Comparison of [11C]diprenorphine and [11C]carfentanil in vivo binding to opiate receptors in man using a dual detector system.

abstract：:A brain slice preparation was used to examine the effects of galanin on the spontaneous firing rate of locus coeruleus noradrenergic neurons. Galanin (10(-9)-10(-7) M), added to the bath, inhibited the firing of 14 out of 19 neurons in a concentration-dependent manner. The observed effect was quite variable, ranging f...

journal_title：European journal of pharmacology

authors： Seutin V,Verbanck P,Massotte L,Dresse A

更新日期：1989-05-19 00:00:00

abstract：:meta-Substituted 2-chlorophenyl(imino)imidazolidines of the clonidine-type (2,3- and 2,5-substituted derivatives) were used in attempts to discriminate between alpha-adrenergic effects (central hypotensive and peripheral hypertensive activities) in rats. The central hypotensive activity of four pairs of substitution i...

journal_title：European journal of pharmacology

authors： de Jonge A,Slothorst-Grisdijk FP,Timmermans PB,Van Zwieten PA

更新日期：1981-05-22 00:00:00

abstract：:Experiments were undertaken to determine the effect of the selective histamine H3 receptor agonist (R)-alpha-methylhistamine on the amplitude of neurally evoked electrodermal (sudomotor) responses in anesthetized cats. (R)-alpha-Methylhistamine produced comparable dose-related depressions of these evoked sympathetic-c...

journal_title：European journal of pharmacology

authors： Koss MC

更新日期：1994-05-12 00:00:00

abstract：:The alpha 1-adrenoceptors present in the liver of rhesus monkeys was characterized using [3H]prazosin. This radioligand binds to monkey liver membranes with high affinity (KD 0.33 nM) to a moderately abundant number of sites (97 fmol/mg of protein). These sites were characterized pharmacologically, by binding competit...

journal_title：European journal of pharmacology

authors： García-Sáinz JA,Romero-Avila MT,González-Espinosa C

更新日期：1996-09-12 00:00:00

abstract：:We report the cloning, molecular characterization, and pharmacological characterization of the canine 5-HT2A and 5-HT2B receptors. The canine and human 5-HT2A receptors share 93% amino acid homology. The canine and human 5-HT2B receptors are also highly conserved (87% homology) with the exception of the carboxyl termi...

journal_title：European journal of pharmacology

authors： Bonaventure P,Nepomuceno D,Miller K,Chen J,Kuei C,Kamme F,Tran DT,Lovenberg TW,Liu C

更新日期：2005-04-25 00:00:00

abstract：:The antithrombotic effect of desethyl KBT-3022, which is the main active metabolite of the new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl] pyrrol-1-ylacetate; a cyclooxygenase inhibitor), was determined using a photochemically induced arterial thrombosis model in the rat femoral artery...

journal_title：European journal of pharmacology

authors： Shimazawa M,Takiguchi Y,Umemura K,Kondo K,Nakashima M

更新日期：1997-06-11 00:00:00

abstract：:The aim of the present study was to determine the effect of a calcium channel blocker on renal function, urinary endothelin excretion and endothelin receptor number in rats. Administration of cyclosporine resulted in a significant impairment of renal function when measured by either [14C]inulin or 24 h creatinine clea...

journal_title：European journal of pharmacology

authors： Brooks DP,Ohlstein EH,Contino LC,Storer B,Pullen M,Caltabiano M,Nambi P

更新日期：1991-02-26 00:00:00

abstract：:The actions of tumor-promoting phorbol esters in smooth muscle excitation-contraction coupling were studied in isolated guinea pig ileum in the presence of various contractile agents. Muscarinic agonists, histamine and bradykinin elicited an initial transient phasic contraction and a subsequent sustained tonic contrac...

journal_title：European journal of pharmacology

authors： Xu SF,Collins MA,Chang KJ

更新日期：1991-08-29 00:00:00

abstract：:Oxidative stress is usually considered as an important factor to the pathogenesis of various diseases. Peroxynitrite (ONOO(-)) and hypochlorite (OCl(-)) are formed in immune cells as a part of the innate host defense system, but excessive reactive oxygen species generation can cause progressive inflammation and tissue...

journal_title：European journal of pharmacology

authors： Ren X,Ding Y,Lu N

更新日期：2016-03-15 00:00:00

abstract：:To identify the site of action of opiate-induced prolactin elevation, in vitro rat hemipituitary incubations were performed in the presence of morphine, met-enkephalin, ala2-met5-enkephalinamide and dopamine (DA) and combinations of opiate with the catecholamine. No opiate stimulated prolactin release directly nor did...

journal_title：European journal of pharmacology

authors： Login IS,Macleod RM

更新日期：1979-12-07 00:00:00

abstract：:The activity of angiotensin-converting enzyme in rat choroid plexus was higher than that of any other organ, being 6--7 times higher than that in lung and more than 50 times higher than in any other region of brain. Rabbit choroid plexus also had high activity of enzyme while that of human choroid plexus was relativel...

journal_title：European journal of pharmacology

authors： Arregui A,Iversen LL

更新日期：1978-11-01 00:00:00

abstract：:We investigated the relationship between tension development and the cytosolic free Ca2+ level ([Ca2+]i) on exposure of the endothelium-denuded isolated rat aorta to palmitoyl-L-alpha-lysophosphatidylcholine. Lysophosphatidylcholine concentration-dependently induced a gradual increase in [Ca2+]i. Application of 10(-4)...

journal_title：European journal of pharmacology

authors： Suenaga H,Kamata K

更新日期：1999-08-06 00:00:00

abstract：:Previous investigations in our laboratory revealed subsensitivity of right ventricular tissue, isolated from one month STZ-diabetic rats, to the inotropic effects of isoproterenol. The present study was concerned with the characterization of this subsensitivity phenomenon. Observations of supersensitivity to methoxami...

journal_title：European journal of pharmacology

authors： Ramanadham S,Tenner TE Jr

更新日期：1987-04-29 00:00:00

abstract：:The functional role of P2X7 receptor (P2X7R) inhibition in cancer-induced bone pain has been highly contradictory. Whereas knockout studies have suggested pro-nociceptive effects, pharmacological studies suggest anti-nociceptive or no effect. The discrepancy is likely linked to the highly polymorphic nature of the P2X...

journal_title：European journal of pharmacology

authors： Falk S,Appel CK,Bennedbæk HB,Al-Dihaissy T,Unger A,Dinkel K,Heegaard AM

更新日期：2019-02-15 00:00:00

abstract：:Atropine-induced locomotor stimulation was investigated in the developing rat pretreated with 6-hydroxydopa at birth. The locomotor stimulation by atropine was first observed on day 20 and gradually increased with age. The treatment with 6-hydroxydopa potentiated atropine-induced locomotor stimulation on days later th...

journal_title：European journal of pharmacology

authors： Nomura Y,Segawa T

更新日期：1978-08-15 00:00:00

abstract：:Cancer cell lines derived from hepatocytes have an altered phenotype and they lack hepatocyte-specific functions. It is at least partly due to the under-expression of transcription factors such as hepatocyte nuclear factor 4α (HNF4α), steroid receptor co-activator 1 (SRC1) etc. Recently, a strategy of transient transf...

journal_title：European journal of pharmacology

authors： Novotna A,Doricakova A,Vrzal R,Pavek P,Dvorak Z

更新日期：2011-11-01 00:00:00

abstract：:Carbocyclic thromboxane A2 (CTA2) constricted rabbit basilar and saphenous arteries. The contractions of the basilar artery, but not those of the saphenous artery, were potently inhibited by the calcium antagonist nimodipine. Selective inhibition of thromboxane-induced vasoconstriction of cerebral vessels may contribu...

journal_title：European journal of pharmacology

authors： Towart R,Perzborn E

更新日期：1981-01-16 00:00:00

abstract：:The effect of resveratrol, an aryl hydrocarbon receptor antagonist, on the teratogenicity induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) was investigated. Pregnant C57BL/6J mice were orally administered resveratrol (50 mg/kg) for 6 consecutive days, from gestational day (GD) 8 to GD13, followed by an oral chall...

journal_title：European journal of pharmacology

authors： Jang JY,Park D,Shin S,Jeon JH,Choi BI,Joo SS,Hwang SY,Nahm SS,Kim YB

更新日期：2008-09-04 00:00:00

abstract：:Fluoxetine has been shown to induce anti-tumour activity. The aim of this study was to determine the effect of fluoxetine on HCT116+/+ and p53 gene-depleted HCT116-/- human colorectal cancer cells and the mechanisms, including potential p53-dependence, of its action. Fluoxetine-induced apoptosis was investigated by mi...

journal_title：European journal of pharmacology

authors： Marcinkute M,Afshinjavid S,Fatokun AA,Javid FA

更新日期：2019-08-15 00:00:00

abstract：:We have examined the role of protein kinase C in the regulation of foetal-calf serum-stimulated cell proliferation in human prostatic smooth muscle cells. The data showed that the proliferative effect to foetal-calf serum (10%, v/v) was partially inhibited by 12-(2-cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-i...

journal_title：European journal of pharmacology

authors： Guh JH,Chueh SC,Hwang TL,Chen J,Teng CM

更新日期：1998-10-23 00:00:00

abstract：:In chloralose-anaesthesized cats, clonidine, an alpha 2-adrenoceptor agonist with an imidazole ring, depressed pudendal nerve reflex activity. Clonidine's inhibitory action on this compound action potential response was mimicked by guanabenz, a non-imidazole alpha 2-adrenoceptor agonist, and was reversed by SK & F 864...

journal_title：European journal of pharmacology

authors： Downie JW,Espey MJ,Gajewski JB

更新日期：1991-03-26 00:00:00

abstract：:The effects of H 25 and H 74 on ouabain-resistant 86Rb+ influx were tested in beta-cell-rich mouse pancreatic islets. Both H 25, which is considered to be a specific inhibitor of Na+, K+, Cl- co-transport, and H 74, a specific inhibitor of K+, Cl- co-transport, reduced the ouabain-resistant 86Rb+ influx. The specific ...

journal_title：European journal of pharmacology

authors： Sandström PE,Sehlin J

更新日期：1993-07-20 00:00:00

abstract：:We studied the relationships between arachidonic acid (AA) metabolism and contractile responses to Na arachidonate (NaA) and the prostaglandins (PGs) in mesenteric arteries isolated from sham-operated and totally pancreatectomized dogs. PGE2 and PGF2 alpha produced a similar dose-dependent relaxation of mesenteric art...

journal_title：European journal of pharmacology

authors： Sterin-Borda L,Franchi AM,Borda ES,Del Castillo E,Gimeno MF,Gimeno AL

更新日期：1984-08-17 00:00:00

abstract：:Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...

journal_title：European journal of pharmacology

authors： Cui L,Xu F,Wu K,Li L,Qiao T,Li Z,Chen T,Sun C

更新日期：2020-08-15 00:00:00

abstract：:The binding of tritium-labelled BIBP3226, N2-(diphenylacetyl)-N-[(4-hydroxy-phenyl)methyl]-D-arginine amide, to human neuroblastoma SK-N-MC cells was investigated. [3H]BIBP3226 reversibly binds to neuropeptide Y receptors of the Y1 subtype expressed in SK-N-MC cells with a KD of 2.1 +/- 0.3 nM (mean +/- S.E.M., n = 3)...

journal_title：European journal of pharmacology

authors： Entzeroth M,Braunger H,Eberlein W,Engel W,Rudolf K,Wienen W,Wieland HA,Willim KD,Doods HN

更新日期：1995-05-24 00:00:00

abstract：:Socially reared and isolation-reared rats treated chronically since weaning with alpha-flupenthixol showed elevated levels of spontaneous locomotor activity compared with control treated rats. However, chronic apomorphine treatment had no effect on spontaneous locomotor activity. Chronic alpha-flupenthixol treatment e...

journal_title：European journal of pharmacology

authors： Sahakian BJ,Robbins TW,Iversen SD

更新日期：1976-05-01 00:00:00

abstract：:The detrimental cardio-toxic effect of doxorubicin, an effective chemotherapeutic agent, limited its clinical use. It has been claimed that doxorubicin cardio-toxicity occurs through calcium ions (Ca2+) overload and reactive oxygen species production. Agmatine, an endogenous imidazoline receptor agonist, induce uptake...

journal_title：European journal of pharmacology

authors： Yarmohmmadi F,Rahimi N,Faghir-Ghanesefat H,Javadian N,Abdollahi A,Pasalar P,Jazayeri F,Ejtemaeemehr S,Dehpour AR

更新日期：2017-02-05 00:00:00

abstract：:The effects of morphine tolerance-dependence and abstinence on 5-HT1A receptors in brain regions and spinal cord of the rat were determined. Tolerance to and physical dependence on morphine was induced in male Sprague-Dawley rats by implanting six morphine pellets (each containing 75 mg of morphine free base) during a...

journal_title：European journal of pharmacology

authors： Gulati A,Bhargava HN

更新日期：1990-07-03 00:00:00

abstract：:Perfused rabbit hearts removed 3H-5-hydroxytryptamine (3H-5-HT) from a perfusion solution containing 2.6 ng/ml and a tissue-to-medium ratio of about 10 was achieved after a 55 min perfusion period. 12.4 +/- 1.0% of the cardiac total radioactivity consisted of metabolites and metabolites appeared in the venous effluent...

journal_title：European journal of pharmacology

authors： Fozard JR,Berry JL

更新日期：1975-06-01 00:00:00

abstract：:Clinically, dexamethasone is known to reduce cerebral edema. To further investigate the mechanism of this neuroprotection, an in vitro model of brain-derived microvessel endothelial cells (BME cells) was used to investigate the effect of dexamethasone on hypoxia-induced hyperpermeability. Furthermore, the expression o...

journal_title：European journal of pharmacology

authors： Fischer S,Renz D,Schaper W,Karliczek GF

更新日期：2001-01-12 00:00:00