Abstract：
:Certain pharmacological properties of methyl beta-carboline-3-carboxylate (beta-CCM), a benzodiazepine receptor ligand, have been investigated in chicks. Although beta-CCM has been established previously as an "inverse agonist" of benzodiazepine receptors in rodents, having effects opposite to those of benzodiazepines in a variety of tests, in chicks this compound had a different pharmacological profile. Firstly, in contrast to the overt convulsant action of beta-CCM in other species, beta-CCM (0.05-40 mg/kg) did not produce convulsions by itself in chicks, but it was only proconvulsant. Secondly and most surprisingly, beta-CCM, like diazepam, produced in chicks a sedation which could be blocked by the benzodiazepine receptor antagonist Ro 15-1788. Thus it appears that beta-CCM can function both as an agonist and as an inverse agonist in this animal.
journal_name
Life Scijournal_title
Life sciencesauthors
Venault P,Prado de Carvalho L,Brown CL,Dodd RH,Rossier J,Chapouthier Gdoi
10.1016/0024-3205(86)90201-8subject
Has Abstractpub_date
1986-09-22 00:00:00pages
1093-100issue
12eissn
0024-3205issn
1879-0631pii
0024-3205(86)90201-8journal_volume
39pub_type
杂志文章相关文献
LIFE SCIENCES文献大全abstract：:The aim of the study was to explore the effect of an acute dose of creatine (Cr) ingestion on serum Cr and serum creatinine (Crn) concentrations. Sixteen healthy subjects ingested a single dose of Cr (20 g) followed by the measurement of serum Cr and Crn concentration for 3 h up to a maximum of 6 h (n=6). In response ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(99)00512-3
更新日期：1999-10-29 00:00:00
abstract：:Thermodynamic analysis of pharmacologic data potentially offers an insight into the molecular events underlying drug-receptor interactions not obtainable by other techniques. Embodied in thermodynamics are the laws governing the interconvertibility of heat and work and, hence, it is a particularly apt framework for th...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/0024-3205(89)90182-3
更新日期：1989-01-01 00:00:00
abstract：:Using a ligation method, rat rectal epithelium was exposed to 2% sodium salicylate, and light and electron microscopic methods were used to assay for: 1) permeability of the epithelium to a marker dye, trypan blue, and 2) damage expressed in terms of disruption of the epithelial surface. Rectal mucosa was exposed to s...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(83)90656-2
更新日期：1983-09-12 00:00:00
abstract：:A series of studies were conducted to determine the effects of leucine-(leu-) enkephalin and methionine-(met-) enkephalin on perfusion pressure. These experiments utilized isolated perfused femoral arterial preparations in pentobarbital-anesthetized cats. The enkephalins were administered intraarterially into the femo...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(82)90047-9
更新日期：1982-10-11 00:00:00
abstract：:Alpha(1)-adrenergic receptors are one of the three subfamilies of G protein coupled receptors activated by epinephrine and norepinephrine to control important functions in many target organs. Three human subtypes (alpha(1A), alpha(1B), alpha(1D)) are derived from separate genes and are highly homologous in their trans...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2003.07.008
更新日期：2003-12-12 00:00:00
abstract：:[3H]ET (etorphine), which is considered either as an "universal" ligand or a mu agonist, interacts with identical affinities KD = 0.33-0.38 nM to hybrid cells and rabbit cerebellum, pure delta and mu-enriched opioid receptor preparations, respectively. In rat brain tissue, [3H]ET binding is inhibited by DAGO (Tyr-D-Al...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(87)90452-8
更新日期：1987-08-10 00:00:00
abstract：:Obesity, the metabolic syndrome (MetS), and type 2 diabetes (T2DM) are associated with heightened cardiovascular risk. Given the vasoconstrictor and proatherogenic properties of endothelin (ET)-1, increased ET-1 activity has been postulated to participate in the derangement of adiposity-related vascular homeostasis. T...
journal_title：Life sciences
pub_type： 杂志文章,评审
doi：10.1016/j.lfs.2014.02.028
更新日期：2014-11-24 00:00:00
abstract：:Rats with experimental allergic encephalomyelitis (EAE) induced with myelin or spinal cord show decreases in the content of sulphatides and cerebrosides and increases in the level of esterified cholesterol in the CNS. In this work it is shown that brain sulphatide changes can be obtained by injection of mixtures conta...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(82)90600-2
更新日期：1982-03-08 00:00:00
abstract：:The relative affinities of nortriptyline (NT) and its 10-hydroxymetabolites to rat brain muscarinic acetylcholine receptors have been determined by competition with 3H-quinuclidinyl benzilate binding. It is shown that the major NT metabolite, E-10-OH-NT, has only 1/18 the affinity of NT for the muscarinic receptor. Si...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(84)90395-3
更新日期：1984-09-24 00:00:00
abstract：AIM:Despite recent advances in therapeutic strategies, cancer is still a leading cause of mortality worldwide. Mitochondrial dysfunction is implicated in cancer initiation and metastasis, and even in chemo- and radio-resistance. However, the precise role of mitochondria in cancer is crosstalk and controversial. This st...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.117339
更新日期：2020-03-01 00:00:00
abstract：:2',6'-Dimethyl substitution of the Tyr(1) residue of opioid agonist peptides and deletion of the positively charged N-terminal amino group or its replacement with a methyl group has recently been shown to represent a general structural modification to convert opioid peptide agonists into antagonists. This conversion r...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(03)00389-8
更新日期：2003-06-27 00:00:00
abstract：:Basic fibroblast growth factor (bFGF) has a neurotrophic effect both in vitro and in vivo, and is considered to play an important role in the maintenance of neuronal functions in the normal brain. Neural damage in brain contusion progresses after the primary injury of trauma because of cerebral hemodynamic and metabol...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(94)00332-7
更新日期：1994-01-01 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：:Two breeds of rats, Charles River Wistar [Crl(Wi)Br.] and HSD Wistar [Wistar per LATI (Budapest) Br.], with remarkable difference in learning performance were selected. The rats were trained in the shuttle box with 100 trials per day and the number of conditioned avoidance responses (CARs), the escape failures (EFs) t...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(96)00037-9
更新日期：1996-01-01 00:00:00
abstract：:Physiological, pharmacological and toxicological responses to two regimens of cocaine administration were compared between spontaneously hypertensive (SHR) and Wistar-Kyoto (WKY) rats. An initial experiment examined renal excretory and hemodynamic function in response to an acute volume load in anesthetized SHR and WK...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(89)90254-3
更新日期：1989-01-01 00:00:00
abstract：:We determined whether two naturally occurring steroids, cortisol and 17beta-estradiol (E2), can rapidly modulate the activity of an important membrane protein, human erythrocyte (RBC) Na+,K+-ATPase, an enzyme that does not bind either hormone directly. We also determined the membrane binding locations for cortisol and...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(99)00360-4
更新日期：1999-01-01 00:00:00
abstract：:Single unit recordings were obtained from putative dopaminergic neurons in the substantia nigra of awake, freely moving rats. The cells exhibited waveforms, range of firing rates and types of firing patterns identical to those of identified DA neurons of anesthetized or paralyzed rats. Two firing patterns were observe...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(85)90448-5
更新日期：1985-05-20 00:00:00
abstract：:We studied the effect of thapsigargin on intracellular calcium levels ([Ca2+]i) measured by fura-2 fluorimetry in Madin Darby canine kidney (MDCK) cells. Thapsigargin elevated [Ca2+]i dose dependently with an EC50 of approximately 0.15 microM. The Ca2+ signal consisted of a slow rise, a gradual decay and a plateau. De...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(98)00561-x
更新日期：1999-01-01 00:00:00
abstract：:Reoxygenation of the ischemic tissue promotes the generation of various reactive oxygen metabolites (ROM) which are known to have deleterious effects on various cellular functions. This study was designed to determine the possible protective effect of mesna (2-Mercaptoethane Sulfonate) on renal ischemia/reperfusion (I...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2004.04.029
更新日期：2004-09-24 00:00:00
abstract：:The putative anxiolytic activity of succinic acid was examined in male mice by using a number of experimental paradigms of anxiety and compared with that of the known anxiolytic compound diazepam. Use of the elevated plus-maze test revealed that diazepam (1.0, 2.0 and 4.0 mg/kg, PO) or succinic acid (3.0 or 6.0 mg/kg,...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2003.06.017
更新日期：2003-11-07 00:00:00
abstract：:The effects of tetrandrine (TET) on the contractile responses of rat aortic rings and perfused rat mesenteric arteries to phenylephrine (PE) were investigated. TET inhibited the maximal contraction to PE in a concentration-dependent manner. TET significantly inhibited the transient contraction in Ca(2+)-free medium pr...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(96)00552-8
更新日期：1996-01-01 00:00:00
abstract：:Proteinase inhibitors were tested for their ability to inhibit prolactin (PRL) and growth hormone (GH) release by cultured anterior pituitary cells of the rat. Inhibitors of microbial origin (chymostatin, elastatinal, leupeptin) had either no or a moderate effect on hormone release while some tripeptide aldehydes, esp...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/0024-3205(85)90636-8
更新日期：1985-02-11 00:00:00
abstract：:Administration of dexamethasone (DEX) during late gestation is a model to study growth restriction in rodents, but the pup's mortality index can be high, depending on DEX dosage, and little is known about the effects of DEX on maternal care (MC). Considering that an inadequate MC can also contribute to pup's mortality...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.118599
更新日期：2021-01-01 00:00:00
abstract：:Mitochondria play a crucial role in the induction and execution of apoptosis. Accordingly, recent suggestions have been made to use agents that directly act on mitochondria to trigger apoptosis so that drug-sensitive and-resistant tumour cells can be eliminated. To test this hypothesis, human hepatocarcinoma HepG2 and...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(02)02103-3
更新日期：2002-10-25 00:00:00
abstract：:Lewis rats were trained to self-stimulate the medial forebrain bundle (MFB) using a rate-frequency paradigm. They were then tested for the effects of the cannabinoid receptor agonist CP 55,940, the selective cannabinoid receptor antagonist SR 141716 and the dopamine D1 receptor antagonist SCH 23390. CP 55,940 (0, 10, ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(01)01366-2
更新日期：2001-11-21 00:00:00
abstract：AIMS:Thiamine is an important cofactor present in many biochemical reactions, and its deprivation can lead to heart dysfunction. Little is known about the influence of thiamine deprivation on the electrophysiological behavior of the isolated heart cells and information about thiamine deficiency in heart morphology is c...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2009.03.011
更新日期：2009-06-05 00:00:00
abstract：AIMS:Inducible nitric oxide synthase (iNOS) pathway has been in the limelight since its discovery as a key mediator in the process of liver fibrogenesis. Therefore, the objective of the current study was to elucidate the in vivo molecular mechanism underlying the hepatic preventive relevance of eugenol (EUG) and telmis...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2018.11.031
更新日期：2019-01-01 00:00:00
abstract：AIMS:Cisplatin is an anticancer agent marred by nephrotoxicity. Limiting this adverse effect may allow the use of higher doses to improve its efficacy. The Wnt/β-catenin signaling pathway plays a critical role in nephrogenesis and repair of renal diseases. BIO, a small molecule agonist of this pathway, exerted a protec...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/j.lfs.2020.118672
更新日期：2020-12-15 00:00:00
abstract：:NSAIDs can elevate blood pressure through mechanisms such as renal vasoconstriction and sodium retention. These effects are particularly evident in hypertensive individuals. Nitric oxide-releasing NSAID derivatives have been shown to have greatly reduced toxicity in the gastrointestinal tract and kidney. We therefore ...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(98)00072-1
更新日期：1998-01-01 00:00:00
abstract：:Brief electrical pulses applied to the rat tail elicit a complex vocal response which includes audible (peeps, chatters) and ultrasonic (USV) components. Aspirin and amitriptyline had no effect on the vocal responses. Morphine showed a dose-dependent and naloxone reversible antinociceptive effect on the 1st and 2nd au...
journal_title：Life sciences
pub_type： 杂志文章
doi：10.1016/s0024-3205(98)00450-0
更新日期：1998-01-01 00:00:00
