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.     

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).     

棒烷肽抗生素G0069A的抗肿瘤作用

体外用MTT法和动物移植性肿瘤模型研究棒烷肽抗生素G0069A的抗肿瘤活性。结果表明,G0069A对多药抗药性肿瘤细胞显示高度的杀伤活性,与阿霉素、长春新碱无交叉抗药性。G0069A经iv或ip给药对小鼠肉瘤180和肝癌22有显著疗效;用小鼠可耐受剂量,对肉瘤180和肝癌22的抑制率分别达87%和74%。提示G0069A是天然来源的具有明显抗肿瘤作用的棒烷肽。     

抗心肌缺血药3-{4-[(2-羟基-3-烷氨基)丙氧基]苯基(苄基)}-取代4(3H)-喹唑酮的合成

β-受体阻断药在心血管病的治疗中占有相当重要的地位,对缺血性心脏病有肯定的疗效。但也存有不良反应或禁忌症,其中有的是由于其选择性不高所致。因此,寻找特异性的β_1受体阻断药是目前研究抗心肌缺血药的一个重要方面。据报道,在β-受体阻断药的基本有效结构的苯环的对位与4(3H)-喹唑酮环的2位     

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.