A dose ratio comparison of the interaction between morphine and cyclazocine with naloxone in rhesus monkeys on the shock titration task.

abstract：:(5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3 .2.1]octane (PTAC) is a potent muscarinic receptor ligand with high affinity for central muscarinic receptors and no or substantially less affinity for a large number of other receptors or binding sites including dopamine receptors. The ligand exhibits parti...

journal_title：European journal of pharmacology

authors： Bymaster FP,Shannon HE,Rasmussen K,Delapp NW,Mitch CH,Ward JS,Calligaro DO,Ludvigsen TS,Sheardown MJ,Olesen PH,Swedberg MD,Sauerberg P,Fink-Jensen A

更新日期：1998-09-04 00:00:00

abstract：:The anticancer drugs camptothecin (CPT) and topotecan (TPT) are known DNA topoisomerase I inhibitors which cause DNA damage and lead to cell death. In this study we provide evidence that CPT and TPT also interfere with the elements of cytoskeleton - microtubules and actin filaments which could be partly responsible fo...

journal_title：European journal of pharmacology

authors： Wang X,Tanaka M,Krstin S,Peixoto HS,Moura CCM,Wink M

更新日期：2016-10-15 00:00:00

abstract：:The effects on rat serum prolactin level of the two isomers constituting the racemic form of amisulpride were compared. (S-)-amisulpride induced hyperprolactinemia at lower doses (ED(50) = 0.09 +/- 0.01 mg/kg) than racemic- (ED(50) = 0.24 +/- 0.03 mg/kg) and (R+)-amisulpride (ED(50) = 4.13 +/- 0.05 mg/kg), in accord w...

journal_title：European journal of pharmacology

authors： Marchese G,Ruiu S,Casti P,Saba P,Gessa GL,Pani L

更新日期：2002-07-19 00:00:00

abstract：:The influence of endothelin-1 on nociception induced by capsaicin was assessed in the mouse hindpaw. Local endothelin-1 injection (1 to 20 pmol/paw) 30 min prior to ipsilateral injection of capsaicin (0.1 microg/paw) increased, in a graded fashion, the time spent licking the injected paw. Maximal hyperalgesia was obta...

journal_title：European journal of pharmacology

authors： Piovezan AP,D'Orléans-Juste P,Tonussi CR,Rae GA

更新日期：1998-06-12 00:00:00

abstract：:LK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their ra...

journal_title：European journal of pharmacology

authors： Louis SN,Nero TL,Iakovidis D,Jackman GP,Louis WJ

更新日期：1999-02-19 00:00:00

abstract：:Inactivation of gamma-aminobutric acid (GABA) as a neurotransmitter is mediated by diffusion in the synaptic cleft followed by binding to transporter sites and translocation into the intracellular compartment. The GABA transporters of which four subtypes have been cloned (GAT1-4) are distributed at presynaptic nerve e...

journal_title：European journal of pharmacology

authors： Schousboe A,Larsson OM,Sarup A,White HS

更新日期：2004-10-01 00:00:00

abstract：:Pretreatment of chick biventer cervicis preparations with ethanol (290 mM) potentiated the EC50 of choline, acetylcholine, carbachol and phenyltrimethylammonium 91%, 319%, 97% and 213%, respectively. Perhaps this interaction of ethanol and neurotransmitter could contribute to the effects on coordination and motor acti...

journal_title：European journal of pharmacology

authors： Clement JG

更新日期：1980-01-25 00:00:00

abstract：:The administration to mice of 1-methyl-4-(2'-methylphenyl)-1,2,3, 6-tetrahydropyridine (2'-CH3-MPTP), a substituted analog of the dopaminergic neurotoxin MPTP caused even more dopaminergic toxicity than MPTP itself. Under conditions in which MPTP was relatively ineffective (i.e. two injections per day of 0.113 mmol/kg...

journal_title：European journal of pharmacology

authors： Youngster SK,Duvoisin RC,Hess A,Sonsalla PK,Kindt MV,Heikkila RE

更新日期：1986-03-18 00:00:00

abstract：:As methamphetamine-induced neurotoxicity has been proposed to involve oxidative stress, reduced and oxidized glutathione (GSH and GSSG, respectively), vitamin E and ascorbate were measured in the striata of rats killed 2 or 24 h after a neurotoxic regimen of methamphetamine. At 2 h, methamphetamine increased GSH and G...

journal_title：European journal of pharmacology

authors： Harold C,Wallace T,Friedman R,Gudelsky G,Yamamoto B

更新日期：2000-07-14 00:00:00

abstract：:The in vivo bronchoconstrictor effect of tachykinins in Fisher 344 rats is accompanied by release into the airways of 5-hydroxytryptamine (5-HT). 5-HT is possibly derived from mast cells. In the present study the presumed mast cell-tachykinin interaction was studied in isolated trachea from Fisher 344 rats. Contractio...

journal_title：European journal of pharmacology

authors： Joos GF,Lefebvre RA,Bullock GR,Pauwels RA

更新日期：1997-11-12 00:00:00

abstract：:The cyclic AMP efflux from rat neostriatal slices induced by simultaneous activation of D-1 (stimulatory) and D-2 (inhibitory) dopamine receptors with 30 microM dopamine was inhibited by morphine (0.3-3 microM), [D-Ala2, D-Leu5]enkephalin (DADLE, 0.03-0.3 microM) but not by [D-Pen2, D-Pen5]enkephalin (DPDPE, 0.03-0.3 ...

journal_title：European journal of pharmacology

authors： Schoffelmeer AN,Hansen HA,Stoof JC,Mulder AH

更新日期：1985-12-03 00:00:00

abstract：:In view of the co-localization of spinal delta- and kappa-opioid receptors, we have investigated the interaction of selective opioid receptor agonists and antagonists in the spinal cord of mice in order to determine if these receptors are organized as heteromers. The finding that norbinaltorphimine (kappa) antagonized...

journal_title：European journal of pharmacology

authors： Portoghese PS,Lunzer MM

更新日期：2003-04-25 00:00:00

abstract：:The ability of putative melatonin receptor antagonists to antagonise melatonin-induced aggregation of pigment granules in cultured neural crest Xenopus laevis melanophores was examined. Neither ML 23 (N-(2,4-dinitrophenyl)-5-methoxytryptamine) nor 6-methoxy-2-benzoxazolinone showed agonist or antagonist activity. N-Ac...

journal_title：European journal of pharmacology

authors： Sugden D

更新日期：1992-03-31 00:00:00

abstract：:The potencies of histamine and methacholine were significantly increased by approximately 2- and 5-fold respectively in human non-diseased isolated bronchi on removal of the epithelium. In contrast, no increases in spasmogen potency were observed following epithelium removal in bronchi obtained from a sample of asthma...

journal_title：European journal of pharmacology

authors： Fernandes LB,Preuss JM,Paterson JW,Goldie RG

更新日期：1990-10-23 00:00:00

abstract：:Recombinant human GABA(A) receptors were investigated in vitro by coexpression of cDNAs coding for alpha1, beta2, and gamma2 subunits in the baculovirus/Sf-9 insect cell system. We report that a single amino acid exchange (isoleucine 121 to valine 121) in the N-terminal, extracellular part of the alpha1 subunit induce...

journal_title：European journal of pharmacology

authors： Westh-Hansen SE,Rasmussen PB,Hastrup S,Nabekura J,Noguchi K,Akaike N,Witt MR,Nielsen M

更新日期：1997-06-25 00:00:00

abstract：:Nitric oxide (NO) is present in the exhaled breath of humans and other mammalian species. It is generated in the lower airways by enzymes of the nitric oxide synthase (NOS) family, although nonenzymatic synthesis and consumptive processes may also influence levels of NO in exhaled breath. The biological properties of ...

journal_title：European journal of pharmacology

authors： Redington AE

更新日期：2006-03-08 00:00:00

abstract：:The effects of 2,3-butanedione monoxime (BDM) and 5-[1-(3,4-dimethoxybenzoyl)-1,2,3,4-tetrahydro-6-quinolyl]-6-me thy l-3,6-dihydro-2H-1,3,4-thiadiazin-2-one (EMD 53998) on cardiac muscle were studied in skinned muscle fibres from the right ventricle of the porcine heart. BDM decreases the Ca2+ sensitivity (pCa50 for ...

journal_title：European journal of pharmacology

authors： Barth Z,Strauss JD,Dohet C,Ruegg JC

更新日期：1996-02-05 00:00:00

abstract：:In animals given citalopram (10 mg/kg) twice daily for 14 days a further dose of 1 mg/kg, administered 24 h after the last dose, markedly increased cortical dialysate serotonin (5-hydroxytryptamine, 5-HT), but had no effect in control animals. The effect on dialysate 5-HT in the dorsal raphe was not increased by the c...

journal_title：European journal of pharmacology

authors： Invernizzi R,Bramante M,Samanin R

更新日期：1994-08-01 00:00:00

abstract：:The development of selective corticotropin-releasing factor type-1 (CRF1) receptor antagonists represents a potential novel treatment for depression. These studies evaluated CRF1 receptor antagonists for antidepressant-like activity in mice. Subchronic dosing of both R 121919 (3-[6-(dimethylamino)-4-methyl-pyrid-3-yl]...

journal_title：European journal of pharmacology

authors： Nielsen DM,Carey GJ,Gold LH

更新日期：2004-09-19 00:00:00

abstract：:Gaboxadol (THIP; 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) is an agonist at GABA(A) receptors. THIP concentrations (0.01-50 mM) were applied rapidly to Sf9 cells expressing the human alpha(1)beta(2)gamma(2S) GABA(A) receptors. The EC(50) values for the peak current in THIP alone or THIP plus 1 microM diazepam we...

journal_title：European journal of pharmacology

authors： Smith M,Lindquist CE,Birnir B

更新日期：2003-09-30 00:00:00

abstract：:Enterobacteria are known to deconjugate amino acid-conjugated bile acids in the intestine. Administration of ampicillin (ABPC; 3 days, 100mg/kg) decreased the expression of ileal farnesoid X receptor (Fxr) target genes, and increased the levels of total bile acids in the intestinal lumen. The primary tauro-conjugates ...

journal_title：European journal of pharmacology

authors： Kuribayashi H,Miyata M,Yamakawa H,Yoshinari K,Yamazoe Y

更新日期：2012-12-15 00:00:00

abstract：:This study investigated the characteristics of atrial natriuretic peptide (ANP) release from superfused sliced atria and ventricles of rats. Right atria spontaneously released more immunoreactive ANP (Ir-ANP: pg/min per mg tissue) (32 +/- 3) than did left atria (11 +/- 2) or right ventricles (1.5 +/- 0.5). Addition of...

journal_title：European journal of pharmacology

authors： Zongazo MA,Carayon A,Masson F,Maistre G,Noé E,Eurin J,Barthelemy C,Komajda M,Legrand JC

更新日期：1991-12-10 00:00:00

abstract：:Increasing evidence demonstrates that oxidative stress plays an important role in brain injury in experimental models of brain ischemia. Thymoquinone, the main constituents of the volatile oil from Negella sativa seeds, is reported to possess strong antioxidant properties. Hence, the present study was undertaken to ev...

journal_title：European journal of pharmacology

authors： Al-Majed AA,Al-Omar FA,Nagi MN

更新日期：2006-08-14 00:00:00

abstract：:In recent years, the pilocarpine model of temporal lobe epilepsy has become the most popular and widely used rodent model of this common and difficult-to-treat type of epilepsy. In this model, the cholinomimetic convulsant pilocarpine is used to induce a status epilepticus, which is followed by hippocampal damage and ...

journal_title：European journal of pharmacology

authors： Müller CJ,Bankstahl M,Gröticke I,Löscher W

更新日期：2009-10-01 00:00:00

abstract：:The role of the alpha 1-adrenoceptor subtypes, and their possible change with maturation, in alpha 1-adrenoceptor-induced pressor responses in the rat has not been established. Thus, the effects of the alpha 1D-, alpha 1A/1D- and alpha 1B/1D-adrenoceptor antagonists, BMY 7378 (8-(2-(4-(2-methoxyphenyl)-1-piperazinyl)e...

journal_title：European journal of pharmacology

authors： Ibarra M,Terrón JA,López-Guerrero JJ,Villalobos-Molina R

更新日期：1997-03-19 00:00:00

abstract：:Vasodilatory responses to bradykinin (BK) and acetylcholine (ACh) were compared in phenylephrine preconstricted perfused kidneys from 30-week-old male stroke-prone spontaneously hypertensive rats (SHRSP) and normotensive Wistar-Kyoto rats (WKY). Responses to ACh did not differ between kidneys from SHRSP and WHY. BK-in...

journal_title：European journal of pharmacology

authors： Stier CT Jr,Selig N,Itskovitz HD

更新日期：1992-01-14 00:00:00

abstract：:Cytokines and cytokine-induced nitric oxide (NO) play important roles in inflammatory glomerular diseases, and both platelet-derived growth factor and transforming growth factor-beta inhibit cytokine-induced NO production. In this study, we demonstrated that a selective endothelin ET(A) receptor antagonist, BQ-485 (He...

journal_title：European journal of pharmacology

authors： Hirahashi J,Nakaki T,Hishikawa K,Marumo T,Hayashi M,Saruta T

更新日期：1999-01-15 00:00:00

abstract：:The human 5-HT transporter (hSERT) has two binding sites for 5-HT and 5-HT uptake inhibitors: the orthosteric high-affinity site and a low-affinity allosteric site. Activation of the allosteric site increases the dissociation half-life for some uptake inhibitors. The objectives of this study were 1) to identify hSERT ...

journal_title：European journal of pharmacology

authors： Plenge P,Gether U,Rasmussen SG

更新日期：2007-07-12 00:00:00

abstract：:Using isolated rabbit gastric glands, the H2-receptor antagonist MK-208 was investigated with respect to its effects on [14C]aminopyrine uptake as an index of gastric acid secretion. In addition to shifting the histamine concentration-response curve to the right in a parallel fashion, the antagonism produced by MK-208...

journal_title：European journal of pharmacology

authors： Shepherd-Rose AJ,Pendleton RG

更新日期：1984-11-13 00:00:00

abstract：:Theophylline (0.1, 0.3 mM) produced a positive inotropism which was maximum by 15 min but was partially or completely absent by 45 min. The mechanism for this response was investigated using post-rest potentiation and positive staircase, phenomenon associated with the sarcoplasmic reticulum and sarcolemma, respectivel...

journal_title：European journal of pharmacology

authors： Zavecz JH

更新日期：1989-01-24 00:00:00