Abstract:
:Considerable evidence has appeared recently connecting the mechanism of action of some antidepressant drugs with the inhibition of the enzymes responsible for enkephalin degradation. Imipramine in vitro inhibits the enkephalin-degrading aminopeptidase MII and interacts with the enzyme in a mixed competitive-noncompetitive manner. The present work shows that imipramine in vitro also inhibits reversibly soluble enkephalin-degrading aminopeptidase activity in rat brain. Kinetic analysis showed that this enzyme has two different binding sites for the drug, and that imipramine interacts with the enzyme in a mixed noncompetitive-acompetitive way.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Gallego M,Casis L,Casis Odoi
10.1016/s0014-2999(98)00686-4subject
Has Abstractpub_date
1998-10-30 00:00:00pages
113-6issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(98)00686-4journal_volume
360pub_type
杂志文章abstract::The spinal cord dorsal horn contains neural mechanisms which can greatly facilitate pain. It is well established that excitatory amino acids, aspartate and glutamate, are involved in the spinal transmission of nociceptive information and in the development of hyperalgesia. In the present study, intrathecal (i.t.) admi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00145-8
更新日期:1996-06-03 00:00:00
abstract::The effects of dopamine (DA) and of two selective DA DA1 agonists (SKF 38393 and SKF 82526) on adenylate cyclase activity were studied with human kidney cortex membrane preparations. DA elicited a dose-related stimulation of adenylate cyclase activity with an EC50 of 60 microM. The selective DA DA1 antagonist SCH 2339...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90667-x
更新日期:1988-05-10 00:00:00
abstract::A series of 26 drugs was tested for in vitro binding to opiate receptors in the presence and absence of 0.1 M NaCl. The results were correlated with assays for in vivo pharmacological potency. Highly significant correlation was found between binding in the presence and absence of sodium ions and analgesic potency. For...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(77)90334-x
更新日期:1977-12-01 00:00:00
abstract::We examined the effect of HSR-81 ((-)-(R)-alpha-[(tert-butylamino)methyl]-2-chloro-4-hydroxybenzyl alcohol L-tartrate), a newly developed, potent and selective beta 2-adrenoceptor agonist, as well as ritodrine and isoproterenol, on the spontaneous rhythmic contraction in uteri isolated from late pregnant, middle pregn...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(96)00277-4
更新日期:1996-07-04 00:00:00
abstract::The present study investigated the mechanisms involved in the antinociception produced by the triterpene 3β, 6β, 16β-trihydroxylup-20(29)-ene (TTHL) in mice. TTHL administered by intra-gastric (i.g.) gavage inhibited glutamate-induced nociception with an ID(50) of 19.0 (13.2-27.5) mg/kg. This action started 60 min (in...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.11.028
更新日期:2011-02-25 00:00:00
abstract::ICI 169,369 is a chemically novel 5-HT antagonist that has higher affinity for the 5-HT2 binding sites in rat cortex than it has for 5-HT1 sites (Ki 1.79 x 10(-8) and 1.58 x 10(-6) M, respectively). In isolated tissue preparations ICI 169,369 was shown to be a competitive antagonist of 5-HT on the rabbit aorta, pig co...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90005-2
更新日期:1988-06-10 00:00:00
abstract::The effects of THIP and isoguvacine on 3H-flunitrazepam binding to washed membranes prepared from the cerebral cortex of adult rats have been examined. THIP, which has only minimal stimulatory effects on benzodiazepine (BZ) receptor binding, has been found to inhibit the stimulation induced by small concentrations (2 ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90321-2
更新日期:1979-10-15 00:00:00
abstract::125I-labelled endothelin-1 was used to identify specific high affinity endothelin-1 binding sites in left ventricular and brain membranes harvested from female age-matched normotensive Wistar Kyoto (WKY) rats and spontaneously hypertensive rats (SHR). Relative to results obtained for brain membranes from normotensive ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90272-8
更新日期:1990-02-27 00:00:00
abstract::Using microdialysis in rat prefrontal cortex, we found that 1 mg/kg of the stimulant methylphenidate and the non-stimulant atomoxetine, two widely used treatments for Attention Deficit/Hyperactivity Disorder (ADHD), produce robust increases in the extracellular levels of histamine, which plays a key role in attention,...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.11.048
更新日期:2007-03-08 00:00:00
abstract::The neuroprotective effects of catalpol, an iridoid glycoside present in the roots of Rehmannia glutinosa, on 1-methyl-4-phenylpyridinium (MPP(+))-induced oxidative stress in cultured mesencephalic neurons, especially dopaminergic neurons, were investigated. Exposure of mesencephalic neurons to 10microM MPP(+) induced...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.04.039
更新日期:2007-07-30 00:00:00
abstract::Alzheimer's disease (AD) is a chronic neurodegenerative disorder that leads to disturbances of cognitive functions. Although the primary cause of AD remains unclear, brain acetylcholine deficiency, oxidative stress and neuroinflammation may be considered the principal pathogenic factors. The present study was construc...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.11.008
更新日期:2014-01-15 00:00:00
abstract::The aim of the study was to assess which tachykinin receptors mediate the contractile response in the guinea-pig isolated bronchi. Experiments with natural tachykinins and receptor-selective tachykinin agonists were performed in the absence or presence of peptidase inhibitors and in bronchi pretreated with phenoxybenz...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90517-t
更新日期:1991-05-17 00:00:00
abstract::The actions of carbachol were studied on the firing response of neostriatal neurons recorded intracellularly from in vitro slice preparations of the rat brain. Carbachol (1-10 microM) reversibly reduced the afterhyperpolarization in neostriatal neurons. This effect was accompanied by an increase in both firing frequen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00263-k
更新日期:1995-08-15 00:00:00
abstract::The effects of prolactin on animal behavior include the stimulation of novelty-induced grooming in rats. This effect has been demonstrated in hyperprolactinaemic animals bearing pituitary homografts under the kidney capsule or after intracerebroventricular (i.c.v.) administration of prolactin. Since plasma prolactin l...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s0014-2999(00)00678-6
更新日期:2000-09-29 00:00:00
abstract::Guanosine 3',5'-cyclic monophosphate (cGMP) is an important second messenger in many biological systems including vascular smooth muscle where it mediates relaxation. Cellular levels of cGMP are regulated primarily by three enzymes; nitric oxide (NO) synthase, soluble guanylate cyclase, and cGMP-phosphodiesterase. Bas...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00307-0
更新日期:1998-06-19 00:00:00
abstract::Chronic administration of amphetamine to cats (twice daily, in doses increasing from 5 to 15 mg/kg over a 10-day period) elicited a number of behaviors e.g., limb flicking, abortive grooming, and excessive head shaking, which were originally proposed as an animal behavioral model for studying the actions of hallucinog...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90138-9
更新日期:1984-04-06 00:00:00
abstract::We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Wh...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00625-7
更新日期:2000-10-06 00:00:00
abstract::Tobramycin inhalation therapy is an effective therapy for cystic fibrosis as well as severe bronchiectasis that is colonized with Pseudomonas aeruginosa. The mechanism responsible for the efficacy of tobramycin in the treatment of severe chronic infectious diseases has not been elucidated. We demonstrate that high-dos...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.03.002
更新日期:2011-05-20 00:00:00
abstract::The pharmacological profile of a novel and newly discovered non-steroidal anti-inflammatory and analgesic compound, 3-(difluoromethyl)-1-(4-methoxyphenyl)-5-[4-(methylsulfinyl)phenyl]pyraz ole (FR140423), was investigated. In recombinant human cyclooxygenase enzyme assays, the inhibition of prostaglandin E2 formation ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00868-1
更新日期:1999-01-22 00:00:00
abstract::Platelet serotonin (5HT) uptake was measured in 18 subjects administered physostigmine salicylate in a double-blind, placebo crossover design. In comparison to placebo, the drug caused a significant transient depression in mood, as measured by self- and observer-rated depression scores. In addition, physostigmine sign...
journal_title:European journal of pharmacology
pub_type: 临床试验,杂志文章
doi:10.1016/0014-2999(85)90543-6
更新日期:1985-02-12 00:00:00
abstract::A single dose of methamphetamine (25 mg/kg i.p.) was administered to young adult gerbils (Meriones unguiculatus) aged 90 days and the number of spices was determined along 40-microns segments of basal, lateral and apical dendrites of pyramidal cells in layers III and V of the prefrontal cortex, after 1.5, 7, 20 and 30...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90937-d
更新日期:1993-09-07 00:00:00
abstract::Sodium nitroprusside produced a dose-dependent increase in extracellular levels of cGMP in the cerebellar cortex in vivo. This was independent of nitric oxide synthase activity. The metalloporphyrins zinc-protoporphyrin-IX, tin-protoporphyrin-IX and zinc-deuteroporphyrin-IX,2,4-bis glycol prevented the increase in cGM...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90149-x
更新日期:1994-05-17 00:00:00
abstract::[Thi5,8,D-Phe7]bradykinin caused hind-paw edema and degranulation of isolated peritoneal mast cells in a dose-dependent manner. Pretreatment with diphenhydramine/methysergide or compound 48/80 completely suppressed the edematous response caused by [Thi5,8,D-Phe7]bradykinin, whereas bradykinin-induced hind-paw swelling...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90836-4
更新日期:1989-02-28 00:00:00
abstract::Stearoyl-CoA Desaturase 1 (SCD1) is a central enzyme that catalyzes the biosynthesis of monounsaturated fatty acids from saturated fatty acids. SCD1 is an emerging target in obesity and insulin resistance due to the improved metabolic profile obtained when the enzyme is genetically inactivated. Here, we have investiga...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.07.004
更新日期:2009-09-15 00:00:00
abstract::A major limitation of cancer treatment is the ability of cancer cells to develop resistance to chemotherapeutic drugs, by the establishment of multidrug resistance. Here, we characterize MC70 as ABC transporters inhibitor and anticancer agent, alone or with chemotherapy. MC70 was analyzed for its interaction with ABCB...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.08.025
更新日期:2011-11-16 00:00:00
abstract::The new dihydropyridine calcium channel antagonist S 11568 and its optical isomers, S 12967 and S 12968 (3 x 10(-6) to 10(-4) M), caused, unlike nifedipine (10(-4) M), equipotent and rapid endothelium-dependent relaxations and increased the content of cyclic GMP in rings of canine femoral arteries. These effects were ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(91)90362-t
更新日期:1991-05-02 00:00:00
abstract::Corticotropin-releasing factor (CRF) plays an important role in sympathetic regulation. Centrally administered CRF elevates plasma catecholamine levels, resulting in CRF-dependent hypertension and tachycardia. We previously reported that brain thromboxane A2 mediates CRF-induced elevation of plasma adrenaline levels, ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.172693
更新日期:2019-11-15 00:00:00
abstract::We tested the hypothesis that calcium from the sarcoplasmic reticulum contributes to exercise-induced muscle damage. Dantrolene sodium (Dantrium) is a muscle relaxant that affects the flux of calcium over the sarcoplasmic membrane. Rats were treated with dantrolene sodium for a week before a 2 h run on a treadmill. We...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90417-5
更新日期:1990-04-10 00:00:00
abstract::The role of protein kinase C in the endothelin-induced contraction was examined in the isolated rabbit saphenous vein in which endothelin-1, endothelin-3, sarafotoxin S6c and IRL 1620 (succinyl-[Glu9,Ala11,15]endothelin-1-(8-21))-induced contraction at the threshold concentrations of 0.1-1 pM. A selective inhibitor of...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00542-0
更新日期:1995-12-27 00:00:00
abstract::A microdialysis/smallbore chromatographic system was used to monitor changes in extracellular dopamine concentration in the striatum of the rat following administration of drugs that block catecholamine uptake. Analysis of 0.5 microliter of dialysate every 5 min showed dose-dependent elevations in extracellular dopami...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90592-9
更新日期:1987-07-23 00:00:00