiate 100 segments of normal and fibrous aorta in vitro. The laser beam was scanned into 8 fiber bundles consisting of 50 fibers each resulting in a reduction of the applied pulse energy. The total repetition rate was increased to 150 Hz in order to keep the repetition rate per fiber bundle close to 20 Hz and to minimize thermal injury. The results demonstrate that effective ablation (etch rate per 8 pulses > 2.0 μm) occurred at an energy fluency of 50 mJ/mm² in both normal and fibrous aorta. Tissue damage (carbonization, tissue separation, fissures, cracks, and vacuolization) was in a range of 100 ± 28 to 152 ± 30 μm for normal aorta and in a range of 57 ± 35 to 110 ± 39 μm for fibrous aorta. We conclude that effective ablation of normal and fibrous human aorta can be achieved by the application of smooth excimer laser coronary angioplasty. This improvement of excimer laser technology may result in a reduction of shock wave- and cavitation-induced damage leading to a reduction of tissue injury. However, this awaits further in vitro and in vivo confirmation. © 1993 Wiley-Liss, Inc.     

VACUOLE SIGN AND SMALL NODE SIGN IN EARLY PERIPHERAL LUNG CANCER PATHOLOGIC BASIS AND DIAGNOSTIC VALUE

Radiologic and pathologic mani;estations of 30 peripheral pulmonary masses around l.5-3 cm in dia- meter were compared to the pathologic basis of va- cuole sign and small node sign on tomogram. Stati stics of 100 conventional X-ray tomograms of peri- pheral pulmonary masses about l-3 cm in diameter suggested that the vacuole sign and small node sign, more common in early peripheral lung cancer than in tuberculoma, are valuable for differentiating early peripheral lung cancer from tuberculoma.