Acceleration of the regeneration of the crushed hypoglossal nerve by testosterone

The effect of testosterone propionate (TP) on regeneration of the crushed hypoglossal nerve was studied in young adult rats. The TP treatment promoted axonal outgrowth as measured by an increase in the proportion of hypoglossal neurons labeled by retrograde transport of horseradish peroxidase injected into the tongue at selected postlesion periods compared with that in controls. The result indicated that TP exerts its effect on regeneration primarily by increasing the metabolic activity in hormone target neurons. The somatotopic organization of the hypoglossal nucleus and its projection into the major nerve branches were unaltered subsequent to crush injury. The maintenance of specificity was attributed to the intact perineurial and endoneurial sheaths which guided regenerating fibers to their original targets.     

Contractile Behaviour of Rat Seminal Vesicle after Gonadectomy, Testosterone Replacement and Cyproterone Treatment

The effects of bilateral gonadectomy, testosterone replacement and cyproterone acetate treatment on seminal vesicle contractions were studied in rats in order to contribute new data on the role of androgens in the spontaneous motility of the seminal vesicle. In gonadectomized-testosterone treated rats the glands exhibited a spontaneous rhythmic activity similar to that of entire animals. The seminal vesicles of gonadectomized as well as of cyproterone treated rats also contracted spontaneously but the contractions showed a smaller amplitude. Such decrease could be related with the well-known atrophy and reduction in the number of smooth muscle cells occurring in seminal vesicles after castration. The results reported in this paper suggest that androgens are not required for the normal spontaneous activity of seminal vesicles.     

Sex difference in the effect of dexamethasone on open-field behavior in rats: Gonadal hormones

Previous experiments indicated that dexamethasone phosphate (DEX) increases open-field defecation in females but not in males. To examine the question of whether this sex difference in response to DEX is due to sex differences in gonadal hormones, female rats were (a) ovariectomized; (b) ovariectomized and injected with testosterone propionate prior to and during open-field testing; or (c) sham operated. Half the females in each group received DEX in their drinking water during the 4 day period of testing. DEX produced the expected reductions in body weight, adrenal weight, and plasma corticosterone levels. Despite the differences between the three groups on a variety of physiological measures, DEX produced comparable increases in open-field defecation in all cases. This indicates that the sex difference in the response of open-field defecation to DEX is not dependent on sex differences in circulating gonadal hormones.     

Validation of a reverse-phase high performance liquid chromatographic method for concurrent assay of a weak base (salmeterol xinafoate) and a pharmacologically active steroid (fluticasone propionate)

The analysis of weakly basic drugs such as salmeterol xinafoate (SX) by reverse-phase liquid chromatography remains a problem, particularly when present in combination with other drugs such as steroids and weak acids. This study describes the validation of an assay for a weakly basic drug, salmeterol (SB), its weakly acidic counter-ion, 1-hydroxy-2-naphthoic acid (XA), and the neutral glucocorticoid, fluticasone propionate (FP) using a second-generation silica stationary phase (Inertsil ODS-2). The assay utilized an Inertsil ODS-2 base-deactivated 250 mm × 4.6 mm, 5 μm HPLC column, with 75:25 methanol:0.6% aqueous ammonium acetate as the mobile phase. Under these near neutral conditions, SB demonstrated a good peak shape (tailing factor = 1.21 ± 0.02, n = 85). The method provided a short analysis time: XA, t_R = 2.96 min; SB, t_R = 5.23 min and FP, t_R = 7.01 min. The assay displayed good sensitivity for both XA (LOD for SX = 0.22 μg mL⁻¹) and SB (LOD for SX = 0.26 μg mL⁻¹). The limit of detection for FP was 0.19 μg mL⁻¹. Neither of the drugs was found to interfere in the determination of the other and the assay accuracy (% recovery) was high (the recoveries were: 99.58 ± 1.85% for XA, 99.49 ± 1.88% for SB and 100.24 ± 1.28% for FP). The assay reproducibility was determined with a mean coefficient of variance for the five calibration concentrations of XA = 0.71 ± 0.18%; SB = 1.11 ± 0.64% and FP = 0.92 ± 0.14%. Analysis of a pressurized metered dose inhaler formulation demonstrated recovery of the analytes that are within pharmacopoeial limits. It was shown that RP-HPLC was suitable for the high throughput analysis of the combination of SX and FP.     

dl—15-甲基前列腺素F_(2α)合并丙酸睾丸酮抗早孕的临床研究新进展(Ⅱ)

本研究在前一阶段工作的基础上,进一步缩短了15-甲PGF_(2α)疗程和减少用药量,并以β-hCG放射免疫测定为主要指标,观察抗早孕效应。停经49天以内的60例早孕妇女随机分为两组,每组30例。组Ⅰ的15-甲PGF_(2α)最高用量为10毫克,组Ⅱ为8毫克;两组用药疗程均为8小时(比以前缩短4小时)。丙酸睾丸酮用法同前。结果两组抗早孕有效率分别为96.67%和100%(p>0.05);15-甲PGF_(2α)平均用量分别为9.67±0.21和7.70±0.19毫克(p<0.05)。组Ⅱ用药比组Ⅰ少2毫克,更适于门诊推广应用。本文并对β-hCG放射免疫测定在药物抗早孕研究中的应用及丙酸睾丸酮的抗早孕机理进行了讨论。     

A STUDY OF THE EFFECTS OF STEROIDS ON α-ADRENOCEPTOR-MEDIATED CONTRACTION OF THE RAT VAS DEFERENS

1. Testosterone propionate (0·5 mg/day) administered for 5 weeks to prepubertal rats increased the weight of sex accessory organs but did not alter the rate of gain of body weight. Methandienone, given in a similar dosage regimen, was without effect on these parameters. The synthetic progestagen, norgestrel, administered orally in a dose of 0·5 mg/day increased the weight of the vas deferens but was without effect on seminal vesicle and testis weights and on the growth rate. Given in combination with testosterone, norgestrel caused a marked decrease in testis weight and reversed the effects of testosterone propionate on seminal vesicle weight. Thus, in the dosage regimen used, this progestagen exhibited an endocrine profile comprising androgenic, synandro-genic and anti-androgenic effects. 2. Rats, which were castrated when they weighed 70–80 g, exhibited rates of gain of body weight which were similar to those of control animals. Testosterone propionate in the doses used reversed castration-induced atrophy of the vas deferens and seminal vesicle. 3. The contractility of the vas deferens of intact rats, determined by direct field electrical stimulation, was unaffected by treatment with the steroids used in this study. However, there was a marked impairment of the contractility of the vas deferens following castration, which was not fully restored by testosterone propionate in the dosage regimen used. 4. The efficacies and potencies of the α-adrenoceptor agonists phenylephrine and 1-metaraminol in causing contraction of the vasa deferentia from intact rats were unaffected by the steroid treatments. In contrast, these agonists did not produce sustained, dose-dependent contractions of the vasa deferentia from castrated rats; however testosterone propionate fully restored the efficacy and potency of both agonists. 5. It is concluded from this study that although adequate testosterone levels are necessary for the maintenance of contractility in the rat vas deferens, the integrity of postjunctional adrenoceptors in not modified by a variety of steroid treatments.     

Retrograde transport of goldfish optic nerve proteins labeled by N-succinimidyl [H]propionate

Following injection of the acylating reagent N-succinimidyl [³H]propionate into the optic nerve of goldfish, labeled protein appeared in the ipsilateral retina and contralateral tectum in a time-dependent manner. Autoradiography indicated the presence of the labeled material in the neuroplasm of the retinal ganglion cells and their projections. While most of the recoverable injected radioactivity was confined to the injection site even after 1 week, labeled proteins arriving in the retina by retrograde flow or in the tectum by anterograde flow had distinctly different patterns, a result suggesting specific transport processes rather than diffusion. In contrast to reported studies with the labeling agent in other species, a prominent 68,000 molecular weight component was not seen. The results are dicussed in relation to the role of retrograde transport in regeneration.     

ABNORMAL FATTY ACIDS IN RAT GLIAL CELLS CULTURED IN VITAMIN B12-DEFICIENT MEDIUM

Rat glial cells cultured in vitamin B¹²-deficient medium contained increased amounts of unbranched fatty acids with 15 and 17 carbon atoms, as well as increased levels of propionate. Addition of vitamin B¹² to the medium caused the levels of the 15-and 17-carbon fatty acids to return to normal. These changes in the fatty acid composition of nerve cells of rats in vitamin B¹² deficiency may be related to the neural lesions in vitamin B¹² deficiency in human beings.     

Effect of Androgens on Antipyrine Metabolism in the Rabbit

The inactivation of endogenous steroids and foreign compounds by the liver hydroxylative pathway, can be modified by androgenic substances. The inhibitory or inductory activity, can be estimated by measuring the half-life of antipyrine. Androgens (testosterone propionate, 5α-dihydro-testosterone and mesterolone) reduce antipyrine metabolism in male rabbits. In females, androgens are not inhibitors, but one of them, 5α-dihydrotestosterone, shows an inductive effect on liver oxidative mechanisms.     

沙美特罗替卡松与噻托溴铵联合吸入在重度、极重度COPD稳定期中的应用

目的观察沙美特罗替卡松与噻托溴铵联合应用对重度、极重度慢性阻塞性肺疾病（COPD）稳定期患者的疗效与预后的影响。方法选取2008年5月至2009年10月于呼吸科门诊就诊的80例稳定期重度极重度COPD患者,采用完全随机法分成两组,一组单用沙美特罗替卡松（SF组）,一组联合应用沙美特罗替卡松和噻托溴铵（联合组）,共治疗12个月。分别于用药后1、3、6和12个月测定患者肺功能（FEV1、FVC、IC）,6分钟步行试验,圣乔治问卷,急性加重次数,急性加重出现时间。结果两组患者治疗后不同时期肺功能指标（FEV1、FVC、IC）、6分钟步行试验及圣乔治问卷评分较治疗前均有明显改善（P〈0.05）,联合组各项指标改善更明显（P〈0.05）。联合组急性加重次数较SF组明显减少（P〈0.05）,且急性加重出现的时间推迟（P〈0.05）。两组间不良反应无显著差异（P〉0.05）。结论沙美特罗替卡松与噻托溴铵联合应用于重度、极重度COPD患者能进一步改善肺功能、运动耐量及生活质量,且不良反应未见明显增加。