Abstract:
:The localization of neuroleptic receptors was studied in the caudate-putamen (CP) and the zona compacta of the substantia nigra using light microscopic autoradiography of 3H-spiperone binding sites. Lesion of the dopaminergic input to the caudate-putamen produced an increase in receptors in the CP, possibly reflecting denervation supersensitivity. Kainic acid lesions and decortication produced significant decreases of 61% and 18% in striatal receptors. This suggests that in the caudate-putamen most of the dopamine receptors are on intrastriatal neurons, but some are also localized to the afferents from the cortex. Lesion of the nigro-striatal dopaminergic pathway produced a large (48%) decrease in receptor sites in the substantia nigra zona compacta while kainic acid intrastrially and striato-nigral pathway lesions had no significant effect. These results suggest that the majority of dopamine receptors in the zona compacta which bind neuroleptics are located on cell bodies and processes of dopaminergic neurons and are anatomically distinct from dopamine-stimulated adenylate cyclase sites.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Murrin LC,Gale K,Kuhar MJdoi
10.1016/0014-2999(79)90222-xsubject
Has Abstractpub_date
1979-12-07 00:00:00pages
229-35issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(79)90222-Xjournal_volume
60pub_type
杂志文章abstract::The effects of intracerebral microinjections of neurotensin and xenopsin on self-stimulation of the medial prefrontal cortex of the rat were studied. Unilateral microinjections into the medial prefrontal cortex of neurotensin at doses of 0.625, 1.25, 2.5, 5 and 10 nmol produced a dose-related decrease of self-stimulat...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90681-7
更新日期:1993-01-26 00:00:00
abstract::Recently the existence of a neurotensin striatonigral pathway strongly up-regulated by methamphetamine has been demonstrated. The aim of the present study was to investigate, using immunohistochemistry and radioimmunoassay, the modulation of this pathway by dopamine antagonists. Rats were injected either with methamph...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90021-3
更新日期:1994-09-01 00:00:00
abstract::The inhibitory action of bicyclic isoxazole gamma-aminobutyric acid (GABA) analogues and their 4,4-diphenyl-3-butenyl (DPB) substituted derivatives has been investigated in cortical neurones and astrocytes as well as in human embryonic kidney (HEK 293) cells transiently expressing either mouse GABA transporter-1 (GAT-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00263-0
更新日期:1999-06-30 00:00:00
abstract::Soluble amyloid β-protein (Aβ) oligomers are primary mediators of synaptic dysfunction associated with the progression of Alzheimer's disease. Such Aβ oligomers exist dependent on their rates of aggregation and metabolism. Use of selective somatostatin receptor-subtype agonists have been identified as a potential mean...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.03.020
更新日期:2012-05-15 00:00:00
abstract::Chronic obstructive pulmonary disease (COPD) is characterized by an airways inflammation and by an enhanced generation of reactive oxygen species. The aim of our study was to assess the inflammation and the oxidative stress in airways of COPD patients with acute exacerbation of disease and in stability. Furthermore, w...
journal_title:European journal of pharmacology
pub_type: 临床试验,杂志文章
doi:10.1016/j.ejphar.2004.10.007
更新日期:2004-11-28 00:00:00
abstract::The effect of local administration of big endothelin-1 (1-38, big ET-1) has been investigated on blood flow in the skin of anaesthetised rats, measured by 133Xe clearance. The local effects of big ET-1 and big endothelin-3 (1-41, big ET-3) have also been determined on microvessel diameter by intravital microscopy of t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90056-n
更新日期:1993-03-23 00:00:00
abstract::We investigated the effects of an L-type and N-type Ca(2+) channel blocker, cilnidipine, on neurally mediated chronotropic responses to clarify the anti-autonomic profile of cilnidipine in anesthetized dogs. Pretreatment with cilnidipine (0.3, 1.0 and 3.0 microg/kg, i.v.), which decreased mean blood pressure by 5 to 3...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)00738-5
更新日期:2001-02-09 00:00:00
abstract::Nerve growth factor (NGF) is known to regulate the development and survival of select populations of neurons via its binding/activation of the TrkA and p75(NTR) receptors. However, in some physiological circumstances NGF dysregulation can result in debilitating pathologies, including diabetic neuropathies, interstitia...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.03.029
更新日期:2013-05-15 00:00:00
abstract::Compound (+)-R,R-D-84 is an optically active trans-hydroxy-substituted derivative of 4-(2-benzhydryloxy-ethyl)-1-(4-fluorobenzyl)piperidine (D-164). As a hydroxypiperidine analog of GBR 12935, (+)-R,R-D-84 is a candidate dopamine transporter compound for the treatment of cocaine dependence. The present work addresses ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.10.028
更新日期:2004-12-03 00:00:00
abstract::SR 57746A, 4-(3-trifluoromethylphenyl)-N-[2-(naphth-2-yl)ethyl]-1,2,3,6- tetrahydropyridine HCl, was studied for its specific 5-HT1A receptor agonist action and antidepressant-like effects in the rat. The compound showed a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50 3 nM), moderate aff...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90768-4
更新日期:1994-02-21 00:00:00
abstract::The thromboxane mimetic U46619 (11 alpha,9 alpha-epoxymethano PGH2) increased 45Ca2+ uptake in sheep coronary artery rings. A larger increase occurred in endothelium-denuded than in endothelium-inact rings (increase in 45Ca2+ uptake: endothelium intact = 9.6 +/- 3.8, endothelium-denuded = 33.2 +/- 8.1 nmol g-1), in ag...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0926-6917(94)90007-8
更新日期:1994-08-03 00:00:00
abstract::In male Swiss mice, muscimol produced myoclonic jerks. A 3 mg/kg (i.p.) dose induced this response in all of the mice tested and the peak response of 73 jerks per min was observed between 27 and 45 min. Increasing the brain serotonin levels by the administration of 5-hydroxytryptophan (80-160 mg/kg) in combination wit...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90087-x
更新日期:1981-07-17 00:00:00
abstract::Some antidepressants, as well as antiepileptics, are effective for treating pain of varying etiology. The present study was designed to characterize the antinociceptive effects of imipramine, a tricyclic antidepressant, fluvoxamine, a selective serotonin reuptake inhibitor, milnacipran, a serotonin noradrenaline reupt...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.08.049
更新日期:2006-11-21 00:00:00
abstract::Corticotropin-releasing factor (CRF) has been suggested to play an important role in the development of drug dependence and withdrawal. Based on the recent finding that CRF receptor antagonists inhibit the stress-induced relapse to opiate dependence and attenuate anxiety-like responses related to cocaine withdrawal, t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)00840-8
更新日期:2001-03-01 00:00:00
abstract::The biodistribution of S-(-)-4-(2-hydroxy-3-(1'-[18F]fluoroisopropyl)- aminopropoxy)carbazole ([18F]S-fluorocarazolol, a non-selective beta-adrenoceptor antagonist) was studied in rats (60 min after 18F injection when specific binding in peripheral organs was maximal). 18F uptake in brain, erythrocytes, heart and lung...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)00636-l
更新日期:1995-01-16 00:00:00
abstract::Behavioural evidence has accumulated that supports the hypothesis that specific territories of the striatum contribute differentially to the control of motor behaviours. The present experiments compare the behavioural effects of microinjections of amphetamine (20 microg/0.5 microl) with those elicited by the D2-class ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00752-3
更新日期:1998-12-04 00:00:00
abstract::1-(Meta-chloro)phenylpiperazine (m-CPP) is a 5-HT receptor agonist which has been purported to be relatively selective for the 5-HT2C receptor. In particular, the hypolocomotion produced by m-CPP has been suggested to be mediated by 5-HT2C receptors. m-CPP binds with high affinity to 5-HT1 as well as 5-HT2 receptors, ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01474-x
更新日期:1998-01-12 00:00:00
abstract::The nicotinic acetylcholine receptors in the rat stomach were characterized by means of a radioligand binding assay with (-)-[3H]nicotine as ligand. Saturation binding studies on the gastric fundus membranes revealed the presence of two binding sites with dissociation constant (KD) values of 3.1 and 289 nM, and maximu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90490-6
更新日期:1988-01-27 00:00:00
abstract::Dopamine hyperpolarizes growth hormone-producing cells (GHC) in the CNS of Lymnaea stagnalis. This effect of dopamine was mimicked by the D-2 receptor agonist LY 141865 and antagonized by the D-2 receptor antagonists (-)-sulpiride and YM 09151-2. SKF 38393, a selective D-1 receptor agonist, increased the excitability ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90735-0
更新日期:1984-11-13 00:00:00
abstract::The neuronal nicotinic acetylcholine receptor alpha4 and beta2 subunits expressed in heterologous expression systems assemble into at least two distinct subunit stoichiometries of alpha4beta2 receptor. The (alpha4)2(beta2)3 stoichiometry is about 100-fold more sensitive to acetylcholine than the (alpha4)3(beta2)2 stoi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.03.077
更新日期:2006-06-06 00:00:00
abstract::Current clinical options for the treatment of neovascular disorders of the posterior segment of the eye have several drawbacks. Photocoagulation lasers can impair peripheral and night vision. Photodynamic therapies as well as intravitreal macromolecule injections (Macugen and Lucentis) require frequent, invasive admin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.04.044
更新日期:2007-07-30 00:00:00
abstract::The effect and role of nitric oxide (NO) in the regulation of ion transport in the mouse cecum were investigated. L-arginine, used to increase NO production, increased short-circuit current (Isc), a measure of ion transport, in a concentration-dependent manner with a maximal increase of 193.8+/-65.5 microA/cm2. This i...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00221-0
更新日期:1998-05-29 00:00:00
abstract::WIN 64338 (phosphonium, [[4-[[2-[[bis(cyclohexylamino) methylene] amino]-3-(2-naphthalenyl) 1-oxopropyl]amino]-phenyl]- tributyl, chloride, monohydrochloride) is the first potent nonpeptide competitive bradykinin B2 receptor antagonist as shown in classical pharmacological preparations with no activity in the rabbit a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(94)90017-5
更新日期:1994-12-15 00:00:00
abstract::Cisplatin (CDDP)-induced nephrotoxicity (CIN) is one of the most serious toxicities caused by this potent antitumor agent. It has been reported that Mg premedication attenuates CIN in clinical trials; however, the mechanism underlying its nephroprotection is not fully understood. Therefore, the aim of this study was t...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2017.05.034
更新日期:2017-09-15 00:00:00
abstract::The effects of acute chronic administration of tricyclic antidepressants on the pituitary-adrenal axis were studied in adult male rats. Acute administration of desipramine, imipramine and chlorimipramine activated the pituitary-adrenal axis. The effect of imipramine was found to be of short duration with a significant...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90812-0
更新日期:1987-08-11 00:00:00
abstract::Glycine displaces [3H]CGP-39653 ([3H]D,L-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid) binding to the glutamate recognition site with both high and low affinity. We reported previously that chronic treatment with antidepressants reduced the proportion of high to low affinity sites, or, even eliminated the high af...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01589-6
更新日期:1998-01-26 00:00:00
abstract::The pharmacological effects of Neuropeptide FF (NPFF) analogs exhibiting different selectivities towards Neuropeptide FF1 (NPFF1) and Neuropeptide FF2 (NPFF2) receptors were investigated after supraspinal administration in mice. Injected into the third ventricle, VPNLPQRF-NH2, which is selective for Neuropeptide FF1 r...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.12.002
更新日期:2005-01-31 00:00:00
abstract::A very strong epidemiological link exists between obesity, the metabolic syndrome, diabetes and diabetes-associated cardiovascular pathologies. For this reason the peripheral effects of the centrally-acting satiety adipokines, adiponectin and leptin, and of non-adipose-derived hormones with similar effects, like ghrel...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.11.052
更新日期:2007-03-08 00:00:00
abstract::Bay k-8644 (methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoro- methylphenyl)-pyridine-5-carboxylate) (a Ca2+ channel agonist of the dihydropyridine class) at 5 mg/kg (s.c.) impaired the anticonvulsant activities of two competitive NMDA receptor antagonists, CGP 37849 (D,L-(E)-2-amino-4-methyl-5-phosphono-3-penten...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90644-0
更新日期:1994-10-13 00:00:00
abstract::In this study, the anti-inflammatory effects of flavonoids isolated from the roots of Glycyrrhiza uralensis (Leguminosae), namely, isoliquiritin (the glycoside of isoliquirigenin) and isoliquiritigenin (the aglycone of isoliquiritin) were evaluated on lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Isoliquirit...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.01.032
更新日期:2008-04-14 00:00:00