The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor.

Abstract:

:The dopamine D4 receptor is a potential target for novel antipsychotic drugs. Most available compounds with affinity for the dopamine D4 receptor also bind to dopamine D2 receptors. This report describe the affinity of the 5-HT2A receptor antagonist RP 62203 (fananserin) for the human dopamine D4 receptor. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D4 receptors with a Ki of 2.93 nM. This compares with an affinity (Ki) of 0.37 nM for the rat 5-HT2A receptor and of 726 mM for the rat dopamine D2 receptor. [3H]Fananserin can be used to label the recombinant dopamine D4 receptor expressed in Chinese hamster ovary cells with a KD of 0.725 nM. Fananserin is, thus, the first compound to be reported that distinguishes between dopamine D4 and D2 receptors.

journal_name

Eur J Pharmacol

authors

Heuillet E,Petitet F,Mignani S,Malleron JL,Lavayre J,Néliat G,Doble A,Blanchard JC

doi

10.1016/s0014-2999(96)00554-7

subject

Has Abstract

pub_date

1996-10-24 00:00:00

pages

229-33

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(96)00554-7

journal_volume

314

pub_type

杂志文章
  • Interference of the PAF receptor antagonist, PCA 4248, with the rat pleurisy evoked by inflammatory mediators or allergen.

    abstract::This study investigated the effect of the platelet-activating factor (PAF) receptor antagonist, PCA 4248, on the rat pleurisy caused by PAF, serotonin, bradykinin, histamine or allergen. The pleurisy was assessed by measuring liquid extravasation and leucocyte infiltration. Oral pretreatment with PCA 4248 (2.5-20 mg/k...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90087-x

    authors: Martins MA,Lima MC,Bozza PT,Faria Neto HC,Silva PM,Sunkel CE,Cordeiro RS

    更新日期:1993-06-11 00:00:00

  • Inositol phosphates formed in rat aorta after alpha 1-adrenoceptor stimulation are inhibited by forskolin.

    abstract::Rat aortic smooth muscle rings without endothelial cells were subjected to alpha 1-adrenoceptor stimulation. We measured the contractile state of the smooth muscle cells and the formation of inositol phosphates (InsPs) on receptor stimulation. Using different extracellular calcium-containing solutions (2.5 mM, 0.1 mM ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0922-4106(05)80034-3

    authors: Manolopoulos VG,Pipili-Synetos E,Den Hertog A,Nelemans A

    更新日期:1991-05-25 00:00:00

  • The dipeptidyl peptidase IV (CD26, EC 3.4.14.5) inhibitor vildagliptin is a potent antihyperalgesic in rats by promoting endomorphin-2 generation in the spinal cord.

    abstract::We have reported previously that the dipeptidyl peptidase IV inhibitor Ile-Pro-Ile had an antihyperalgesic action in rats when given intrathecally in the carrageenan-induced hyperalgesia, as detected by the Randall-Selitto test. Vildagliptin, a non-peptide inhibitor of the same enzyme, which is already on the market a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.09.060

    authors: Király K,Lambeir AM,Szalai J,Szentirmay A,Luyten W,Barna I,Puskár Z,Kozsurek M,Rónai AZ

    更新日期:2011-01-10 00:00:00

  • Tachykinin NK(2) receptor mediates contraction and ion transport in rat colon by different mechanisms.

    abstract::We have characterized the tachykinin NK(2) receptor-mediated contraction and vectorial ion transport responses in the muscularis mucosae and mucosa of the rat isolated distal colon, respectively. The tachykinin NK(2) receptor-selective antagonist nepadutant (c([(beta-D-GlcNAc)Asn-Asp-Trp-Phe-Dpr-Leu]c(2beta-5beta))) p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(01)00836-6

    authors: Patacchini R,Cox HM,Ståhl S,Tough IR,Maggi CA

    更新日期:2001-03-01 00:00:00

  • Antagonism of pentobarbital-induced hormonal changes by TRH in rats.

    abstract::In adult male rats, injection of TRH into a lateral ventricle of the brain 5 min prior to pentobarbital (PB) administration caused a significant dose-related inhibition of prolactin (PRL) release, in doses ranging from 500 to 5 ng. Among 8 TRH analogues devoid of thyrotropin-releasing activity, 6 were found to signifi...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90276-x

    authors: Taché Y,Ruisseau PD,Ducharme JR,Collu R

    更新日期:1977-10-15 00:00:00

  • Spinal antinociceptive effects of AA501, a novel chimeric peptide with opioid receptor agonist and tachykinin receptor antagonist moieties.

    abstract::The use of "multimodal" combination analgesic therapies or novel single molecules possessing multiple analgesic targets is becoming increasingly attractive. In previous experiments we showed that a substance P antagonist injected intrathecally potentiated the antinociceptive effects of potent opioid receptor agonist, ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2004.02.023

    authors: Bonney IM,Foran SE,Marchand JE,Lipkowski AW,Carr DB

    更新日期:2004-03-19 00:00:00

  • A novel TLR4-binding peptide that inhibits LPS-induced activation of NF-kappaB and in vivo toxicity.

    abstract::Lipopolysaccharide (LPS) is a component of the outer membrane of Gram-negative bacteria. It is a ligand for Toll-like receptor 4 (TLR4), which plays an essential role in innate immunity. Macrophages and dendritic cells exposed to LPS overproduce proinflammatory mediators, leading to septic shock. In this study, we scr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.07.037

    authors: Sugiyama K,Muroi M,Tanamoto K

    更新日期:2008-10-10 00:00:00

  • In vitro profile of the antidepressant candidate OPC-14523 at rat and human 5-HT1A receptors.

    abstract::This study determined the in vitro functional profile of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate (OPC-14523) at rat and human serotonin (5-HT) 5-HT1A receptors and binding affinity of OPC-14523 at human frontocortical 5-HT1A receptors. OPC-14523 (1 microM...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.05.035

    authors: Jordan S,Chen R,Koprivica V,Hamilton R,Whitehead RE,Tottori K,Kikuchi T

    更新日期:2005-07-11 00:00:00

  • Intrathecal Raf-1-selective siRNA attenuates sustained morphine-mediated thermal hyperalgesia.

    abstract::Studies have demonstrated that long-term opioid treatment leads to an increased sensitivity to painful (hyperalgesia) or normally innocuous (allodynia) stimuli. The molecular mechanisms that lead to paradoxical pain sensitization upon chronic opioid treatment are not completely understood. Enhanced excitatory pain neu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2008.10.033

    authors: Tumati S,Milnes TL,Yamamura HI,Vanderah TW,Roeske WR,Varga EV

    更新日期:2008-12-28 00:00:00

  • Binding of the muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide at cholinoceptor sites.

    abstract::The binding of the bisquaternary muscarine receptor antagonist heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)-ammonium bromide (C7/3-phth) was investigated at a number of cholinergic binding sites using (-)-[3H]nicotine, [3H]pirenzepine and (-)-[3H]quinuclidinyl benzilate ([3H]QNB) in both central and peripheral tissu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90002-q

    authors: Christopoulos A,Loiacono R,Mitchelson F

    更新日期:1993-06-15 00:00:00

  • Reduction of renal lipid content and proteinuria by a PPAR-γ agonist in a rat model of angiotensin II-induced hypertension.

    abstract::An excess of lipids may accumulate in the kidney in conditions such as diabetes and hypertension, and can potentially cause renal injury. We previously reported that an infusion of angiotensin II into a rat induced deposition of lipids in the renal tubular epithelial cells. Here we have examined the effect of pioglita...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.02.027

    authors: Sakamoto A,Hongo M,Saito K,Nagai R,Ishizaka N

    更新日期:2012-05-05 00:00:00

  • Inhibition of synaptosomal [3H]noradrenaline uptake by beta-adrenoceptor blocking drugs: influence of lipophilicity.

    abstract::Ten beta-adrenoceptor blocking drugs varying in lipophilicity and beta-adrenoceptor blocking potency were examined for inhibitory effects on synaptosomal [3H]noradrenaline uptake. All compounds produced a concentration-dependent inhibition of noradrenaline uptake, but were at least one order of magnitude less potent t...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90263-2

    authors: Street JA,Walsh A

    更新日期:1984-07-13 00:00:00

  • Presynaptic inhibition by clonidine of neurotransmitter amino acid release in various brain regions.

    abstract::The release of endogenous aspartic acid (Asp), glutamic acid (Glu) and gamma-aminobutyric acid (GABA) was investigated in synaptosomes prepared from various regions of the rat brain. The basal release of Asp, Glu and GABA from various regions was 12-35, 24-107 and 15-43 pmol/min per mg protein, respectively. Exposure ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90511-2

    authors: Kamisaki Y,Hamahashi T,Hamada T,Maeda K,Itoh T

    更新日期:1992-06-24 00:00:00

  • Acute delta 9-tetrahydrocannabinol exposure alters Ca2+ ATPase activity in neuroendocrine and gonadal tissues in mice.

    abstract::Acute administration of delta 9-tetrahydrocannabinol (THC) (50 mg/kg) at puberty (35-40 days) significantly (P less than 0.05) reduced Ca2+ ATPase activity in hypothalamic plasma membranes but increased, although not significantly, enzyme activity in hypothalamic tissue obtained from adult mice. In contrast, testicula...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90186-5

    authors: Dalterio SL,Bernard SA,Esquivel CR

    更新日期:1987-05-07 00:00:00

  • SP600125 blocks the proteolysis of cytoskeletal proteins in apoptosis induced by gas signaling molecule (NO) via decreasing the activation of caspase-3 in rabbit chondrocytes.

    abstract::NO plays a key role in the pathological mechanisms of articular diseases. As cytoskeletal proteins are responsible for the polymerization, stabilization, and dynamics of the cytoskeleton network, we investigated whether cytoskeletal proteins are the intracellular pathological targets of NO. We aimed at clarifying whet...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.01.032

    authors: Kao XB,Chen Q,Gao Y,Fan P,Chen JH,Wang ZL,Wang YQ,Chen YN,Yan YP

    更新日期:2018-04-05 00:00:00

  • Anxiolytic activity on locus coeruleus-mediated suppression of muricidal aggression.

    abstract::The evidence suggests that stimulation of brain noradrenergic neurons plays an inhibitory role in rat mouse-killing (muricidal) aggression. Anxiolytic benzodiazepines inhibit locus coeruleus activity and previous data showed that chlordiazepoxide was capable of antagonizing the locus coeruleus-mediated suppression of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90625-3

    authors: Kozak W,Valzelli L,Garattini S

    更新日期:1984-10-15 00:00:00

  • Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys.

    abstract::Inhibition of local cortisol regeneration from circulating cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the risk factors associated with the metabolic syndrome. Chronic modulation of glucocorticoid homeostasis may result in hypothalamic-pituitary-adrenal (HPA) axis s...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.07.004

    authors: Hamilton BS,Schoelch C,Schuler-Metz A,Krosky P,Lala DS,Claremon DA,McGeehan GM

    更新日期:2016-10-15 00:00:00

  • Use of decorin to prevent epidural fibrosis in a post-laminectomy rat model.

    abstract::The formation of epidural fibrosis adjacent to the dura mater is a complex multi-step process that is associated with a marked reduction in tissue cellularity and the excessive deposition of extracellular matrix components. Extensive epidural fibrosis is a major cause of post-laminectomy syndrome. Decorin strongly inh...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2013.12.017

    authors: Turkoglu E,Dinc C,Tuncer C,Oktay M,Serbes G,Sekerci Z

    更新日期:2014-02-05 00:00:00

  • Effects of systemic treatment with irbesartan and losartan on central responses to angiotensin II in conscious, normotensive rats.

    abstract::Angiotensin AT1 receptor antagonists represent a novel class of cardiovascular drugs. In conscious, normotensive rats, irbesartan ((2-n-butyl-3-[(2'-(1H-tetrazol-5-yl)-biphenyl-4-yl) methyl]-1,3-diaza-spiro[4,4]non) and losartan ((2 n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl -4-yl) methyl] imid...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(98)00983-2

    authors: Culman J,von Heyer C,Piepenburg B,Rascher W,Unger T

    更新日期:1999-02-19 00:00:00

  • Silibinin ameliorates diabetic nephropathy via improving diabetic condition in the mice.

    abstract::Diabetic nephropathy (DN) is a major cause of end-stage renal disease and one of the most severe diabetic complications. However, there is lack of effective treatments for DN and the underlying mechanisms of the renal injury remain unclear. In current study, we evaluated the effects of silibinin on DN and further expl...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2018.12.031

    authors: Liu Y,Ye J,Cao Y,Zhang R,Wang Y,Zhang S,Dai W,Ye S

    更新日期:2019-02-15 00:00:00

  • Monoamine reuptake site occupancy of sibutramine: Relationship to antidepressant-like and thermogenic effects in rats.

    abstract::Sibutramine was formerly marketed as an anti-obesity agent. The current study investigated the relationships between monoamine reuptake site occupancy for sibutramine and both its antidepressant-like efficacy and thermogenic effects. Sibutramine's effects on locomotor activity (LMA) and food intake were also evaluated...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.03.024

    authors: Li YW,Langdon S,Pieschl R,Strong T,Wright RN,Rohrbach K,Lelas S,Lodge NJ

    更新日期:2014-08-15 00:00:00

  • Homovanillic acid in caudate and pre-frontal cortex following neuroleptics.

    abstract::Homovanillic acid (HVA) was measured in rat caudate and pre-frontal cortex 3 h following a single dose of a variety of neuroleptics. Thioridazine, haloperidol, fluphenazine, and metoclopramide increased HVA levels in caudate more than in pre-frontal cortex; whereas sulpiride and clozapine produced greater increases in...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(84)90438-2

    authors: Bowers MB Jr

    更新日期:1984-03-16 00:00:00

  • Picrotoxin changes the effects of imipramine and desipramine in rats in the forced swimming test.

    abstract::The aim was to find whether the chloride channel blocker, picrotoxin, at subconvulsant doses could affect the activity of imipramine or desipramine in the 'forced swimming' test with rats. It was found that picrotoxin enhanced the anti-immobility effects of imipramine and desipramine whereas open field activity remain...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90242-x

    authors: Fernández-Teruel A,Escorihuela RM,Boix F,Tobeña A

    更新日期:1990-05-31 00:00:00

  • Acute inhibition of glutathione biosynthesis alters endothelial function and blood pressure in rats.

    abstract::The cardiovascular and biochemical responses during acute oxidative stress induced by D,L-buthionine-(S,R)-sulfoximine (BSO) were investigated in Sprague-Dawley rats. Mean arterial pressure, heart rate and vascular reactivity were measured after subcutaneous injection of BSO (4 mmol/kg). Control rats received saline. ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02500-1

    authors: Ganafa AA,Socci RR,Eatman D,Silvestrova N,Abukhalaf IK,Bayorh MA

    更新日期:2002-11-15 00:00:00

  • Decreased peripheral benzodiazepine binding sites in platelets of neuroleptic-treated schizophrenics.

    abstract::A decrease of 30% was observed in the density of peripheral-type benzodiazepine binding sites in platelets of nine schizophrenics maintained on chronic neuroleptic treatment as compared to platelets of six untreated schizophrenics and 15 healthy volunteers. The equilibrium dissociation constant for binding by [3H]PK 1...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(86)90500-5

    authors: Gavish M,Weizman A,Karp L,Tyano S,Tanne Z

    更新日期:1986-02-18 00:00:00

  • The "low-dose" concept and the paradoxical effects of prolactin on grooming and sexual behavior.

    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

    authors: Drago F,Lissandrello CO

    更新日期:2000-09-29 00:00:00

  • Effects of 3-aminobenzamide, an inhibitor of poly (ADP-ribose) polymerase, in a mouse model of acute pancreatitis induced by cerulein.

    abstract::Poly (ADP-ribose) polymerase (PARP), a nuclear enzyme activated by strand breaks in DNA, plays an important role in the colon injury associated with experimental colitis. The aim of the present study was to examine the effects of 3-aminobenzamide (3-AB), an inhibitor of PARP activity, in the development of acute pancr...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2006.08.008

    authors: Mazzon E,Genovese T,Di Paola R,Muià C,Crisafulli C,Malleo G,Esposito E,Meli R,Sessa E,Cuzzocrea S

    更新日期:2006-11-07 00:00:00

  • Analgesic effect of thalidomide on inflammatory pain.

    abstract::Tumor necrosis factor alpha (TNF-alpha) may have a pivotal role in the genesis of mechanical inflammatory hyperalgesia in rats and in the nociceptive writhing response in mice. Thalidomide has been shown to selectively inhibit TNF-alpha production. We therefore investigated the effect of thalidomide on these responses...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(99)00918-8

    authors: Ribeiro RA,Vale ML,Ferreira SH,Cunha FQ

    更新日期:2000-03-10 00:00:00

  • Evidence for a physiological role of endocannabinoids in the modulation of seizure threshold and severity.

    abstract::The anticonvulsant effect of cannabinoids has been shown to be mediated through activation of the cannabinoid CB(1) receptor. This study was initiated to evaluate the effects of endogenously occurring cannabinoids (endocannabinoids) on seizure severity and threshold. The anticonvulsant effect of the endocannabinoid, a...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(02)02331-2

    authors: Wallace MJ,Martin BR,DeLorenzo RJ

    更新日期:2002-10-11 00:00:00

  • Ginkgolide B, a constituent of Ginkgo biloba, facilitates glutamate exocytosis from rat hippocampal nerve terminals.

    abstract::Although previous studies have demonstrated that Ginkgo biloba extract has modest effects in the improvement of memory and cognitive function of the Alzheimer's disease patients, the mechanism(s) underlying its beneficial effects remain(s) unclear. In this study, the effect of ginkgolide B, one of the major constituen...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.03.027

    authors: Wang SJ,Chen HH

    更新日期:2005-05-09 00:00:00