Induction of lymphomas by urethane in combination with diethylstilboestrol in CFLP mice

Summary The combination of urethane and the non-steroidal oestrogen diethylstilboestrol induced lymphomas in CFLP mice.This work was supported by grants from the Ministry of Health of Hungary (Grants No. 2-10-0401-01-2/K, 2-11-0801-01-1/VR, 2-09-0801-01-1/E).     

3[H]-Sulpiride labels mesolimbic non-dopaminergic sites that bind antidepressant drugs

3[H]-(-)-Sulpiride and 3[H]-spiperone binding was compared in rat amygdala, nucleus accumbens and striatum, using (+/-)-sulpiride to define specific binding. 3[H]-(-)-Sulpiride bound to twice as many sites in amygdala and nucleus accumbens as 3[H]-spiperone. 3[H]-(-)-Sulpiride binding was directed to these additional sites by using 1 microM spiperone to mask dopaminergic binding. The binding of 3[H]-(-)-sulpiride to these sites was high affinity, reversible, Na+-dependent, but not stereospecific. Metoclopramide, tiapride and antidepressant medications, but not other neuroleptics, ADTN, or serotonin displaced 3[H]-(-)-sulpiride binding to these sites. These data suggest that 3[H]-(-)-sulpiride labels mesolimbic sites other than dopamine receptors which may mediate antidepressant effects.     

Pharmacological studies of a new analgesic, dl-erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride, in experimental animals.

dl-Erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride showed orally a definite analgesic activity, without producing the significant morphine-like physical dependence liability, and its analgesic potency was about a half that of codeine and far superior to aminopyrine in experimental animals.     

Pharmacological studies of a new analgesic,dl-erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride,in experimental animals

Summary dl-Erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride showed orally a definite analgesic activity, without producing the significant morphine-like physical dependence liability, and its analgesic potency was about a half that of codeine and far superior to aminopyrine in experimental animals.     

Suan Shu Shu A Book on Numbers and Computations

In December and January of 1983–1984, archaeologists excavating the tomb of an ancient Chinese provincial bureaucrat at a Western Han Dynasty site near Zhangjiashan, in Jiangling county, Hubei Province, discovered a number of books on bamboo strips, including inter alia works on legal statutes, military practice, and medicine. Among these was a previously unknown mathematical work on some 200 bamboo strips, the Suan shu shu, or Book of Numbers and Computations. Based upon other works found in the tomb, especially a copy of the Er nian lü ling (Laws and Decrees of the Second Year (of the reign of empress Lü, i.e. Lü Hou)), archaeologists have dated the tomb to ca. 186 BCE (Lü Hou’s regency lasted from 188 to 180 BCE). The Suan shu shu, as the earliest yet discovered work devoted specifically to mathematics from ancient China, has stirred considerable interest among Chinese historians of science. The translation and commentary offered here draw extensively on the works cited in Sect. 3 below. Several appendixes devoted to specific issues related to translating the Suan shu shu, including its title and the problem of determining English equivalents for various commodities that arise in the text, may be found in Appendix II. An erratum to this article can be found at     

Fatty acid modulation of antiestrogen action and antiestrogen-binding protein in cultured lymphoid cells

Nonsteroidal antiestrogens reversibly and specifically inhibited the proliferation of two estrogen receptor-negative lymphoid cell lines (EL4 and Raji) in a dose-dependent manner. [3H]Thymidine incorporation of concanavalin A-stimulated primary splenocytes was also inhibited by 10(-6) M clomiphene (1-[4-(2-diethylaminoethoxy)phenyl]-1,2-diphenyl-2-chloroethylene). The antiproliferative effect could be prevented by the simultaneous presence in the growth medium of 10(-5) M linoleic acid or 10(-5) M arachidonic acid but not by 10(-6) M estradiol. Both lymphoid cell lines had high affinity antiestrogen-binding sites whose affinity could be altered by conditions of growth. Growth of EL4 cells in RPMI 1640 medium supplemented with charcoal-pretreated 5% fetal calf serum (charcoal-stripped medium) resulted in significantly higher affinity (Kd 0.54 nM +/- 0.11 nM; n = 6) than growth in medium supplemented with untreated serum (complete medium) (Kd = 1.68 nM +/- 0.48 nM; n = 6) (p less than 0.001). This change in affinity was partly due to removal of fatty acids from the growth medium by charcoal pretreatment, since addition of 10(-5) M linoleic acid or 10(-5) M gamma-linolenic to charcoal-stripped medium decreased the affinity of the antiestrogen-binding protein. In contrast, growth in 10(-5) M stearic acid or 10(-5) M oleic acid did not significantly alter the affinity of the antiestrogen-binding protein, whereas 10(-5) M palmitic acid significantly increased its affinity. The same fatty acids were also tested for their intrinsic effects on EL4 cell proliferation. Oleic, linoleic and gamma-linolenic acids were growth stimulatory while stearic and palmitic acids were not. Thus linoleic and gamma-linolenic acids whose presence in the growth medium was associated with decreased affinity of [3H]tamoxifen (1-[4-(2-dimethylaminoethoxy)phenyl]-1,2-diphenylbut-1(Z)-ene) binding to the intracellular antiestrogen-binding protein were also growth stimulatory. Unsaturated fatty acids have previously been shown to inhibit binding of [3H]tamoxifen to the antiestrogen-binding protein in a cell-free system. The present observations demonstrate that unsaturated fatty acids also modify the affinity of the antiestrogen-binding protein in intact cells.     

Phosphoramidon enhances allatostatin-mediated inhibition of juvenile hormone biosynthesis in the corpora allata of the cockroach, Diploptera punctata.

Use of enkephalinase inhibitor phosphoramidon in the in vitro radiochemical assay for juvenile hormone biosynthesis enhanced allatostatin-mediated inhibition of hormone production by corpora allata of the cockroach, Diploptera punctata. Significant increases in inhibition in day 2 virgin female CA by AST 1 (at 10(-7) M) and AST 4 (10(-8)-10(-7) M) were observed in the presence of phosphoramidon (10(-5) M or greater). No significant increase in inhibition were seen in CA from day 6 mated females with AST 4 (10(-9)-10(-7) M) and phosphoramidon combined. Phosphoramidon alone had no effect on JH biosynthesis. Analysis of allatostatin content of the CA, as determined by ELISA, revealed that addition of phosphoramidon to the medium increased the endogenous allatostatin content in CA of virgin and mated females. The similarity in primary structure between allatostatins and enkephalin-like peptides and their similar distribution makes it probable that phosphoramidon acts by preventing breakdown of allatostatins within the CA.     

Enantiomeric cannabinoids: stereospecificity of psychotropic activity

The 1,1-dimethylheptyl homolog of (-)-(3R,4R)-7-hydroxy-delta-6- tetrahydrocannabinol (compound II) is highly psychotropic in mice, rats and pigeons. The (+)-(3S,4S) enantiomer (III) was found to be psychotropically inactive at doses up to several thousand times those of the ED50 of (II).     

Reduction of efferent renal nerve activity by propranolol in rabbits]

During intravenous infusion of propranolol (0.3--0.8 mg/kg) in the Rabbit, systolic arterial pressure is decreased (-6.5 +/- 4.2 mmHg) and electrical activity recorded from central end of the renal nerve is reduced significantly (-8.7 +/- 14.-%) with regard to the activity obtained, at the same pressure levels, by hemorrhage (+7.9 +/- 6.4%; p less than 0.25) or by intravenous infusion of the peripheral vasodilator sodium nitroprusside (+14.1 +/- 9.9%; p less than 0.01).     

Two novel prolactin release-inhibiting 8α-amino-ergolines

Summary Prolactin secretion inhibition and changes in striatal dopamine metabolism in rats were compared after the administration of 8a-amino-ergoline CH 29-717 and 2 derivates. CQ 32-084 was similar to but less potent than CH 29-717. while 32-085, the 1-methyl derivative, showed delayed dopaminomimetic effects.     

Potentiative effects of sulfhydryl compounds on carrageenin-induced oedema in rats and relationship to their potencies as inhibitors of angiostin-coverting enzyme in vivo.

Carrageenin-induced oedema in rats was potentiated by oral administration of (4R)-3-[(2S)-3-mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (SA291) and related sulfhydryl compounds, and the effect was closely correlated with their potencies as inhibitors of angiotensin-converting enzyme in vivo.     

Time and theophylline influence on the quantitative variations of the glomerular basement membrane ferritin pathway (author's transl)

A fine quantitative evaluation of ferritin aggregates in rat GBM permits to counts 5.08 +/- 1.51 and 18.30 +/- 3.21 g/cm2, respectively 30 and 60 min after ferritin injection; likewise, 30 min after ferritin administration, 5.08 +/- 1.51 and 17.11 +/- 3.9 g/cm2, respectively in normal and theophylline-treated animals.     

Protracted analgesia in young and adult rats maternally exposed to methadone

Summary The analgesic response to the hot-plate test was studied in 21-, 45-, 60-, 120- and 300-day-old rats maternally exposed to methadone (5 mg/kg). An elevation in nociceptive threshold, in the absence of further exposure to methadone, was observed in young and adult rats perinatally subjected to methadone.This research was supported by grant DA 01618.     

Aneuploidy of glandular epithelial cells in histologically normal prostate glands

The percentage of aneuploidy in normal prostate glands from subjects 13-38 years old and 45-66 years old ranged from 0-78% and 0-63%, respectively. In contrast to adults, aneuploidy was absent in fetal and postnatal prostates. It is concluded that aneuploidy is a fundamental attribute of histologically normal adult prostate glands.     

Effect of unilateral ureteral obstruction on renal polyamine levels in rats

Summary Unilateral ureteral obstruction in rats, resulted in considerable alterations of polyamine levels in the obstructed kidney during a 72-h observation period, as compared with respective values for the contralateral control kidney.This work was supported in part by the Ministry of Health, Hungary (1-04-0301-03-02/H). The skilful technical assistance of Ms G. Mayer and Mrs I. Harmos is highly appreciated.     

第一性原理研究高压下单轴压缩硝基甲烷的结构性质

运用第一性原理方法,计算研究了在0～40GPa压强范围内硝基甲烷键长的变化研究和固态硝基甲烷结构性席随属强的变化。研究发现,在低于20GPa时所有的键变化都比较小,在2～30GPa时被压缩,在30-40GPa时又被拉伸。在40GPa高压下,几乎所有的键都处于拉伸状态,只剩下部分N-O键被压缩。此外,C—H键在压强下的拉伸与甲基的转动和原予闯电荷的转移有关。在30GPa时H原子的电荷转移到C和N原予,而甲基的转动使得分子间的距离变小。逮使得C—H键较弱而容易拉伸。     

Degenerative atrophy of central terminals of primary sensory neurons induced by blockade of axoplasmic transport in peripheral nerves

Summary Perineural colchicine- or vinblastine-treatment results in disappearance of non-lysosomal acid phosphatase activity, characterizing axon terminals in the Rolando substance of the normal spinal cord. Ultrastructural alterations are identical with those seen in the course of degenerative atrophy.Supported by research grant No. 4-01-0303-01-1 from the Hungarian Ministry of Health.     

(S)-(+)-4,4,4-Trifluoro-3-(indole-3-)butyric acid,a novel fluorinated plant growth regulator

Racemic 4,4,4-trifluoro-3-(indole-3-)butyric acid (TFIBA) has been synthesized and shown to inhibitAvena coleoptile elongation. (S)-(+)-TFIBA (fig. 1), which was prepared by an enzymatic method and markedly promotes root growth of Chinese cabbage, lettuce and rice plants, is a novel fluorinated plant growth regulator. Activity of the (S)-(+)-enantiomer of TFIBA was 10-fold greater than that of the (R)-(–)-enantiomer in the first two plant species and 5-fold greater in rice.     

Potentiative effects of sulfhydryl compounds on carrageenin-induced oedema in rats and relationship to their potencies as inhibitors of angiostin-converting enzyme in vivo

Summary Carrageenin-induced oedema in rats was potentiated by oral administration of (4R)-3-[(2S)-3-mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (SA291) and related sulfhydryl compounds, and the effect was closely correlated with their potencies as inhibitors of angiotensin-converting enzyme in vivo.Acknowledgment. The authors wish to thank Prof. H. Fujimura, Department of Pharmacology, Gifu University School of Medicine, for his helpful advice.     

Anticonvulsant action of YG 19-256 in baboons with photosensitive epilepsy.

YG 19-256, 4-(1,3,4,9b-tetrahydro-5 methyl-2H-indeno[1,2-c]pyridine-2-yl)-2-butanone methane sulphonate, 1-3 mg/kg i.v., abolished or reduced photically-induced myoclonic responses for 1.5-6.5 h in baboons, Papio papio, without producing signs of acute neurological toxicity.