Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.

abstract：:We have eliminated putative palmitoylation sites in the carboxyl tail of the human dopamine D1 receptor by replacing the two cysteine residues with alanines either separately or together. The wild type and the three mutated dopamine D1 receptors were stably expressed in baby hamster kidney cells and characterized to d...

journal_title：European journal of pharmacology

authors： Jin H,Zastawny R,George SR,O'Dowd BF

更新日期：1997-04-11 00:00:00

abstract：:Affinity cross-linking of the bradykinin B2 receptor was performed using [125I-Tyr8]bradykinin, disulfosuccinimidyl tartrate as linker and crude membranes from guinea pig ileum smooth muscle immobilized on Whatman GF/B glass fiber filters. After SDS (sodium dodecylsulfate)-polyacrylamide gel electrophoresis under redu...

journal_title：European journal of pharmacology

authors： Graness A,Liebmann C

更新日期：1994-07-15 00:00:00

abstract：:The present study was conducted with an aim to explore the possible role of naringin against ischemia reperfusion induced-neurobehavioral alterations, oxidative damage, cellular and histopathological alterations in cortex, striatum, hippocampus areas of brain. Male Wistar rats (200-220 g) were subjected to bilateral c...

journal_title：European journal of pharmacology

authors： Gaur V,Aggarwal A,Kumar A

更新日期：2009-08-15 00:00:00

abstract：:We have shown that the major active agent of Cannabis sativa, Delta(9)-tetrahydrocannabinol, activates peroxisome proliferator-activated receptor gamma [PPARgamma, O'Sullivan, S.E., Tarling, E.J., Bennett, A.J., Kendall, D.A., Randall, M.D., 2005c. Novel time-dependent vascular actions of delta9-tetrahydrocannabinol m...

journal_title：European journal of pharmacology

authors： O'Sullivan SE,Sun Y,Bennett AJ,Randall MD,Kendall DA

更新日期：2009-06-10 00:00:00

abstract：:Type 1 cannabinoid (CB1) and dopamine 2 long form (D2L) receptors can physically interact to form heteromers that display unique pharmacology in vitro compared to homomeric complexes. Co-expression of CB1 and D2L and co-application of CB1 and D2 agonists increases cAMP levels while administration of either agonist alo...

journal_title：European journal of pharmacology

authors： Bagher AM,Laprairie RB,Toguri JT,Kelly MEM,Denovan-Wright EM

更新日期：2017-10-15 00:00:00

abstract：:Saturable, high-affinity binding sites for [3H]saxitoxin were identified in equine portal vein smooth muscle membranes. These sites had a dissociation constant of 0.29 nM and a maximal binding capacity of 115 fmol.mg-1 of protein. A similar dissociation constant was obtained with cells prepared from rat portal vein. S...

journal_title：European journal of pharmacology

authors： Mironneau J,Martin C,Arnaudeau S,Jmari K,Rakotoarisoa L,Sayet I,Mironneau C

更新日期：1990-08-10 00:00:00

abstract：:Barbiturates and the related depressant drugs, etazolate and etomidate, inhibited both the binding of [3H]bicuculline methochloride (BMC) to gamma-aminobutyric acid (GABA) receptor sites and the binding of [3H] beta-carboline-3-carboxylic acid methyl ester (beta CCM) to benzodiazepine receptor sites in mammalian brain...

journal_title：European journal of pharmacology

authors： Wong EH,Snowman AM,Leeb-Lundberg LM,Olsen RW

更新日期：1984-07-13 00:00:00

abstract：:We investigated the endothelin production and endothelin receptor activity of pericardial mesothelial cells obtained from spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats. The pericardial mesothelial cells were maintained in vitro and the production of endothelin-1 by these cells was evaluated by usin...

journal_title：European journal of pharmacology

authors： Kuwahara M,Kuwahara M

更新日期：1998-04-24 00:00:00

abstract：:In the attempt to find a pharmacological treatment for the spasm of the internal anal sphincter, usually associated with anal fissures, the activity of caerulein on human internal and sphincter was investigated in vitro and in vivo. In the isolated distal part of the internal and sphincter, caerulein (0.61 microM) dep...

journal_title：European journal of pharmacology

authors： Carpenedo F,Infantino A,Floreani M,Dodi G

更新日期：1983-02-18 00:00:00

abstract：:We investigated the mechanism of action of a novel 'high ceiling' diuretic, M17055, in in vivo clearance studies with anesthetized dogs during water diuresis and in vitro microperfusion studies of isolated rabbit renal tubules. In the clearance study, intravenous infusion of M17055 (1 mg/kg per h) decreased free water...

journal_title：European journal of pharmacology

authors： Shinkawa T,Yamasaki F,Notsu T,Nakakuki M,Nishijima K,Yoshitomi K,Imai M

更新日期：1993-07-20 00:00:00

abstract：:Antidepressant activity of partial agonists at strychnine-insensitive glycine receptors, 1-aminocyclopropanecarboxylic acid (ACPC) and D-cycloserine, was studied in a chronic mild stress model of depression. In this model, a substantial decrease in consumption of a palatable sucrose solution is observed over time in r...

journal_title：European journal of pharmacology

authors： Papp M,Moryl E

更新日期：1996-12-05 00:00:00

abstract：:Grooming behaviour in mice was dose dependently increased by SK&F 38393 (1.87-30 mg/kg), whereas it was dose dependently decreased by RU 24926 (2.5-10 mg/kg) or LY 171555 (0.4-1.6 mg/kg) alone or combined with SK&F 38393 or apomorphine (0.39-6 mg/kg). The inhibitory effect of 0.75 mg/kg apomorphine on grooming behavio...

journal_title：European journal of pharmacology

authors： Vasse M,Protais P

更新日期：1988-10-26 00:00:00

abstract：:The involvement of dopamine D-1 and D-2 receptor mechanisms was investigated in the forced swimming test with rats. d,1-Sulpiride, a D-2 receptor antagonist, reported to reduce desipramine-induced anti-immobility, did not alter the brain levels of desipramine. In addition, the anti-immobility effect of desipramine was...

journal_title：European journal of pharmacology

authors： Borsini F,Lecci A,Mancinelli A,D'Aranno V,Meli A

更新日期：1988-04-13 00:00:00

abstract：:The effects of a 1,5-benzothiazepine derivative, (+)-cis-3-(acetyloxy)-5-[2-[[2-(3,4-dimethoxyphenyl)ethyl]-methyla mino]ethyl]-2,3-dihydro-2-(4-methyoxyphenyl)-1,5-benzothiazepine-4 (5H)-one (DTZ323), on membrane currents were investigated in guinea-pig ventricular myocytes using the whole-cell patch-clamp technique....

journal_title：European journal of pharmacology

authors： Kurokawa J,Adachi-Akahane S,Nagao T

更新日期：1997-05-01 00:00:00

abstract：:In 36 healthy subjects of various ages (14-76 years) the number of alpha 2-adrenergic receptors in platelets - as determined by [3H]yohimbine binding - and plasma catecholamine levels were measured. A highly significant negative correlation (r = -0.666, P less than 0.001) between the number of alpha 2-adrenergic recep...

journal_title：European journal of pharmacology

authors： Brodde OE,Anlauf M,Graben N,Bock KD

更新日期：1982-07-09 00:00:00

abstract：:The goals of the present study were: (1) to investigate the binding properties of (R)- and (S)-procyclidine and two achiral derivatives of muscarinic M1, M2 and M4 receptor subtypes and (2) to identify the interactions which allow these receptors to discriminate between the two stereoisomers. (R)-Procyclidine showed a...

journal_title：European journal of pharmacology

authors： Waelbroeck M,Camus J,Tastenoy M,Lambrecht G,Mutschler E,Tacke R,Christophe J

更新日期：1990-09-18 00:00:00

abstract：:Cocaine and a cocaine analog, WIN 36,065-2, were administered daily for 3 or 4 days. Both compounds developed sensitization to their locomotor stimulatory effects, with similarly shaped dose-response curves. Dosages giving optimal sensitization were 25 mg/kg per day for cocaine and 3 mg/kg for WIN 35,065-2. At 40 mg/k...

journal_title：European journal of pharmacology

authors： Reith ME

更新日期：1986-10-14 00:00:00

abstract：:Animal studies have shown that endogenous estrogens such as 17β-estradiol (E2) can modulate lipid profiles in vivo, and this effect is generally thought to be mediated by the estrogen receptors (ERs). The present study sought to test a hypothesis that some of the endogenous estrogen metabolites that have very weak est...

journal_title：European journal of pharmacology

authors： Wang P,Zhu BT

更新日期：2017-04-05 00:00:00

abstract：:The biological activity of two galanin (GAL) fragments, GAL-(1-16) and GAL-(17-29), was tested in vivo by using a spinal nociceptive flexor reflex model in the rat. Intrathecal (i.t.) GAL-(1-16) had a similar biphasic effect on the flexor reflex, with facilitation at lower doses and facilitation followed by depression...

journal_title：European journal of pharmacology

authors： Xu XJ,Wiesenfeld-Hallin Z,Fisone G,Bartfai T,Hökfelt T

更新日期：1990-06-21 00:00:00

abstract：:Painful diabetic neuropathy is a common complication of diabetes mellitus, which often makes the patients suffer from severe hyperalgesia and allodynia. Thus far, the treatment of painful diabetic neuropathy remains unsatisfactory. Metformin, which is the first-line drug for type-2 diabetes, has been proved to attenua...

journal_title：European journal of pharmacology

authors： Ma J,Yu H,Liu J,Chen Y,Wang Q,Xiang L

更新日期：2015-10-05 00:00:00

abstract：:Nonalcoholic steatohepatitis (NASH) is one of the most common liver diseases involving chronic accumulation of fat and inflammation, often leading to advanced fibrosis, cirrhosis and carcinoma. However, the pathological mechanism for this is unknown. GPR120/FFAR4 has been recognized as a functional fatty acid receptor...

journal_title：European journal of pharmacology

authors： Nakamoto K,Shimada K,Harada S,Morimoto Y,Hirasawa A,Tokuyama S

更新日期：2018-02-05 00:00:00

abstract：:Cultured chick hepatocytes were used to investigate the hepatotoxicity of methotrexate alone and in combination with paracetamol. Treatment with methotrexate alone at concentrations as high as 1 mg/ml resulted in no toxicity in cultured chick hepatocytes, as indicated by no detachment of cells and no effect on protein...

journal_title：European journal of pharmacology

authors： Lindenthal J,Sinclair JF,Howell S,Cargill I,Sinclair PR,Taylor T

更新日期：1993-04-01 00:00:00

abstract：:The role of central vs. peripheral actions of clonidine was investigated in the rat following the separate and combined administration of clonidine and 2-deoxy-D-glucose (2-DG). Clonidine or 2-DG alone stimulated serum glucose and corticosterone but hypothalamic noradrenaline neuronal activity and ACTH release were st...

journal_title：European journal of pharmacology

authors： Smythe GA,Bradshaw JE,Gleeson RM,Grunstein HS,Nicholson MV

更新日期：1985-05-20 00:00:00

abstract：:The open field is a very popular animal model of anxiety-like behavior. An overview of the literature on the action elicited by effective or putative anxiolytics in animal subjected to this procedure indicates that classical treatments such as benzodiazepine receptor full agonists or 5-HT(1A) receptor full or partial ...

journal_title：European journal of pharmacology

authors： Prut L,Belzung C

更新日期：2003-02-28 00:00:00

abstract：:The role of tuberoinfundibular and periventricular-hypophysial dopaminergic neurons in mediating rimcazole-induced decreases in plasma concentrations of prolactin and alpha-melanocyte stimulating hormone was assessed. Dopaminergic neuronal activity was estimated by measuring concentrations of 3,4-dihydroxyphenylacetic...

journal_title：European journal of pharmacology

authors： Eaton MJ,Lookingland KJ,Moore KE

更新日期：1996-03-28 00:00:00

abstract：:The electrophysiological effects of the putative P2-purinoceptor antagonist reactive blue 2 (RB2) were investigated in strips of circular muscle of rat caecum with the sucrose gap technique. RB2 (0.1-1 mM) antagonized in a concentration-dependent manner, the amplitude, rate of rise and speed of onset of the inhibitory...

journal_title：European journal of pharmacology

authors： Manzini S,Hoyle CH,Burnstock G

更新日期：1986-08-15 00:00:00

abstract：:The pharmacological properties of geissoschizine methyl ether, isolated from Uncaria sinensis Oliv., were analyzed in vitro and in vivo using mice central serotonin neurons. In the in vitro experiment, geissoschizine methyl ether inhibited [3H]8-hydroxy-2-(di-n-propylamino)tetralin) ([3H]8-OH-DPAT) (K(i)=0.8 microM), ...

journal_title：European journal of pharmacology

authors： Pengsuparp T,Indra B,Nakagawasai O,Tadano T,Mimaki Y,Sashida Y,Ohizumi Y,Kisara K

更新日期：2001-08-17 00:00:00

abstract：:The behavioural and electrocortical power spectrum effects of tryptoline and the 5-hydroxy and 5-methoxy derivatives were studied after microinjection of the drugs into the third cerebral ventricle in freely moving rats. The three compounds produced a dose-dependent desynchronication in electrocortical activity with a...

journal_title：European journal of pharmacology

authors： Nistico G,De Sarro GB,Langer SZ

更新日期：1987-10-06 00:00:00

abstract：:Anandamide (AEA), an endogenous cannabinoid and vanilloid receptor ligand, possesses anti-inflammatory properties. Transport of AEA through cytoplasm is facilitated by heat shock protein (HSP) Hsp70, which enhances the rate of cellular AEA uptake, possibly via direct interactions. In lungs, increased HSP expression is...

journal_title：European journal of pharmacology

authors： Kopczyńska B,Sulejczak D,Wełniak-Kamińska M,Gietka A,Grieb P

更新日期：2011-10-01 00:00:00

abstract：:The in vivo pharmacological profiles of the selective tachykinin NK1 receptor agonists, [Sar9,Met(O2)11]substance P and GR 73632, were examined in gerbils. Both agonists induced a pronounced chromodacryorrhea following intravenous injection which was stereoselectively antagonised by the tachykinin NK1 receptor antagon...

journal_title：European journal of pharmacology

authors： Bristow LJ,Young L

更新日期：1994-03-03 00:00:00