Abstract:
:Premazepam (PRZ) in vitro competitively displaced 3H-diazepam (DIA), 3H-flunitrazepam (FLU) and 3H-RO 15-1788 from their binding sites on rat brain synaptosomes, with a potency intermediate to other benzodiazepines (BDZs), and Hill coefficients near 1 in different brain regions. Incubation at 37 degrees C reduced premazepam's affinity for BDZ receptors to a lower extent than other benzodiazepines and had no effect on the Hill coefficient. The IC50 of PRZ on 3H-RO 15-1788 and 3H-FLU binding was markedly reduced by GABA in rat cortex, like those of reference classical BDZs, but was GABA-independent in the cerebellum. The IC50 of the BDZ antagonist, RO 15-1788 was unaffected by GABA in both brain areas. The possibility that PRZ behaves as a partial agonist in the cortex and as an antagonist in the cerebellum is discussed.
journal_name
Life Scijournal_title
Life sciencesauthors
Barone D,Colombo G,Glasser A,Luzzani F,Mennini Tdoi
10.1016/0024-3205(84)90646-5subject
Has Abstractpub_date
1984-07-23 00:00:00pages
365-71issue
4eissn
0024-3205issn
1879-0631pii
0024-3205(84)90646-5journal_volume
35pub_type
杂志文章相关文献
LIFE SCIENCES文献大全abstract::Intravenous injection of prostacyclin (100 micrograms/kg) in rats resulted in a decrease of systolic blood pressure within 2 minutes. Concentrations of cAMP in 15 brain regions and nuclei were determined by radioimmunoassay. In lower brain stem nuclei, such as the nucleus of the solitary tract and the lateral reticula...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(87)90439-5
更新日期:1987-12-07 00:00:00
abstract::To understand whether chronic inflammation alters the development of morphine tolerance, the tail-flick test was used to evaluate the analgesic effect of morphine (75 mg tablet, s.c.) in the arthritic rats at the day 9-12 after the inoculation with Freund's adjuvant. Spinal cord monoamines and amino acid neurotransmit...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(99)00008-9
更新日期:1999-01-01 00:00:00
abstract::14C-Imipramine was administered to male and female Sprague-Dawley rats and animals were sacrificed at 4, 8, 12, and 20 hours later. At all time points, total radioactivity in female lung was several-fold higher than in males. In addition, female lungs had a higher concentration of desmethylimipramine (DMI) as compared...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(82)90610-5
更新日期:1982-03-01 00:00:00
abstract::Neuron specific enolase (NSE), an isoenzyme of the glycolytic enzyme enolase, has been established by immunocytochemical means as a marker of morphological and functional maturation in central neurons and appears late in development. However, little is known about the presence of NSE in developing peripheral neurons a...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(84)90598-8
更新日期:1984-01-16 00:00:00
abstract:AIMS:Cerebral atrophy resulting from neurodegeneration is highly prevalent in individuals with diabetes; however, the underlying mechanisms for diabetic neurodegeneration are not fully understood. Here we hypothesized that hyperglycemia induces molecular signaling that favors induction of proliferation in post mitotic,...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2018.05.019
更新日期:2018-07-15 00:00:00
abstract:AIMS:In this study, we investigated the effects of Bax-inhibiting peptide (Bip)-V5, an anti-apoptosis membrane-permeable peptide, on the 6-hydroxydopamine (6-OHDA) induced Parkinson's disease (PD) model rats. MATERIALS AND METHODS:Rats were randomly divided into five groups: Control, 6-OHDA only, Vehicle+6-OHDA, zVAD+...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2015.11.019
更新日期:2016-01-01 00:00:00
abstract::Testosterone propionate, cortisone, or sesame oil vehicle were given to rats during the last week of pregnancy so that effects of the hormones on anogenital distance, breeding capacity and vaginal opening of the female progeny could be contrasted. Testosterone significantly increased anogenital distance and delayed va...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(92)90248-n
更新日期:1992-01-01 00:00:00
abstract:AIMS:The mechanisms underlying the changes in blood-brain barrier (BBB) integrity and the generation of seizures in childhood associated with preexisting brain lesions like cortical dysplasia (CD) are poorly understood. We investigated the effects of levetiracetam (LEV) on BBB integrity and the survival during hyperthe...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2010.09.014
更新日期:2010-11-20 00:00:00
abstract::Platelet functions are becoming the useful tool for delineating the etiology of pregnancy induced hypertension. Electronmicroscopic studies, efflux and content of 5-HT in platelets and platelet aggregation responses towards various aggregating agents have been measured in 25 normotensive pregnant subjects and 31 PIH s...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(94)00735-7
更新日期:1994-01-01 00:00:00
abstract:AIMS:Reactive oxygen species (ROS) are generated in the ischaemic myocardium especially during early reperfusion and affect myocardial function and viability. Monoterpenes have been proposed to play beneficial roles in diverse physiological systems; however, the mechanisms of action remain largely unknown. This study a...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2017.01.008
更新日期:2017-03-01 00:00:00
abstract::Tobacco smoke exposure has been shown to inhibit brain and platelet MAO B in animals and in humans. Though the mechanism(s) responsible for MAO B inhibition are not known, studies in rodents have shown that nicotine administration does not inhibit brain MAO B. In this study we investigated whether brain MAO B is also ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(98)00251-3
更新日期:1998-01-01 00:00:00
abstract::The pressor effect of hemoglobin-based blood substitutes is due partly to their capacity to scavenge nitric oxide (NO), a potent vasodilator. NO also appears to modulate the release of norepinephrine (NE) from sympathetic nerve endings in some blood vessels. Thus studies were designed to determine if contraction occur...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(96)00269-x
更新日期:1996-01-01 00:00:00
abstract::Excessive fibrosis and extracellular matrix deposition resulting from upregulation of target genes expression mediated by transforming growth factor-beta (TGF-β)/SMAD and hypoxia inducible factor-1 (HIF-1) signaling pathways are the main mechanisms that drive keloid formation. Sumoylation is a protein posttranslationa...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2020.117859
更新日期:2020-08-15 00:00:00
abstract::18-Hydroxycorticosterone (18-OHB) is a precursor of aldosterone and is the only corticosteroid, other than aldosterone, that is synthesized predominantly in the zona glomerulosa. Administration of the dopamine antagonist, metoclopramide results in parallel rises in plasma 18-OHB and aldosterone levels without affectin...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(83)90157-1
更新日期:1983-12-19 00:00:00
abstract::Several serotonin (5-HT) receptor antagonists with varying specificities for the 5-HT receptor types, were studied with regard to their effects on blood glucose levels in mice. The non-selective antagonists, metergoline and methysergide, proved to be hyperglycemic at doses commonly used to antagonize 5-HT receptors. I...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(91)90023-5
更新日期:1991-01-01 00:00:00
abstract:AIMS:Oxaliplatin (l-OHP) is a key drug in therapeutic regimens for metastatic or advanced-stage colorectal cancer, but causes peripheral neuropathy as a dose-limiting adverse effect. It is reported that this peripheral neuropathy results from l-OHP accumulation in dorsal root ganglion (DRG) neurons, and that one of the...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2018.07.006
更新日期:2018-08-15 00:00:00
abstract::This study was designed to evaluate the effects of roxithromycin (RXM), a newly synthesized macrolide antibiotic on allergic responses in mice. RXM was orally administered into BALB/c mice once a day for 42 days in a single dose of 5 mg/kg body weight. Spleen cells (Sp C) collected from mice on day 7, 14, 28 and 42 po...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(93)90154-u
更新日期:1993-01-01 00:00:00
abstract::An animal model of haloperidol-induced tardive dyskinesia was studied in relation to the dietary manipulation of tryptophan and its effect on the movement disorder. This study showed a significant negative behavioral response to the neuroleptic drug, haloperidol. Increased dietary tryptophan (1.0 vs. 0.3%) significant...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(87)90602-3
更新日期:1987-10-05 00:00:00
abstract::Dehydroepiandrosterone (DHEA), the major secretory product of the human adrenal cortex, significantly declines with advanced age. We have previously demonstrated that DHEA prevents the reduction in non-amyloidogenic APP processing, following prolonged stimulation of the muscarinic receptor, in PC12 cells that express ...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(96)00496-1
更新日期:1996-01-01 00:00:00
abstract::Phencyclidine hydrochloride (PCP) was tested for its ability to alter a variety of immune effector and regulatory functions in vitro. B6C3F1 murine splenic lymphocytes or elicited peritoneal macrophages were cultured in vitro with medium only or medium containing 10(-10)-10(-4) M PCP. Macrophages cultured with or with...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(93)90584-p
更新日期:1993-01-01 00:00:00
abstract::We report an ongoing within-family selective breeding project for the severity of handling-induced withdrawal seizures in mice made physically dependent on ethanol by inhalation. Two Withdrawal Seizure Prone (WSP) and two Withdrawal Seizure Resistant (WSR) lines have been subjected to five generations of selection, an...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(83)90751-8
更新日期:1983-09-05 00:00:00
abstract::Environmental estrogens (endocrine disruptive chemicals) have been shown to affect reproduction in wild life and it has been reported that maternal exposure with those chemicals have adverse effects on the male reproductive tract. However, little is known about the potential effects of prepubertal or pubertal exposure...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(99)00502-0
更新日期:1999-01-01 00:00:00
abstract::Nitric oxide (NO) is a highly reactive free radical that is involved in a variety of different biological process. In recent reports, the putative role of NO in the neuropathogenesis of brain inflammation has been demonstrated. And then the relation between neuronal NO and convulsive seizures induced by virus has been...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2003.08.014
更新日期:2004-01-30 00:00:00
abstract::We compared the relative abilities of atropine sulfate and methylatropine, injected i.v. and into the cerebral ventricles (icv), to block pharmacological responses mediated through central and peripheral muscarinic receptors. The hypotensive response to i.v. injection of acetylcholine (peripheral muscarinic receptors)...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(88)90389-x
更新日期:1988-01-01 00:00:00
abstract:AIMS:Acetylcholine (ACh) has been shown to increase ion and water excretion in the kidneys, resulting in hypotension. However, no evidence of renal parasympathetic innervation has been shown, and the source of ACh acting on nephrons is still unknown. The aim of the present study was to identify ACh-producing cells in t...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2011.07.011
更新日期:2011-09-12 00:00:00
abstract::Anandamide (arachidonylethanolamide; AEA) is an endogenous ligand for the cannabinoid receptor and its pharmacological effects are under intensive study. However, AEA has a low aqueous solubility and stability which may restrict its use and may eventually endanger the reliability of the obtained results. In the presen...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(96)00024-0
更新日期:1996-01-01 00:00:00
abstract:AIMS:Brain injuries based on their causes are divided into two categories, TBI and NTBI. TBI is caused by damages such as head injury, but non-physical injury causes NTBI. Prolactin is one of the blood factors that increase during brain injury. It has been assumed to play a regenerative role in post-injury recovery. M...
journal_title:Life sciences
pub_type: 杂志文章,评审
doi:10.1016/j.lfs.2020.118547
更新日期:2020-12-15 00:00:00
abstract::Inert gas narcosis is a neurological syndrome appearing when humans or animals are exposed to hyperbaric inert gases (nitrogen, argon) composed by motor and cognitive impairments. Inert gas narcosis induces a decrease of the dopamine release at the striatum level, structure involved in the regulation of the extrapyram...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/s0024-3205(03)00183-8
更新日期:2003-05-02 00:00:00
abstract::Infusion of oxytocin (OT) into normal dogs, in doses which produced plasma levels of OT in the physiological range, has been shown to increase plasma levels of glucose, insulin and glucagon and increase rates of glucose production and uptake. This study sought to determine whether there was a correlation between these...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/0024-3205(92)90477-7
更新日期:1992-01-01 00:00:00
abstract::Thymic and spleen cells were treated in vitro or in vivo with insulin. The in vitro treatments were done with 10(-6), 10(-9), 10(-12) and 10(-15) M concentrations for 30 min and after that histamine, serotonin, endorphin and triiodothyronine (T3) content of the cells were detected by using antibodies to the hormones a...
journal_title:Life sciences
pub_type: 杂志文章
doi:10.1016/j.lfs.2005.05.084
更新日期:2006-02-02 00:00:00