ISSN:0272-4391    

DOI:10.1002/ddr.430020402

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractIn a 4‐wk double‐blind clinical trial four doses (1, 5, 10, and 20 mg) of flutroline were compared in newly admitted schizophrenic patients. Although there were few statistically significant differences among the four dosage groups, there were at least five indications of greater thereapeutic effectiveness in the higher dosages. The most favorable changes were seen in the 20‐mg group, which was the only group to show improvement in all five factors of the Brief Psychiatric Rating Scale and in which a significant elevation of serum prolactin level occurred at a 6‐hr post‐dose sampling. In a previous clinical trial in which three different daily doses of flutroline (1, 20, and 100 mg) were compared, 20 and 100 mg were found to be equal in their therapeutic effects and superior to 1 mg. Since no dosage between 1 and 20 mg were employed, the possibility that therapeutic effects with flutroline may already be present in daily doses below 20 mg could not be ignored. While the present findings are in favor of this contention, they also indicate that therapeutic efficacy with 20 mg is greater than with 1‐, 5‐, or 10

ISSN:0272-4391    

DOI:10.1002/ddr.430020403

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractTwo patients with ballism were treated successfully with diazepam. It is suggested that diazepam acted as an indirect GABAmimetic drug to correct a functional GABA deficiency secondary to hyperactivity of the dopamine system in the subthalamic nucleus as a cause for ballism.

ISSN:0272-4391    

DOI:10.1002/ddr.430020404

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractThe isolated, electrically stimulated rat epididymal fat pad in vitro was tested under various conditions as a model for neuronally induced lipolysis. A 24‐hr fast, or a preincubation without electrical stimulation, decreased spontaneous lipolysis as measured by glycerol release; however, only slight alterations were seen in the response of the pads during a 40‐min period of electrical stimulation. Spontaneous (nonstimulated) lipolysis was reduced by pretreatment with alpha‐methyl‐paratyrosine‐methylester and increased by pretreatment with reserpine; both of these treatments abolished the response to stimulation. The effects of addition of a variety of agents to the incubation medium confirm the role of a sympathetic nervous‐cyclic 3′,5′‐adenosine‐monphosphate media

ISSN:0272-4391    

DOI:10.1002/ddr.430020405

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractThe pituitary‐adrenal axis suppression and lysosomal membrane stabilization of methyl steroid‐21‐oates, synthesized by modifying the 17β‐ketol side chain of prednisolone, were investigated by measuring plasma corticosterone and by determining abilities of the drugs to decrease extrusion of three liver lysosomal marker enzymes (acid phosphatase, beta‐glucuronidase, and aryl sulfatase) during incubation in severely hypo‐osmotic buffer. Animals were injected with 10 mg/kg drug suspensions i.m. at 20 hr and 2.5 hr prior to sacrifice. The parent compound prednisolone significantly suppressed pituitary adrenal function indicated by decreased plasma corticosterone levels. In contrast, the derivatives did not alter plasma corticosterone levels. When compared to controls, prednisolone, methyl 20‐dihydroprednisolonate, 1‐dehydro‐11β‐hydroxyandrostenedione, and to a lesser extent methyl prednisolonate retained significant lysosomal stabilization capacities, indicative of antiinflammatory activity. These data suggest that the new ester derivatives of prednisolone retained beneficial antiinflammatory activity but were devoid of significant adverse effects upon the p

ISSN:0272-4391    

DOI:10.1002/ddr.430020406

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractThe present study was undertaken to confirm and extend previous observations on the use of morphine‐induced Straub tail and rotarod performance in mice as a means of assessing the efficacy of a compound as a muscle relaxant and its potential for depressant side‐effects, respectively. The ratio of the rotarod to Straub tail ED50s was calculated as an index of specificity. Our results generally confirmed previous reports in the case of diazepam, chlordiazepoxide and dantrolene. Additionally, the recently introduced muscle relaxants, cyclobenzaprine, baclofen, and DS 103‐282 were found effective in blocking Straub tail and their reported clinical specificity was reflected by the specificity observed in the mouse tests. DS 103–282 was found to be the most potent and specific. It is concluded that muscle relaxants with specificity ratios significantly greater than 1.0 appear to have comparatively few depressant effects at therapeutic doses. The relatively simple methods used in the present study appear to be useful in the initial assessment of compounds as potential muscle re

ISSN:0272-4391    

DOI:10.1002/ddr.430020407

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractTR5379 is a novel morphinan with potent antinociceptive activity in the mouse abdominal constriction procedure. It is a narcotic antagonist with a potency similar to that of butorphanol. In rats and monkeys, TR5379 does not appear to induce any physical dependence. Following a 6‐day chronic administration of TR5379 to rats, no indications of withdrawal were observed. TR5379 did not substitute for morphine in either the physically dependent rat or the physically dependent monkey. In the chronically morphinized rat, an acute dose of TR5379 caused the rapid onset of a marked withdrawal syndrom

ISSN:0272-4391    

DOI:10.1002/ddr.430020408

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractThe effects of pancuronium bromide (60, 120, 300, and 600 μg.kg−1, i.v.) and its monoquaternary analogue Org NC 45 (300,750, and 1500 μg.kg−1, i.v.) on the systemic and regional hemodynamic variables were studied in the anesthetized pig. Pancuronium exhibited a dose‐dependent positive chronotropic and inotropic activity. The enhanced oxygen requirement of the myocardium was successfully met by a combination of higher blood supply to, and oxygen extraction by, the tissue. No changes were noticed in cerebral, renal or hepatic arterial blood flow. On the other hand, Org NC 45, which unlike pancuronium lacks vagolytic and sympathomimetic actions, did not cause an increase in heart rate or left ventricular dP/dtmax(LV dp/dtmax). Instead, in the two highest doses (750 and 1500 μg.kg−1) Org NC 45 decreased arterial blood pressure, LV dP/dtmaxand the blood supply to the brain, kidneys, and liver. Neither compounds showed any effect on cardiac metabolism of glucose, lactate, or free fatty acids (FFA), although arterial blood glucose concentration did decrease following the two highest doses of each compound. Since Org NC 45, in a dose of 300 μg/kg−1, which is seven to ten times the ED90for neuromuscular paralysis in man, is completely devoid of systemic and regional hemodynamic effects, and pancuronium in similar dose ratio is not, Org NC 45 might be preferred for use in cardi

ISSN:0272-4391    

DOI:10.1002/ddr.430020409

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractThe effect of chronic intravenous infusion of desmethylimipramine (DMI), amitriptyline, mianserin, bupropion, alprazolam, or diazepam on the density of beta‐adrenergic receptors in the rat cerebral cortex has been investigated in this study. DMI and amitriptyline significantly decreased the density of beta‐adrenergic receptors. Mainserin, bupropion, alprazolam, and diazepam had no significant effect on the density of beta‐adrenergic receptors. Results of this study indicate that mechanisms other than beta‐adrenergic receptors may be involved in the antidepressant activity of thes

ISSN:0272-4391    

DOI:10.1002/ddr.430020410

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY

摘要:

AbstractSynaptosomes (isolated nerve endings) from rat corpus striatum responded to several depolarizing agents by releasing dopamine. Among these agents were KCl, glutamic acid, ouabain, and veratrine. Substance P hexapeptide (SP6) also caused dopamine release, but the magnitude of this effect was small and variable. A number of other neuropeptides (cholecystokinin 1–8, des‐Tyr‐γ‐endorphin, Leu5‐β‐endorphin and substance P) did not alter dopamine release. SP6‐induced dopamine release may result from substance P receptor‐induced depolarization; however, the lack of robustness of the response in this preparation makes it unsuitable for studying agonists and antagonis

ISSN:0272-4391    

DOI:10.1002/ddr.430020411

出版商:Wiley Subscription Services, Inc., A Wiley Company    

年代:1982

数据来源: WILEY