Abstract：
:5-(2'-[18F]Fluoroethyl)flumazenil ([18F]FEF), a fluorine-18-labeled analogue of the benzodiazepine antagonist flumazenil, was evaluated for use with positron emission tomography (PET). PET imaging of a baboon after i.v. injection of [18F]FEF showed that the radiofluorinated ligand rapidly localized in vivo within benzodiazepine receptor-rich cerebral tissues, and that selective disposition was retained for over 2 h. Coinjection of unlabeled flumazenil (0.55 mg/kg i.v.) abolished the heterogeneous cerebral distribution of the tracer; receptor-specific uptake was reduced by approximately 95%. The fluorinated benzodiazepine antagonist was degraded in vivo only to polar radiometabolites that do not cross the blood-brain barrier. [18F]FEF has advantages over existing PET radiopharmaceuticals, and is a promising radioligand for non-invasive evaluation of central benzodiazepine receptor binding in vivo.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Moerlein SM,Perlmutter JSdoi
10.1016/0014-2999(92)90153-ukeywords:
subject
Has Abstractpub_date
1992-07-21 00:00:00pages
109-15issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(92)90153-Ujournal_volume
218pub_type
杂志文章abstract：:The persistence of neurogenesis raises the idea that neurons produced by the resident or transplanted neural stem cells could replace the neurons lost from brain injury or neurodegenerative disease. Therefore, compounds or methods for promoting neuronal differentiation become the focus of neurodegenerative disease the...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.05.017
更新日期：2016-09-05 00:00:00
abstract：:This work evaluates the antinociceptive and constipating effects of the combination of 3.2 mg/kg s.c. morphine with 177.8 mg/kg s.c. metamizol in acutely and chronically treated (once a day for 12 days) rats. On the 13th day, antinociceptive effects were assessed using a model of inflammatory nociception, pain-induced...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01344-4
更新日期：2002-04-26 00:00:00
abstract：:Galangin, a flavonol derived from Alpinia officinarum Hance and used as food additives in southern China, induces apoptosis and autophagy to suppress the proliferation of HepG2 cells. In this study, we demonstrated that galangin induced autophagy by increasing the ratio of AMP/TAN in HepG2 cells. It stimulated the pho...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.08.026
更新日期：2013-10-15 00:00:00
abstract：:Bronchoconstrictor responses were measured in lungs isolated from spontaneously hypertensive (SHR) and normotensive rats, perfused via the airways. Lungs from SHRs were more responsive than lungs from normotensive rats to methacholine, 5-hydroxytryptamine (5-HT), arachidonic acid or prostaglandin H(2). The responses o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.02.005
更新日期：2004-03-19 00:00:00
abstract：:There is some controversy as to whether 5-HT(2C) receptor agonists are anxiogenic or anxiolytic. The effects of the novel 5-HT(2C) receptor agonist, (S)-2-chloro-5-fluoro-indol-1-yl)-1-methyl ethylamine fumarate (RO 60 0175), in three models of anxiety were therefore tested. RO 60 0175 was found to induce hypolocomoti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00706-2
更新日期：2000-01-10 00:00:00
abstract：:Lergotrile and apomorphine, two direct-acting dopamine agonists, caused marked hyperglycemia in fasted rats, while compounds which release endogenous dopamine (amphetamine, methylphenidate) or inhibit dopamine reuptake (LR5182), failed to elevate blood glucose. The effect of lergotrile was dose dependent, causing bloo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90028-1
更新日期：1979-10-26 00:00:00
abstract：:The non N-methyl-D-aspartate (NMDA) receptor antagonists dinitroquinoxaline-2,3-dione (DNQX) and 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), both inhibit the visually driven response of sustained ganglion cells in the cat retina in vivo. In contrast to these findings, the potent NMDA receptor antagonist 3-[+/- )-2-ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90483-4
更新日期：1989-05-19 00:00:00
abstract：:To investigate the role of ATP-sensitive K+(KATP) channels on pacemaker activity in interstitial cells of Cajal (ICC), whole-cell patch clamping, RT-PCR, and intracellular Ca2+([Ca2+]i) imaging were performed in cultured colonic ICC. Pinacidil (a K+ channel opener) hyperpolarized the membrane and inhibited the generat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.05.029
更新日期：2017-08-15 00:00:00
abstract：:Nerisopam, an anxiolytic and antipsychotic homophthalazine induces rapid, intense expression of Fos-like immunoreactivity in the rostral, dorsomedial and lateral parts of the striatum in the rat. Fos-positive cells also occurred in the globus pallidus, the olfactory tubercle and in the accumbens nucleus (in the cone a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01008-x
更新日期：1997-07-16 00:00:00
abstract：:Rats were injected with 15 mg/kg (i.p.) mianserin or vehicle (saline) for 4, 10 or 21 days and 5-HT2 receptor binding and mRNA levels measured. Treatment with mianserin induced a substantial decrease in 5-HT2 radioligand binding (44-59% decrease; P less than 0.05 vs. control). No changes in the amount of 5-HT2 or, as ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90093-w
更新日期：1991-06-19 00:00:00
abstract：:Gastric lesions were provoked in all rats that had received intraperitoneally a single dose of the dopamine antagonists haloperidol, metoclopramide or domperidone 24 h before. Dose-dependence was demonstrated for haloperidol. This drug induced gastric lesions as early as 90 min after its application. The ulcerogenic e...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90522-4
更新日期：1986-11-12 00:00:00
abstract：:Acute leukemia is a malignant clonal hematopoietic stem cell disease. In the current study, we examined the effects of bryostatin 5 on acute monocytic leukemia cells in vitro and in vivo. We also explored the mechanisms and pathways underlying the increase in apoptosis induced by bryostatin 5. Bryostatin 5 inhibited t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.08.012
更新日期：2013-10-15 00:00:00
abstract：:Intracellular recording was used to study the effect of uncouplers of oxidative phosphorylation on miniature endplate potentials (m.e.p.p.s) in skeletal muscles from dystrophic mice and their clinically normal littermates. Control m.e.p.p. frequency in muscles from dystrophic mice was not significantly different from ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90637-1
更新日期：1988-02-16 00:00:00
abstract：:The effects of loxapine and its hydroxylated metabolites 7-hydroxyloxapine and 8-hydroxyloxapine on 3H-spiroperidol binding to rat striatal membranes were investigated. Whereas 7-hydroxyloxapine and loxapine displayed strong affinities for 3H-spiroperidol binding sites, 8-hydroxyloxapine was essentially inactive. The ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90396-0
更新日期：1979-04-15 00:00:00
abstract：:A characteristic of endothelia damage and repair is the turnover of extracellular matrix components. As a part of extracellular matrix glycosaminoglycan (GAG), hyaluronic acid (HA, main component of glycocalyx) is not only involved in inflammation, proliferation, differentiation of cells, and tissue remodeling, but al...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172413
更新日期：2019-08-05 00:00:00
abstract：:Flavonoids are polyphenols frequently consumed in the diet they have been suggested to exert a number of beneficial actions on human health, including anti-inflammatory activity. This study investigated the immunomodulatory effects of two flavonoids, Chrysin and Hesperetin. The effects of flavonoids on B and T cell pr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.07.017
更新日期：2017-10-05 00:00:00
abstract：:D,L-Propranolol given in single doses by gavage or s.c. injection to awake rats, always slowed the heart without affecting blood pressure. Doses of 0.2 mg/100 g injected twice daily lowered systolic pressure after 3 days in DOCA hypertensive but not in normotensive or spontaneously hypertensive rats. When chronic trea...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90038-3
更新日期：1977-06-15 00:00:00
abstract：:The direct relaxing effect of halothane on airway smooth muscle has been reported to involve the reduction of the cytosolic Ca2+ concentration ([Ca2+]i) and the [Ca2+]i-independent inhibitory mechanism. To clarify the extent of the contribution of these mechanisms, the effect of halothane on the [Ca2+]i-tension relati...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00617-6
更新日期：1996-11-21 00:00:00
abstract：:In conscious rats, intracerebroventricular (i.c.v.) treatment with the GABA agonist muscimol (1-100 ng) suppressed the pressor responses to ANG II (100 ng i.c.v.) in a dose-dependent and reversible fashion. Treatment i.c.v. with GABA (1-500 micrograms) produced a similar but shorter inhibition. Inhibition of endogenou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90207-8
更新日期：1983-05-20 00:00:00
abstract：:We have already demonstrated that arachidonic acid (AA) inhibits carrageenin-induced granuloma growth in vivo and that this effect is related to an increase in prostaglandin E2 formation. As prostaglandin E1 has been shown to be more effective in inhibiting granuloma growth than prostaglandin E2 we investigated the ef...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90234-7
更新日期：1986-05-27 00:00:00
abstract：:Inflammatory processes are critical promoting factors of chronic pain states, mostly by inducing peripheral and central sensitization of the nociceptive system. These processes are associated with a massive increase in glutamatergic transmission, sometimes facilitated by spinal disinhibition. In this study, we used et...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.12.018
更新日期：2019-01-15 00:00:00
abstract：:Levtiracetam (Lev), an inhibitor of SV2A (synaptic vesicle protein A2), affected the ATP-dependent priming of Ca(2+)-regulated exocytosis in antral mucous cells of guinea pig. In antral mucous cells, the Ca(2+)-regulated exocytosis, which is activated by acetylcholine (ACh), consists of an initial peak that declines r...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.09.037
更新日期：2013-12-05 00:00:00
abstract：:Fructose-2,6-bisphosphate is a potent activator of 6-phosphofructo-1-kinase, a key enzyme in glycolysis. We previously revealed that sulfonylureas stimulate fructose-2,6-bisphosphate production in the rat liver by activating 6-phosphofructo-2-kinase. In the present study, we show that CS-045, a new antidiabetic agent,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90462-6
更新日期：1994-03-21 00:00:00
abstract：:Cats, sedated and paralyzed, showed a significant increase in body temperature after intravenous injection of morphine while animals with additional spinal blockade (C3) from injection of 2% lidocaine solution, did not. The results suggest that motor activity is not necessary for morphine-induced hyperthermia in the c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90113-9
更新日期：1978-06-01 00:00:00
abstract：:We used in vitro autoradiography to identify the endothelin-1 receptor subtype(s) in the superficial gray layer of the superior colliculus of rats. These studies showed dense binding of (3-[125I]iodotyrosyl13)-[Ala11,15]Ac-endothelin-1-(6-2 1) (BQ3020) (for endothelin ETB receptors), while tissues incubated with [125I...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00205-2
更新日期：1998-04-17 00:00:00
abstract：:Salvianolic acid B (SalB) is a polyphenolic compound found in Salvia miltiorrhiza Bunge that has several anti-oxidative and anti-inflammatory effects. In the present study, we investigated whether SalB has neuroprotective effects in an amyloid β (Aβ) peptide-induced Alzheimer's disease mouse model. Mice were injected ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.02.015
更新日期：2013-03-15 00:00:00
abstract：:Nonsteroidal anti-inflammatory drugs (NSAID) inhibit cyclooxygenase activity and cause gastrointestinal damage in part by promoting leukocyte accumulation in the mucosa. Our aim was to evaluate the effects of selective blockade of the isoenzymes cyclooxygenase-1 and cyclooxygenase-2 on leukocyte adhesion in vivo. Leuk...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01342-0
更新日期：2002-04-05 00:00:00
abstract：:Longitudinal organ bath preparations of the rat duodenum, jejunum and ileum were tested for their responsiveness to GABA-receptor agonists. The GABAA-receptor agonists, GABA and 3APS, induced non-adrenergic, non-cholinergic relaxations and/or contractions, although the magnitude and type of response varied depending u...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90274-3
更新日期：1987-09-11 00:00:00
abstract：:Cannabinoid CB(2) receptor is reported to be expressed in varying amounts in different human immune subpopulations. To examine the expression pattern of CB(2) in the mouse, immune cell subpopulations were purified and studied by semiquantitative Reverse Transcription-Polymerase Chain Reaction (RT-PCR). CB(2) mRNA was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01122-0
更新日期：2001-07-06 00:00:00
abstract：:The purpose of the present study was to characterize the nature of the behavioural response to substance P (SP) infusion into the substantia nigra and to evaluate this response in 6-hydroxydopamine (6-OHDA) caudate lesioned rats. The effects of SP infusions (3 microgram in 1 microliter bilaterally) were assessed in an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90216-4
更新日期：1979-12-07 00:00:00
