速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的研究速效止咳糖浆药理作用.方法采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用.结果速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数,并延长咳嗽潜伏期;对组胺-乙酰胆碱诱发的喘息有保护作用,表现为明显抑制哮喘反应,引喘潜伏期明显延长,并可浓度依赖性的拮抗Ach的收缩支气管作用;增加小鼠气管内酚红排出量.结论速效止咳糖浆具有镇咳、平喘、祛痰作用,为临床治疗慢性支气管炎提供药理学依据.     

速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的 研究速效止咳糖药理作用。方法 采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用。结果 速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数，并延长咳嗽潜伏期；对组胺－乙酰胆碱诱发的喘息有保护作用，表现为明显抑制哮喘反应，引喘潜伏期明显延长，并可浓度依赖性的拮抗Ach的收缩支气管作用；增加小鼠气管内酚红排出量。结论 速效止咳糖浆具有镇咳、平喘、祛痰作用，为临床治疗慢性支气管炎提供药理学依据。     

速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的　研究速效止咳糖浆药理作用。方法　采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用。结果　速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数 ,并延长咳嗽潜伏期 ;对组胺 -乙酰胆碱诱发的喘息有保护作用 ,表现为明显抑制哮喘反应 ,引喘潜伏期明显延长 ,并可浓度依赖性的拮抗Ach的收缩支气管作用 ;增加小鼠气管内酚红排出量。结论　速效止咳糖浆具有镇咳、平喘、祛痰作用 ,为临床治疗慢性支气管炎提供药理学依据     

咳尔康口服液止咳祛痰平喘的实验研究

［摘要］目的观察咳尔康口服液的止咳、祛痰、平喘作用。方法采用氨水致小鼠咳嗽观察潜伏期及3 min内咳嗽次数;采用乙酰胆碱和组胺混合液致豚鼠哮喘发作观察哮喘潜伏期;采用小鼠呼吸道酚红分泌实验观察祛痰作用。结果与0.9%氯化钠溶液对照组比较,咳尔康口服液可明显延长实验动物咳嗽的潜伏期,减少咳嗽次数;明显延长哮喘发作潜伏期;极显著地增加小鼠呼吸道的酚红分泌量。结论咳尔康口服液具有镇咳、平喘和祛痰作用。     

复方紫菀合剂药效学实验研究

目的 :观察研究不同浓度的紫菀合剂止咳、祛痰、平喘作用 ,方法 :采用小鼠“浓氨水”法、“酚红”法及豚鼠“离体气管螺旋条”法观察合剂在止咳、祛痰、平喘等方面的作用。结果 :紫菀合剂对小鼠“浓氨水”法、“酚红”法诱发的咳嗽、咯痰具有明显的抑制作用。可延长咳嗽潜伏期 (P <0 .0 1) ,使咳嗽次数减少 ,排痰量增加。能降低组织胺引起的豚鼠离体气管平滑肌收缩幅度 (P <0 .0 1)。结论 :复方紫菀合剂具有明显的止咳、祛痰、平喘作用     

气管炎丸的药理学研究

目的:研究气管炎丸的止咳、平喘、祛痰作用。方法:采用豚鼠离体气管法和拘橼酸引喘法观察气管炎丸的平喘作用;用雾化氨水刺激小鼠引咳法观察该药的镇咳作用;用小鼠酚红实验观察其祛痰作用。结果:该药可以有效地降低动物由氨水刺激引咳的咳嗽次数,可以明显延长豚鼠致喘的潜伏期,对乙酰胆碱及组胺造成的豚鼠离体气管平滑肌收缩有显著的拮抗作用,可以增加小鼠气管及支气管酚红的分泌量。结论:气管炎丸具有较好的止咳、平喘、祛痰效果。     

止咳清肺口服液止咳和化痰作用的实验研究

目的观察止咳清肺口服液的止咳和祛痰作用。方法采用小鼠氨水引咳法观察镇咳作用;采用小鼠酚红排泌法观察化痰作用。结果止咳清肺口服液可显著减少氨水引起小鼠咳嗽的次数,并延长咳嗽潜伏期,明显增加小鼠气管酚红排泌量。结论止咳清肺口服液有显著的止咳和祛痰作用。     

雪梨止咳颗粒(浸膏粉)药效学研究

目的 观察雪梨止咳颗粒(浸膏粉)的止咳、化痰作用.方法 采用小鼠氨水引咳法、豚鼠柠檬酸引咳法观察雪梨止咳颗粒的止咳作用;小鼠呼吸道酚红排泌法观察其化痰作用.结果 雪梨止咳颗粒(浸膏粉)可明显延长氨水喷雾致咳小鼠的咳嗽潜伏期,显著减少其咳嗽次数;延长柠檬酸喷雾致咳豚鼠的咳嗽潜伏期,减少其咳嗽次数;增加小鼠呼吸道酚红排泌量.结论 雪梨止咳颗粒(浸膏粉)对造模小鼠、豚鼠具有止咳作用,对造模小鼠具有化痰作用.     

浙贝母叶与浙贝母花醇提物的止咳化痰平喘活性研究

目的 考察浙贝母叶与浙贝母花醇提物的止咳、化痰及平喘活性。 方法 分别采用小鼠氨水引咳法和豚鼠枸橼酸引咳法研究浙贝母叶与浙贝母花醇提物的止咳活性; 小鼠气管酚红排泌法研究化痰活性; 豚鼠整体动物引喘法研究平喘活性。 结果 浙贝母叶醇提物可明显延长小鼠和豚鼠的咳嗽潜伏期并减少咳嗽次数, 显著增加小鼠呼吸道黏膜酚红的排泌量, 显著延长豚鼠哮喘潜伏期（均 P＜ 0.05）; 浙贝母花醇提物可明显延长小鼠和豚鼠的咳嗽潜伏期并减少咳嗽次数, 显著增加小鼠呼吸道黏膜酚红的排泌量（均 P＜ 0.05）, 但不能延长豚鼠哮喘潜伏期（P＞ 0.05）。 结论 浙贝母叶醇提物具有明显的止咳、化痰及平喘活性; 浙贝母花醇提物具有明显的止咳、化痰活性, 但现有剂量下, 没有平喘活性。     

天山花楸水提取液镇咳平喘作用的实验研究

目的观察天山花楸水提取液止咳、平喘作用。方法采用氨水喷雾致小鼠咳嗽法,2%氯化乙酰胆碱和0.1%磷酸组织胺等容积混合液致豚鼠哮喘法,离体豚鼠气管螺旋条法和小鼠耳二甲苯致炎法进行实验。结果天山花楸水提取液明显减少氨水喷雾致小鼠咳嗽次数,使豚鼠哮喘潜伏期明显延长,气管解痉百分率增高,明显抑制二甲苯致小鼠的耳廓肿胀。结论天山花楸水提取液具有止咳、平喘作用。     

alpha-glucosidase (CHO) (Genzyme)

Genzyme General is developing recombinant human alpha-glucosidase, produced in mammalian cell culture, as a potential treatment for Pompe disease. By July 2004, enrollment was completed in two clinical trials and an observational study in adults. Genzyme was planning to file for regulatory approval in Europe during 2004, followed by filings in the US and Japan in mid-2005.     

(S)-oxybutynin (Sepracor)

Sepracor is developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.     

Allosteric interaction of zinc with recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) GABA(A) receptors

In a recent study we have provided evidence that inhibition of native GABA(A) receptors by zinc depends primarily on the allosteric modulation of receptor gating. Both the kinetics and the sensitivity of the GABA(A) receptor to zinc depend on subunit composition, especially on the presence of the gamma(2) subunit. To analyze the mechanism of action of zinc its effects have been tested on recombinant alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors expressed in HEK 293 cells. The currents produced by ultrafast application of GABA have been measured to assess the impact of zinc ions on GABA(A) receptor gating with resolution corresponding to the time scale of synaptic currents. While, as expected, zinc markedly reduced the peak amplitude of alpha(1)beta(2)-mediated currents, its effect on kinetics was significantly different from that observed for alpha(1)beta(2)gamma(2). In particular, unlike alpha(1)beta(2)gamma(2), zinc did not affect the onset of alpha(1)beta(2)-mediated responses. Moreover, zinc increased the extent of desensitisation of alpha(1)beta(2)gamma(2) receptors and reduced desensitisation of alpha(1)beta(2) ones. Quantitative analysis suggests that zinc exerts an allosteric modulation on both alpha(1)beta(2)gamma(2) and alpha(1)beta(2) receptors. Zinc effects on alpha(1)beta(2)gamma(2) were qualitatively similar to those reported for native receptors.     

Di(isononyl) phthalate (DINP) and di(isodecyl) phthalate (DIDP) are not mutagenic

Recently there have been reports of liver and kidney tumors in rodents following long-term exposure to di(isononyl) phthalate (DINP). Mechanistic studies suggested that the liver tumors were a consequence of peroxisomal proliferation, whereas the kidney tumors (found only in male rats) were associated with induction of alpha(2u)-globulin. Because both peroxisomal proliferation and alpha(2u)-globulin are considered to be non-genotoxic carcinogenic processes, it seemed appropriate to investigate the genotoxic potential of DINP. Additional studies were also conducted on di(isodecyl) phthalate (DIDP), a structurally related substance that also induces peroxisomal proliferation, although it has not been tested in a carcinogenicity bioassay. The DINP was tested in Salmonella, in vitro cytogenetics and mouse micronucleus assays, whereas DIDP was evaluated in a mouse micronucleus test. All of these tests produced negative results, i.e. neither phthalate was mutagenic in any of the test systems. These data are consistent with results of other published and unpublished genotoxicity tests and provide support for the hypothesis that the liver and kidney tumors induced by DINP were the result of non-genotoxic processes.     

Developmental toxicity of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Two phthalate esters, di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), have been assessed for their potential to cause developmental toxicity in the rat. Groups of 22 timed-mated Sprague-Dawley rats were administered 250, 500, or 1000 mg/kg D79P or D911P daily by oral gavage (5 ml/kg) between gestation days (GD) 1 and 19. Control animals received the vehicle (olive oil) alone. On GD20, the animals were sacrificed and the fetuses examined. Treatment resulted in no signs of maternal toxicity, as assessed by adjusted maternal bodyweight gain throughout gestation and clinical examinations, and no effects upon litter size, fetal survival or bodyweight. Pups of the high dose D79P and intermediate and high dose D911P groups showed increased incidences of supernumerary lumbar ribs. There was a significant increase in dilated renal pelves in pups of the low dose D79P and high dose D911P groups, but only for D911P was there a significant trend. Consequently, the no observed adverse effect level (NOAEL) for maternal toxicity for both D79P and D911P is 1000 mg/kg/day. The NOAEL values for developmental toxicity are 500 mg/kg/day D79P and 250 mg/kg/day D911P.     

1,2-环己二胺柠檬酸铂(Ⅱ)及异柠檬酸铂(Ⅱ)的合成和抗癌活性

报道了1,2-环己二胺异柠檬酸铂(Ⅱ)及1,2-环己二胺柠檬酸铂(Ⅱ)的合成及鉴定方法。抗癌试验表明前者在40及80mg/kg 剂量下对小鼠 L1210、P388及S180均有明显的抑瘤作用,且有部分动物可治愈;后者对 L1210也有明显的抑瘤作用,但较前者为弱。     

Two-generation reproduction toxicity studies of di-(C(7)-C(9) alkyl) phthalate and di-(C(9)-C(11) alkyl) phthalate in the rat

Di-(C(7)-C(9) alkyl) phthalate (D79P) and di-(C(9)-C(11) alkyl) phthalate (D911P), based on high-normality linear oxo-alcohols, have been assessed for their impact upon reproductive performance in Sprague-Dawley rats. Rats were continuously exposed to either D79P or D911P at dietary levels of 0%, 0.1%, 0.5%, or 1.0% over two generations. Selected F(0) offspring (F(1) generation) were exposed to the same dietary concentration of D79P or D911P as the respective F(0) animals, and were mated to produce F(1) offspring. Both D79P and D911P markedly reduced body weight gain in F(0) and F(1) adult males at the highest dose, but females were affected to a lesser extent. There was no impairment of fertility, fecundity, or development in either generation, but body weights of offspring in the 1.0% D79P and 1.0% D911P groups were slightly and transiently reduced over the weaning period. Although decreases in the weight of several organs were accounted for by depressed body weight, ovary weights were reduced in both generations exposed to 1.0% D79P, and epididymidal weights were slightly reduced in adults of both generations exposed to 1.0% D911P. However, ovarian function-assessed by the oestrus cycle and mating behaviour-and epididymidal sperm concentration, motility, and morphology were unaffected by either substance. Treatment resulted in liver changes, particularly in males, characterised by increased liver weight in young animals, histopathologic changes and reduced organ weight in mature animals, and an increase in palmitoyl CoA oxidase activity. In conclusion, neither D79P nor D911P impaired reproductive function in rats when administered in the diet at levels that induce systemic toxicity, and the NOAEL for effects on reproduction in the rat is 0.5% for both D79P and D911P.     

4（R）—（6—氨基—9H—嘌呤—9—基）—2（R）—（羟甲基）四氢呋喃—3（R）—醇的合成

为寻找抗HIV化合物,我们以D－核糖为原料,经甲基化、硅烷基化、还原裂解反应制得重要中间体1－脱氧核糖（5）,再通过形成环状亚砜化合物,与NaN3发生反应后,经过还原、缩合、环合、氨化、脱保护基反应制得异脱氧腺嘌呤核苷（1）,各步反应收率均超过70％。其抗HIV活性测定尚在进行中。     

Psychopharmacological profile of 1-(m-(trifluoromethyl) phenyl) piperazine (TFMPP)

The effect of TFMPP, an agonist of the 5-HT1b receptors, was studied in mice on several psychopharmacological parameters. In contrast to imipramine-like drugs, TFMPP neither antagonized reserpine-induced hypothermia nor increased yohimbine-induced toxicity. Similarly to imipramine-like drugs, TFMPP antagonized oxotremorine-induced hypothermia and was active in the behavioural despair test. In addition, TFMPP normalized a social behavioural deficit induced by isolation. The effects of TFMPP on oxotremorine-induced hypothermia in the behavioural despair test and in the isolation-induced social behavioural deficit are all antagonized by d-1 propranolol. It is concluded that TFMPP seems to possess psychotropic activity resembling only in part that of imipramine-like drugs and that these actions may be mediated through 5-HT1b receptors.