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1.
薄荷醇对戊巴比妥中枢抑制作用的影响   总被引:1,自引:0,他引:1  
研究薄荷醇经胃肠道给药对成巴比妥中枢抑制作用的影响,结果发现,薄荷醇对戊巴比妥的中枢抑制作用具有一定的量效关系,含4.5%的薄荷醇溶液可明显使小鼠的入睡时间缩恒,并使急性死亡率增加,而含1.5%和0.5%的薄荷醇溶液对成巴比妥的中枢抑制作用无明显影响。  相似文献   
2.
It is well established that the circadian clock of the suprachiasmatic nuclei (SCN) is entrained by light. More recently, the potent effects of arousing, non-photic cues on the clock have been recognized. The neural mediators of non-photic entrainment are yet to be identified. To examine the contribution of the thalamic intergeniculate leaflet (IGL) and its NPY-immunopositive projection, the geniculo-hypothalamic tract to non-photic entrainment by arousal, male Syrian hamsters received lesions of the IGL (IGLX) which ablated NPY-immunoreactivity in the SCN. Their circadian responses to both photic and non-photic cues were then tested. Lesions resulted in a delay in the timing of activity onset following lights out, but had no effect on the behavioural or cellular circadian responses to phase-advancing light pulses presented at circadian time (CT) CT19 (where CT12 represents the time of activity onset). Injection with a benzodiazepine (chlordiazepoxide, 100 mg/kg) at CT6 suppressed wheel-running, increased general locomotion of intact controls and induced large phase advances of the circadian rhythm of wheel-running. Chlordiazepoxide also inhibited wheel-running in lesioned animals, but there was no significant increase in general locomotion and the lesioned animals did not phase advance. Serial arousal by injection of saline at intervals of 23.5 h for 6 days entrained the circadian rhythm of wheel-running of intact hamsters and was associated with an increase in general locomotor activity. Entrainment by serial arousal was abolished by IGLX. However, the lesioned animals did show a clear behavioural response to every presentation of the non-photic cue. These results show that the IGL is a necessary component of the neural pathways mediating both arousal- and benzodiazepine-induced non-photic entrainment.  相似文献   
3.
短效催眠药唑吡坦和三唑仑对人体前庭功能的影响   总被引:3,自引:1,他引:2  
目的 :探讨两种短效催眠药唑吡坦和三唑仑对人体前庭功能的影响 ,为在应急条件下对飞行员服用该药提供试验依据。方法 :8名受试者 ,采用三阶段交叉双盲给药设计方法 ,分别交叉服用三唑仑 (0 .2 5mg)、唑吡坦 (10mg)、安慰剂 ,每次间隔 1周 ,在服药前 1h及服药后1、2、3、4、6、8、10h分别进行一组前庭功能测试 ,包括视动性眼震 (OKN)、前庭眼动反射 (VOR)、前庭眼动反射固视抑制 (VOR -Fix)、视前庭眼动反射 (VVOR)。结果 :与安慰剂组比较 ,服用唑吡坦和三唑仑后均能显著降低VOR、OKN、SPT增益 ,在服药 2h后降到最低〔VOR :(0 .5 1± 0 .0 4 ) ,(0 .5 2± 0 .0 5 )vs (0 .6 7± 0 .13) ;OKN :(0 .32± 0 .0 2 ) ,(0 .6 2± 0 .0 6 )vs (0 .82± 0 .0 7) ;SPT :(0 .71± 0 .14 ) ,(0 .6 6± 0 .0 6 )vs (0 .93± 0 .0 3)〕。其中唑吡坦对OKN增益的降低要强于三唑仑 ,但这种影响持续时间不长 ,在服药 6h后即消失。两种短效催眠药对VVOR增益、SPT相位及VOR -Fix均无明显影响。结论 :唑吡坦及三唑仑对人体前庭功能具有一定的影响 ,但这种影响持续时间较短 ,对人体的空间定向及平衡能力无残留后遗效应  相似文献   
4.
Urine samples from 402 victims of ski accidents were analyzed for the presence of benzodiazepines (BZD) and alcohol. Eighty-one (20%) samples were positive for alcohol; BZD were detected in 34 (8.5%) cases. Ten of the samples (2.5%) were found to be positive for both alcohol and BZD. Subjects who were positive for either alcohol or BZD or both were older than the other persons examined. The prevalence of alcohol was significantly higher among male accident victims. BZD intake could be demonstrated to have a significant influence on the severity of injuries. Besides an increased awareness of the need for skier education regarding drug use, heightened attention of medical caregivers is warranted to inform their patients about potential accident hazards in sport activities when BZD are prescribed.  相似文献   
5.
6.
The question whether the benzodiazepine receptor site in astrocytes or in neurons might be identical to the adenosine uptake site was studied by determining pharmacological profiles, inhibition types, and the effects of benzodiazepine antagonsts in primary cultures of either astrocytes or neurons. Fourteen different benzodiazepines and five different adenosine uptake inhibitors displaced [3H] diazepam and inhibited adenosine uptake in both astrocytes and neurons. However, the rank orders (determined as IC50 values) with which these two parameters were affected were profoundly different, indicating dissimilarities between these two sites. For several of the compounds a difference in inhibition type (competitive vs. noncompetitive) was observed between the benzodiazepine-binding site and the adenosine uptake site in astrocytes and/or neurons, which further corroborated the conclusion of a difference between the benzodiazepine-binding site and the adenosine uptake site. Finally, the neuronal benzodiazepine antagonists RO 15-1788 and CGS-8216 and the astrocytic benzodiazepine antagonist PK 11195, which reverse the action of benzodiazepines, were not able to reverse inhibition of adenosine uptake by diazepam but exerted an inhibitory effect of their own.  相似文献   
7.
Exposure of primary cultured astrocytes for 3 days to 1 μM of either dopamine, serotonin or norepinephrine resulted in upregulation (25–34% increase in Bmax) of the peripheral-type benzodiazepine receptors (PBRs) labeled with [3H]Ro5-4864. A similar treatment with γ-aminobutyric acid [GABA] caused a 2-fold increase in the affinity (Kd) of [3H]Ro5-4864. The monoamines tested and GABA had no effect on the binding parameters of [3H]PK 11195, another selective PBR ligand. The present study indicates that Ro5-4864 binding sites are susceptible to regulation by specific neurotransmitters and provides further evidence for the distinction between Ro5-4864 and PK 11195 binding sites of the PBRs in cultured astrocytes.  相似文献   
8.
The 11C-labelled benzodiazepine antagonist Ro 15–1788 (flumazenil) and positron emission tomography (PET) were used to determine quantitative characteristics of benzodiazepine receptor binding in the neocortex of healthy young men. Saturating doses of unlabelled flumazenil administered i.v., before or together with the ligand-reduced 11C-flumazenil accumulation in the neocortex by about 90 per cent. Saturating doses of unlabelled flumazenil had little effect on the accumulation of radioactivity in the benzodiazepine receptor-poor regions such as pons or white matter. By giving graded doses of unlabelled flumazenil together with the tracer, saturation isotherms were obtained allowing the calculation of receptor density (Bmax) and equilibrium dissociation constant (Kd) values on the basis of certain assumptions Bmax values were in the order of 90 pmol/g and Kd values in the order of 10 nM in the neocortex. Scatchard and Hill plots of the radioactivity data indicated that 11C-flumazenil binds to saturable sites of a homogeneous population. The data indicate that intravenous doses of 1 or 2 mg flumazenil result in a benzodiazepine receptor occupancy of about 50 per cent. The method described should be useful for studying regional differences in benzodiazepine receptor characteristics in the living human brain in healthy subjects and neuropsychiatric disorders, and also in relation to treatment with drugs interacting with benzodiazepine receptors.  相似文献   
9.
Impairment on neuropsychological tests during steady-state drug use and withdrawal, and after discontinuation of benzodiazepines, was studied in primary benzodiazepine-dependent patients. One group of patients was tested before and the other group after the initiation of a gradual tapering-off of the drug, and both groups were tested approximately 1 year later. At the initial assessment, both groups of patients showed impairment on most of the tests of general intelligence and on several of the tests in the Halstead-Reitan battery, as well as on a test of nonverbal memory, in comparison with healthy controls. At follow-up the patient groups had reached the level of the control group. This study confirmed earlier observations of neuropsychological deficits in long-term benzodiazepine-using patients and demonstrated that these changes are at least partly reversible by discontinuing drug intake.  相似文献   
10.
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