一种新的阿片受点不可逆激动剂7α-二(β-氯乙基)胺甲基-6,14-乙烯撑基四氢奥利文的药理研究

α-CAM是一新的阿片受点不可逆激动剂,在离体组织(GPI,MVD,RVD和RbVD)及大鼠脑P_2膜制备上均表现不可逆作用。对小鼠镇痛(icv)ED_(50)为0.12 nmol/鼠,镇痛作用可持续2～3 d,是迄今所知镇痛时间最长的化合物。一次注射(icv)即可使小鼠成瘾,可作为研究成瘾机理的工具药。     

一种新的阿片受点不可逆激动剂7α-二(β-氯乙基)胺甲基-6,14-乙烯撑基四氢奥利文的药理研究

α-CAM是一新的阿片受点不可逆激动剂,在离体组织(GPI,MVD,RVD和RbVD)及大鼠脑P₂膜制备上均表现不可逆作用。对小鼠镇痛(icv)ED₅₀为0.12 nmol/鼠,镇痛作用可持续2～3 d,是迄今所知镇痛时间最长的化合物。一次注射(icv)即可使小鼠成瘾,可作为研究成瘾机理的工具药。     

缩氨基硫脲及其过渡金属络合物的合成与抗菌活性

本文设计合成了8种缩氨基硫脲化合物及其12种过渡金属络合物,并进行了抑菌实验。结果表明:芳醛(酮)的邻位存在杂原子或取代基团为其缩氨基硫脲活性表现必不可少的结构因素。络合物的抑菌活性一般较缩氨基硫脲本身高,二者遵循不同的抑菌机制。     

Vagina: evaluation with MR imaging. Part I. Normal anatomy and congenital anomalies

The appearance of the vagina was evaluated on magnetic resonance (MR) images of 65 subjects who were healthy or had disease unrelated to the vagina and 24 patients with suspected congenital anomalies of the vagina. MR imaging accurately demonstrated the presence of (n = 78) or complete (n = 7) or partial (n = 4) absence of the vagina in each case. Partial (n = 2) or complete (n = 2) duplication of the vagina was also correctly diagnosed. Regardless of field strength, T2-predominant images were essential for evaluation. The transverse plane was optimal, and a 5-mm section thickness was preferable. Estrogen stimulation affected the appearance of the vagina: The contrast between the vaginal wall and the central mucus-containing area was greatest during the early proliferative and late secretory phases. MR imaging offers unique depiction of congenital anomalies and should be used when results of physical examination or other radiologic studies, such as ultrasound, are inconclusive.     

1-乙基-6-氟-1,4-二氢-4-氧-7-(4-对硝基苯甲酰基-1-哌嗪基)喹啉-3-羧酸及其类似物的合成

Syntheses of thirteen new compounds of 1-ethyl-6-flouro-1, 4-dihydro-4-oxo-7-[(4-p-nitrobenzoyl)1-piperazinyl] quinoline-3-carboxylic acid and its analogues are reported. The structures were determined by IR, 1HNMR and elemental analysis. Four compounds have been subjected to antibacterial activity tests in vitro. Compound I1 was shown to have significant activity.     

硫酸镁治疗妊娠高血压综合征的群体药动学—药效学

用 NONMEM 程序分析硫酸镁治疗妊娠高血压综合征患者的群体药动学-药效学,以快—慢速率相继静脉输注二室开放模型拟合60例患者的群体药动学参数,以效应室与中央室连接的三室模型,用参数法拟合26例患者的Sigmoid E_max药效学模型的群体参数。采用分光光度法测定血镁浓度(以给药前的基础值作调整),选择舒张压降低的百分率为药效指标。硫酸镁的群体药动学参数为:群体典型值K₁₀(h^-1),K₁₂(h^-1),K₂₁(h^-1)和Vc(L)分别等于1.62,20.8,2.70,27.0,其个体间变异σ_K10(%),σ_K12(%),σ_K21(%),σ_Vc(%)分别等于25.70,14.13,24.33,34.04,浓度的残差变异σ_E(%)等于15.03。硫酸镁的群体药效学参数为:群体典型值E_max(%),C_e(50)(μg·ml^-1),υ,K_eo(h^-1)分别等于28.73,28.39,4.22,0.43。其个体间变异σ_Emax(%),σ_Ce(50)(%),σ_υ(%),σ_Keo(%)分别等于56.32,62.24,33.47,42.76。效应的残差变异σ'_E(%)等于28.54。     

Vagina: evaluation with MR imaging. Part II. Neoplasms

The potential of magnetic resonance (MR) imaging in the detection of vaginal tumors and the assessment of their extent was evaluated retrospectively in 87 patients in whom primary, metastatic, or recurrent vaginal cancer was clinically suspected. MR findings were compared with the results of surgery and/or biopsy. Results of histopathologic study verified a normal vagina in 51 patients, benign cysts in two, primary tumor in four, metastatic cancer in 22, and recurrent tumor in eight. MR imaging demonstrated the two benign cysts, correctly depicting their size and location, and demonstrated and enabled correct staging of the four primary tumors. MR accuracy for demonstrating metastatic cancer was 92%, sensitivity was 95%, and specificity was 90%. Tumor extension to the vagina was reliably excluded (negative predictive value = 97%), but false-positive interpretations occurred (positive predictive value = 84%) primarily because inflammation (n = 2) and congestion (n = 2) could not be distinguished from tumor invasion. An additional role of MR imaging was the ability to differentiate tumor from fibrotic tissue in patients with suspected recurrent vaginal carcinoma. The overall accuracy of MR imaging for recurrent vaginal cancer was 82% (14 of 17).     

1-乙基-6-氟-1,4-二氢-4-氧-7-(4-对硝基苯甲酰基-1-哌嗪基)喹啉-3-羧酸及其类似物的合成

氟哌酸(norfloxacin)是吡酮酸类药物的优秀代表之一,其特点是抗菌谱广,抗菌作用强,该药对绿脓杆菌的作用较庆大霉素强,并远优于萘啶酸和吡哌酸,但美中不足的是易于代谢和体内生物利用度及血浓度较低,从而影响了实际效果。为了改善疗效,根据药物在体内作用和代谢以及口服给药的特点,设计合成了系列氟哌酸的新类似物,以期通过改造化合物结构来改变化合物的理化性质,体内代谢途径,获得血浓度和活性高、毒副作用小,疗效更好的抗菌药物。合成路线如下:     

Subsequent reproduction and obstetric outcome after methotrexate treatment of cervical pregnancy: a review of original literature and international collaborative follow-up

The case reports of 22 patients with cervical pregnancies treated by methotrexate (MTX) administration and published in English literature between 1983 and 1995 were reviewed, by either original paper review or follow-up under international collaboration, to determine the subsequent reproductive performance and obstetric outcomes. Out of 22 cases, 18 (78%) MTX chemotherapy attempts succeeded with complete remission and four (22%) failed. Of the 13 women who wished to conceive and could be followed for at least 3 years, nine succeeded in having live births without congenital malformations, one spontaneously aborted and three suffered infertility. In general, MTX chemotherapy alone or combined with adjuvant methods such as subsequent cervical curettage or cervical tamponade, or intracervical potassium chloride injection, appears to be a convenient and effective method for the treatment of the majority of cervical pregnancies before 12 weeks gestation, and has not been shown to have detrimental effects on subsequent reproductive capacities, obstetric outcomes and progeny health for those cases with successful preservation of the uteri.