Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists

The resolution of three 2-substituted derivatives of idazoxan is described. The enantiomers show large separations in activity in a variety of in vitro and in vivo tests, and the active isomers are all potent and selective antagonists at the alpha 2-adrenoreceptor. The significance of these results in relation to those published on the enantiomers of idazoxan and to those on optically active alpha 2-adrenoreceptor agonists is discussed.     

Dose Escalated External Beam Radiotherapy versus Neoadjuvant Androgen Deprivation Therapy and Conventional Dose External Beam Radiotherapy for Clinically Localized Prostate Cancer: Do we Need Both?

Strahlentherapie und Onkologie - Several randomized trials have demonstrated that men with localized prostate cancer benefit from the use of short-term neoadjuvant androgen deprivation therapy...     

青蒿琥酯皮肤擦剂在小鼠和兔体内的药代动力学研究

将青蒿琥酯溶于苯二甲酸二甲酯,加适量氨酮制成皮肤擦剂。给兔脱毛后,皮肤涂抹此擦剂25mg/kg后,血药浓度达峰时间平均为2 h,峰浓度平均为1.80μg/ml。药物在兔体内平均驻留时间为3.54 h,清除半衰期约为2.46 h。给小鼠脱毛皮肤涂抹擦剂6.7,31.3和71.4 mg/kg,血药浓度在给药后0.5～4 h达高峰,峰浓度分别为0.82,2.05和7.11μg/ml,体内药物平均驻留时间为3.39,2.79及3.54 h,清除半衰期为2.35,1.93及2.45 h。可见,给兔及小鼠皮肤擦剂后,青蒿琥酯吸收良好,血药浓度维持时间较长。     

Modulation of the hypolipidemic effect of fish oils by dietary fiber in rats: studies with rice and wheat bran

Adult male rats were fed a purified diet containing rice bran or wheat bran with or without a marine fish oil to investigate the possible effects of such dietary combinations on lipid metabolism. Plasma and hepatic triacylglycerols and hepatic lipogenesis were lowered significantly by feeding fish oil with rice bran but not with wheat bran. Plasma cholesterol and hepatic cholesterol synthesis were significantly lower in animals fed fish oil with either bran. Liver microsomal free cholesterol was significantly lower in rats fed rice bran alone than in all other groups. Hepatic low density lipoprotein (LDL) receptor activity was significantly higher in the two groups fed rice bran than in the two groups fed wheat bran. Fish oil significantly decreased hepatic LDL receptor activity and increased hepatic high density lipoprotein (HDL) binding activity with wheat bran but had no significant effects on these parameters when added to the rice bran diet. However, when the data for all groups were pooled, there was a significant negative correlation between hepatic HDL binding activity and LDL receptor activity. Cecal volatile fatty acids were significantly higher in rats fed rice bran, were unaffected by adding fish oil to either bran diet and did not appear to mediate any of the effects of the brans and fish oil on plasma lipids and hepatic lipid metabolism. The combination of rice bran plus fish oil therefore appears to have more beneficial effects on lipid metabolism than wheat bran plus fish oil.     

Infratentorial stereotactic biopsy. A review of 11 cases.

A review of the stereotactic cases performed at the University of Iowa between February, 1985, and December, 1990, yielded 12 infratentorial stereotactic biopsies in 11 patients. A definitive diagnosis was obtained in 9 of 11 patients. One patient required a second biopsy to obtain a diagnosis and 1 yielded cystic fluid only. The pathological diagnosis obtained included 4 high-grade gliomas, 2 undifferentiated adenocarcinomas, 2 low-grade astrocytomas, 1 malignant ependymoma, 1 pontine hematoma and 1 cyst. None of the patients experienced increased neurological deficit following biopsy and there was no mortality. One patient developed postoperative meningitis. We conclude that stereotactic biopsy of infratentorial lesions can be performed safely with a high probability of obtaining a diagnosis. Adequate tissue diagnosis is necessary to direct further therapy.