Abstract:
:The affinity and intrinsic activity of dopamine receptor agonists were determined at the human dopamine hD21 and hD4.4 receptors. (-)-3-Hydroxy-N-n-propylpiperidine ((-)3-PPP) had an intrinsic activity of 46% and 83%, whereas (+)-N-propylnorapomorphine ((+)-NPA) had intrinsic activities of 61% and 58% at the dopamine hD21 and hD4.4 receptors, respectively. Affinities also varied. A single, or multiple, dopamine D2-type receptor(s) may be involved in schizophrenia and agonists are being tested as therapy. Understanding their properties at the individual dopamine D2-family receptors is important.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Lahti RA,Mutin A,Cochrane EV,Tepper PG,Dijkstra D,Wikström H,Tamminga CAdoi
10.1016/0014-2999(96)00127-6subject
Has Abstractpub_date
1996-04-22 00:00:00pages
R11-3issue
1-3eissn
0014-2999issn
1879-0712pii
0014-2999(96)00127-6journal_volume
301pub_type
杂志文章abstract::The Kd values of the multiple agonist binding sites in cardiac muscarinic receptors (mAChR) and pD2 values for negative inotropic actions were determined independently and their relation was examined. The guinea-pig cardiac mAChR is known to have three agonist binding sites (super-high (SH), high (H) and low (L) affin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(85)90293-6
更新日期:1985-12-17 00:00:00
abstract::Several recent reports have demonstrated a role for selective cannabinoid CB2 receptor agonists in pain modulation, showing both analgesic and antihyperalgesic activities. While the mechanism of action is poorly understood, it has been postulated that these effects may be indirect, involving release of endogenous opio...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.10.043
更新日期:2005-12-28 00:00:00
abstract::It has been shown that inflammation of rat paws elicits accumulation of opioid peptide beta-endorphin-containing immune cells in the inflamed subcutaneous tissue, contributing to immunocyte-produced pain suppression. However, the possible mechanisms involved in the pharmacological application of beta-endorphin in rat ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.08.012
更新日期:2006-11-07 00:00:00
abstract::The response of lymph vessels, arterioles and venules in the exteriorized rat mesentery to endothelin-1, vasopressin and norepinephrine was examined with the aid of high-resolution television microscopy. On a molar basis, endothelin-1 was more potent than vasopressin to contract the three types of vessels. Norepinephr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90135-0
更新日期:1989-10-24 00:00:00
abstract::The effects of riluzole, an anticonvulsant and neuroprotective compound, on excitatory amino acid-evoked currents were studied in Xenopus laevis oocytes injected with mRNA from rat whole brain or cortex. Responses to kainic acid were blocked by riluzole (IC50 = 167 microM) as well as by the quinoxalinedione antagonist...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90147-a
更新日期:1993-04-28 00:00:00
abstract::To date, 5-hydroxytryptamine1A (5-HT1A) receptor-mediated functional assays (adenylyl cyclase inhibition, high-affinity GTPase activity and [35S]guanosine-5'-O-(gamma-thio)-triphosphate ([35S]GTPgammaS) binding) have been performed mainly in hippocampal membranes. In the current study, 5-HT-stimulated G protein activa...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.07.018
更新日期:2005-10-03 00:00:00
abstract::Obese mice display overactive bladder (OAB) associated with impaired urethra smooth muscle (USM) function. In this study, we evaluated the role of the adipose tissue surrounding the urethra and prostate in obese mice (here referred as periprostatic adipose tissue; PPAT) to the USM dysfunction. Male C57BL6/JUnib mice f...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.08.010
更新日期:2018-10-05 00:00:00
abstract::Antiarrhythmic drugs have been considered to be transported by the organic cation transport system. The purpose of this study was to elucidate the molecular mechanism underlying the transport of antiarrhythmic drugs using cells from the second segment of the proximal tubule (S2) cells of mice expressing human-organic ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.07.098
更新日期:2004-09-19 00:00:00
abstract::Drugs belonging to different chemical classes having the ability to improve behavioral performance in animal learning and memory tests may share the common ability to stimulate protein kinase C activity in rat brain cortex. In vitro acetyl-L-carnitine (100 nM) promoted in rat brain cortex slices a significant increase...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90216-x
更新日期:1994-11-14 00:00:00
abstract::The effects of 2-methylthio ATP, an ATP analogue that is more specific for the P2Y receptor, were investigated on insulin secretion in the anesthetized dog in vivo. 2-Methylthio ATP was infused directly into the pancreaticoduodenal artery for 15 min. The infusion was performed so as to obtain a pancreaticoduodenal art...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(88)90418-9
更新日期:1988-10-11 00:00:00
abstract::Chronic lithium treatment was examined for effects on the blood pressure of spontaneously hypertensive rats (SHRs). Treated rats were allowed continuous access to a pelleted lithium diet (1.7 g LiCl (40 mmol)/kg diet) for 21 days. Control SHRs were fed a similar diet lacking the lithium. Two groups of control rats wer...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90112-6
更新日期:1981-12-17 00:00:00
abstract::Ionic currents and contraction were recorded under voltage clamp conditions in single fibres isolated from rat soleus muscles denervated for more than 20 days. The effects of amphiphiles on depolarization-contraction (d.c.) coupling in Na-free TEA-containing solutions were analyzed. An anionic amphiphile, sodium dodec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90878-9
更新日期:1989-12-12 00:00:00
abstract::The effects of group 2- versus group 3-selective metabotropic glutamate (mGlu) receptor agonists were examined against forskolin (10 microM)-, vasoactive intestinal peptide (VIP; 1 microM)- and 5'-N-ethylcarboxamidoadenosine (NECA; 10 microM)-stimulated cAMP accumulations in adult rat hippocampal slices (in the presen...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00747-4
更新日期:1996-02-22 00:00:00
abstract::In vivo microdialysis was used to study the effects of the locally applied GABA B receptor antagonist 2-hydroxysaclofen and GABA B receptor agonist baclofen on the basal dopamine efflux as well as on the endomorphin-1- and endomorphin-2-induced dopamine efflux in the nucleus accumbens of freely moving rats. 2-Hydroxys...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.12.008
更新日期:2008-03-10 00:00:00
abstract::Estrogen-related receptor alpha (ERRα), one of orphan nuclear receptors, has been recently revealed as an oncogenic regulator in a variety of cancers. However, the linking gain of ERRα expression and cancer progression in cutaneous squamous cell carcinoma (cSCC) is largely unknown. Here, we showed that the mRNA and pr...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2018.02.025
更新日期:2018-04-15 00:00:00
abstract::Previous studies have shown that treatment of guinea-pig isolated vas deferens with the affinity label periodate-oxidized ATP (2',3'-dialdehyde ATP), results in two irreversible effects on biphasic contractile responses to ATP, i.e., potentiation of the P2X purinoceptor-mediated first phase and inhibition of the ecto-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00352-l
更新日期:1995-08-04 00:00:00
abstract::To determine the role of protein kinase C in the regulation of intestinal fluid transport, experiments were performed with the rat jejunum in vivo, using the active phorbol ester, 4-beta-phorbol 12-myristate 13-acetate (PMA), as stimulator of protein kinase C. Intraluminally administered PMA dose dependently reversed ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90053-9
更新日期:1990-07-17 00:00:00
abstract::The loss of cholinergic neurons and synapses relates to the severity of dementia in several neurodegenerative pathologies; and the vesicular acetylcholine transporter (VAChT) provides a reliable biomarker of cholinergic function. We recently characterized and (11)C-labeled a new VAChT inhibitor, (-)-TZ659. Here we rep...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2015.02.001
更新日期:2015-04-05 00:00:00
abstract::The objective of this study was to determine the in vivo effectiveness of the selective endothelin ETA receptor antagonist PD 156707 (sodium 2-benzo[1,3]dioxol-5-yl-4-(4-methoxy-phenyl)-4-oxo-3-(3,4,5-trimet hoxy- benzyl)-but-2-enoate). Effectiveness was defined by the ability of the compound to block increases in ren...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00954-5
更新日期:1997-03-05 00:00:00
abstract::The role of dopamine transmission on striatal acetylcholine release was investigated by using brain microdialysis. Blockade of dopamine D2 receptors with (-)-sulpiride or haloperidol increased acetylcholine release to a maximum of 80% (after 50 and 0.5 mg/kg, respectively). This effect was prevented by blockade of dop...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)90409-x
更新日期:1994-01-14 00:00:00
abstract::alpha-Adrenoceptors have been classified into alpha(1)- and alpha(2)-adrenoceptors. Recently, the alpha(1)-adrenoceptors were divided into two subtypes: alpha(1L) with low affinity and alpha(1H) with high affinity for prazosin. Little is known concerning the role of each subtype of alpha(1)-adrenoceptor in asthma. We ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)02248-3
更新日期:2002-09-27 00:00:00
abstract::The effect of water immersion stress on the plasma concentration of histamine, in Wistar and mast cell-deficient (Ws/Ws) rats, was investigated. The histamine content of the plasma, skin and gastric mucosa, as well as the level of activity of histidine decarboxylase in the gastric mucosa, were determined by high perfo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00670-0
更新日期:1998-11-06 00:00:00
abstract::Oxidative stress plays an important role in inflammatory process of celiac disease. We have studied the effect of the lycopene, quercetin and tyrosol natural antioxidants on the inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) gene expression in RAW 264.7 macrophages stimulated by gliadin in associa...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2007.03.051
更新日期:2007-07-02 00:00:00
abstract::Apelin, a ligand for apelin-angiotension receptor-like 1 (APJ), has recently been shown to be a potent positive inotropic agent in normal hearts. In humans, levels of apelin have been shown to rise in early-stage heart failure and to fall in late-stage heart failure. In this study, we tested the hypothesis that apelin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.09.034
更新日期:2006-12-28 00:00:00
abstract::Diabetes mellitus is associated with an increased risk of cardiovascular disease. Endothelial dysfunction (i.e. decreased endothelium-dependent vasorelaxation) plays a key role in the pathogenesis of diabetic vascular disease. The present study was undertaken to determine whether diabetes induced by streptozotocin alt...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.01.063
更新日期:2006-03-27 00:00:00
abstract::Since estrogen and selective estrogen receptor modulators can inhibit inflammatory responses, we studied the regulatory role of several selective estrogen receptor modulators on interleukin-6 (IL-6) expression in human retinal pigment epithelial cells (ARPE-19). ARPE-19 cells were exposed to lipopolysaccharide with si...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.05.006
更新日期:2010-08-25 00:00:00
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 benz...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)90153-u
更新日期:1992-07-21 00:00:00
abstract::We examined the effects of YM-31636 (2-(1H-imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole monofumarate), a novel 5-HT3 receptor agonist, on gastrointestinal functions including visceral pain reflex in rats. Injection of YM-31636 increased the number of fecal pellets. This effect was completely inhibited by ramosetron, ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)01425-x
更新日期:2001-11-09 00:00:00
abstract::Histone deacetylases (HDACs) can regulate cancer progression and its inhibitors (HDACIs) have been widely used for cancer therapy. Valproic acid (VPA, 2-propylpentanoic acid) can inhibit the class I HDAC and suppress the malignancy of solid cancers. Our present study revealed that 1 mM VPA, which has no effect on cell...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2019.172745
更新日期:2019-12-15 00:00:00
abstract::The effects of the alpha-agonists clonidine and guanfacine on rat cortical norepinephrine turnover during morphine withdrawal were assessed. Cortical norepinephrine levels were measured, after administration of alpha-methyl-p-tyrosine, by fluorometric assay. Chronic treatment with morphine did not affect norepinephrin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90368-x
更新日期:1981-04-09 00:00:00