共查询到19条相似文献,搜索用时 468 毫秒
1.
2.
3.
4.
5.
从天然植物制取(一)棉酚 总被引:1,自引:0,他引:1
本文首次报道从天然植物——海岛棉籽中分离出(-)棉酚。同时发现了受试的各种棉籽所含棉酚的光学活性的规律。(1)棉籽中棉酚的两个对映体(-)棉酚和(+)棉酚一般是不等量的,故其成分应为(±)棉酚和过量的(-)棉酚或(+)棉酚;(2)同种属棉籽含有相同旋光性的过量对映体,如海岛棉籽均含有过量的(-)棉酚,多数品种所含棉酚的光学纯度为10~25%,陆地棉籽则均含有过量的(+)棉酚,其相应棉酚的光学纯度为10~20%。 相似文献
6.
7.
8.
9.
10.
11.
Racemic, (-) and (+) gossypol, provided by the Department of Organic Chemistry of our institute, was suspended in 2.5% tween 80 solution. Adult male Wistar rats 190~220 g in weight were allotted to 5 groups. Animals in group 1 received 2.5% tween 80 solution as control. Rats in group 2 were treated with racemic gossypol at the dosage of 30 mg/kg for 2 weeks. Animals in group 3 and 4 were given 15 mg/kg of (-) gossypol for 2 weeks and 30 mg/kg of (-) gossypol for 1 week respectively. Rats in group 5 were treated with (+) gossypol at the dosage of 30 mg/kg for 2 weeks.Four weeks from the beginning of gossypol treatment the rats were cohabited with adult females for 7 days. Then the motility of the sperms in the cauda epididymides was estimated The female rats were examined for pregnancy 7 days later.Treatment with (-) gossypol at 30 mg/kg caused significant decreases in body weight of the rats (P<0.05). One of the five rats died 7 days after the last administration, while (+) gossypol and racemic gossypol at the dosage employed had no effect on the body weight. (+) Gossypol at 30 mg/kg for 2 weeks had no effect on the motility of the sperms in the cauda epididymides and no effect on the fertility of the animals: nor was there any effect on the weights of the testis, epididymis, prostate and seminal vesicle. The sperms of the cauda epididymides were found to be dead in the groups treated with 15 and 30 mg/kg of (-)gossypol. Raccmic gossypol given for 2 weeks at 30 mg/kg caused loss of fertility of the male rats which confirmed our previous findings.(?)t may be postulated that (+) gossypol has no antifertility effect nor toxicity at the dosage employed. (-) Gossypol is the active stereoisomer of racemic gossypol. 相似文献
12.
以L-苹果酸(2)为原料,经与苄胺缩合、还原、氢解脱苄、磺酰化、烷基化、脱保护基、水解后成盐制得氢溴酸达非那新关键中间体3-(S)-(-)-(1-氨甲酰基-1,1-二苯甲基)吡咯烷酒石酸盐,总收率约22%(以2计). 相似文献
13.
Besides 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL), [4-(methylnitrosamino)-1-(3-pyridyl)but-1-yl]-β-O-d-glucosiduronic acid (NNAL-Glu) is another important metabolite of the tobacco-specific nitrosamine 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone
(NNK) which has been detected in the urine of tobacco users and non-smokers heavily exposed to sidestream cigarette smoke.
In order to evaluate the toxicological significance of NNAL-Glu formation and excretion, the metabolism of [5-3H]-NNAL-Glu was studied in rats. Five male F344 rats were administered 3.7 mg/kg [5-3H]-NNAL-Glu by i.v. injection and the metabolites in urine analysed by HPLC. More than 90% of the radioactivity was excreted
in urine within the first 24 h. Unchanged NNAL-Glu accounted for 81.2±3.1% of the total radioactivity; the remaining part
of the dose appears to be deconjugated resulting in the urinary excretion of NNAL (3.6±1.7%) and its α-hydroxylation (11.5±2.2%)
and N-oxidation (3.6±1.6%) products. The presence of α-hydroxylation products of NNAL-Glu in urine suggests that this NNK metabolite
may be activated in vivo to carcinogenic intermediates.
Received: 25 April 1994 / Accepted: 29 June 1994 相似文献
14.
Functional effects of the σ ligand, (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP), were explored in perfused rat tail and rabbit ear arteries in vitro. In the rat tail artery (+)-3PPP inhibited contractile responses to adrenergic nerve stimulation, an effect which was reversed to potentiation by the dopamine D2 receptor antagonist sulpiride. In the rabbit ear artery, however, (+)-3PPP potentiated contractile responses to nerve stimulation, an effect which was unchanged by sulpiride. In the rat tail artery, blockade of norepinephrine uptake by cocaine and deoxycorticosterone in the presence of sulpiride revealed two additional actions of (+)-3PPP. First, an inhibitory action on the monoamine uptake site was confirmed by direct measurement of [3H]norepmephrine accumulation. Second, at higher concentrations, an action to inhibit contractile responses to adrenergic nerve stimulation was manifested at a still unidentified site. These studies demonstrate that the observed functional effect of (+)-3PPP results from its combined actions on three individual sites with the net effect dependent on the relative densities of these different receptor sites in each type of vessel. 相似文献
15.
目的 研究DDPH对α1-肾上腺素受体(α1-AR)及其亚型的拮抗作用。方法 放射配体结合实验和离体血管收缩功能实验。结果 DDPH对125I-BE2254与大鼠脑皮质和脾脏α1-AR结合呈竞争性拮抗作用。pKI值在两者间无显著性差别, Hill系数均接近于1.0。在分别稳定表达α1A,α1B或α1D-AR的克隆HEK293细胞中,其拮抗的pKI值α1A和α1D比α1B-AR高约2倍,Hill系数均接近于1.0。并拮抗去甲肾上腺素(NE)介导大鼠主动脉,肾动脉和脾脏收缩的pA2值,在三者间无显著差别,斜率接近1.0。结论 DDPH对α1-AR有竞争性拮抗作用,但其作用对α1-AR亚型无选择性。 相似文献
16.
目的合成1-(2,4-二氯苯基)-2-(1-咪唑基)乙醇.方法以2,4-二氯苯甲醛为原料,在碱性条件下与锍内鎓盐反应得到的1-(2,4-二氯苯基)环氧乙烷与咪唑反应得到抗真茵药物咪康唑中间体1-(2,4-二氯苯基)-2-(1-咪唑基)乙醇.结果此工艺具有反应条件温和、易控,原料便宜易得等优点,总收率54%,产品纯度≥99.0%.结论该合成工艺可行,具有工业生产价值. 相似文献
17.
Christian Thomsen Per Olaf S?rensen Jan Egebjerg 《British journal of pharmacology》1997,120(6):983-985
The selectivity of new derivatives of the γ-aminobutyric acid (GABA)-uptake inhibitor, tiagabine was characterized at the four cloned mouse GABA transporters (mGAT1 through mGAT4) by measuring [3H]-GABA uptake into stably transfected baby hamster kidney cells. While tiagabine is a highly selective inhibitor of mGAT1 (Ki=0.11±0.02 μM), these derivatives exhibited low potencies at mGAT1 but differential activities at mGAT2, mGAT3 and mGAT4. In particular, 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol (NNC 05-2090) was a potent inhibitor of mGAT2 (Ki=1.4±0.3 μM) showing at least 10 fold selectivity over mGAT1, mGAT3 and mGAT4. NNC 05-2090 is the first subtype selective inhibitor of mGAT2 and may represent a novel useful tool for investigating the physiological roles of GAT2 in the brain and periphery. 相似文献
18.
采用液相色谱-串联质谱法对大鼠灌胃1-[1-(6-甲氧基-2-萘基)乙基]-2-(4-硝基苄基)-6,7-二甲氧基-1,2,3,4-四氢异喹啉氢溴酸盐(编号P91024)后粪便、尿液、胆汁和血浆中的主要代谢产物进行研究。通过比较给药样品和空白样品的全扫描总离子流色谱和选择离子扫描色谱图差别寻找I相代谢产物;根据其一级和二级质谱图,确定I相代谢产物的分子结构。完全提取I相代谢产物后的样品溶液,再用葡糖醛酸酶酶解,得II相结合物的苷元部分,采用与I相代谢产物鉴定同样方法寻找和鉴定II相代谢产物苷元的结构,进而确证II相代谢产物的分子结构。从大鼠粪便中鉴定出P91024的2个I相代谢物,从胆汁中鉴定出1个I相和5个II相代谢产物,从尿液中鉴定出1个I相和3个II相代谢产物,从血浆中鉴定出4个I相和1个II相代谢产物;并分别分析推测出它们的结构。P91024在大鼠体内被代谢转化为多种产物,利用LC-MS/MS可以快速寻找和鉴定。 相似文献
19.
地拉韦定(delavirdine)是由美国Pharmacia&Upjohn公司研制的非核苷HIV-1逆转录酶抑制剂(NNRTIs),临床与其它抗HIV药联合使用,用于治疗获得性免疫缺陷综合征[1].1-(5-硝基吲哚-2-羰基)-4-[3-(1-甲基乙胺基)-2-吡啶基]哌嗪(1)是其重要中间体.文献[2-4]以5-硝基吲哚-2-羧酸(2)和1-[3-(1-甲基乙胺基)-2-吡啶基]哌嗪(3)为原料,在1-(3-二甲胺基丙基)-3-乙基碳二亚胺(EDC)作用下缩合制得.EDC价昂,后处理用氯仿作提取溶剂,且需通过柱色谱纯化,不适于规模化生产. 相似文献