Tissue selectivity of substance P alkyl esters: suggesting multiple receptors.

abstract：:Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared bindi...

journal_title：European journal of pharmacology

authors： Wilcox KM,Paul IA,Woolverton WL

更新日期：1999-02-19 00:00:00

abstract：:Rats were treated with ethanol in the drinking fluid 2 X 1 h daily for 83 weeks. [3H]Muscimol, [3H]quinuclidinyl benzilate ( [3H]QNB) and [3H]nicotine binding was measured in selected brain areas 7, 14 and 21 days after withdrawal of ethanol. A significant increase (P less than 0.05) when compared to controls was foun...

journal_title：European journal of pharmacology

authors： Nordberg A,Wahlström G,Eriksson B

更新日期：1985-09-24 00:00:00

abstract：:Prior studies demonstrated that guanabenz reduces systemic blood pressure by inhibiting central sympathetic outflow as well as by adrenergic neuron blockade. Potential mechanisms responsible for the reduction of efferent sympathetic activity were examined in the present series. Guanabenz failed to modify carotid sinus...

journal_title：European journal of pharmacology

authors： Baum T,Shropshire AT

更新日期：1976-05-01 00:00:00

abstract：:By far the most attention has been paid to the deleterious actions of nonsteroidal anti-inflammatory drugs (NSAIDs), including isoform selective agents that inhibit cyclooxygenase (COX), on the upper gastrointestinal tract, particularly the gastric and duodenal mucosa. However, recent studies confirm a relatively high...

journal_title：European journal of pharmacology

authors： Whittle BJ

更新日期：2004-10-01 00:00:00

abstract：:As there is increasing evidence that purines are involved in cerebral vasodilatation, purine receptors were characterized pharmacologically in pial arteries from rabbit, cat and man, and compared with purine receptors in various non-cerebral vascular beds. Use of agonists and antagonists allows purine receptors to be ...

journal_title：European journal of pharmacology

authors： Hardebo JE,Kåhrström J,Owman C

更新日期：1987-12-15 00:00:00

abstract：:Pigs were subjected to acute, intermittent hypoxia (fraction of inhaled O2 0.1, n = 10). The increase in mean pulmonary artery pressure during hypoxia was not altered after i.v. administration of the selective endothelin ETB receptor antagonist BQ-788 (N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D -1- me...

journal_title：European journal of pharmacology

authors： Holm P,Liska J,Franco-Cereceda A

更新日期：1997-03-26 00:00:00

abstract：:Microglia initially undergo rapid activation in response to injury and stressful stimuli, such as hypoxia. Oxidative stress and the inflammatory response play critical roles in hypoxic-ischemic brain injury. Carvedilol is a β-blocker used to treat high blood pressure and heart failure. In this study, we investigated w...

journal_title：European journal of pharmacology

authors： Gao X,Wu B,Fu Z,Zhang Z,Xu G

更新日期：2017-11-05 00:00:00

abstract：:The development of anticonvulsant tolerance with RO 16-6028, a benzodiazepine receptor partial agonist, was assessed in mice using an i.v. infusion of pentylenetetrazol as the convulsive stimulus. In contrast to other benzodiazepines tested previously in this seizure model the anticonvulsant protection afforded by RO ...

journal_title：European journal of pharmacology

authors： Haigh JR,Feely M

更新日期：1988-03-01 00:00:00

abstract：:We investigated the effects of antithrombin, a plasma inhibitor of coagulation factors, in rats with puromycin aminonucleoside-induced nephrosis, which is an experimental model of human nephrotic syndrome. Antithrombin (50 or 500 IU/kg/i.v.) was administered to rats once a day for 10 days immediately after the injecti...

journal_title：European journal of pharmacology

authors： Yamashita J,Nakajima K,Ohno Y,Kaneshiro Y,Matsuo T,Tanaka H,Kaneko K

更新日期：2008-07-28 00:00:00

abstract：:Three peptide components of atrial natriuretic factor (ANF) caused relaxation of carbachol-contracted guinea-pig isolated tracheal smooth muscle. These were the 1-28, 5-28 and 5-27 peptide sequences (ANF(1-28), ANF-(5-28) and ANF-(5-27)). The peptides were 10-30 times more potent in epithelium-denuded than in epitheli...

journal_title：European journal of pharmacology

authors： Fernandes LB,Preuss JM,Goldie RG

更新日期：1992-03-03 00:00:00

abstract：:The goal of this report is to present the results obtained with three new GABAB receptor antagonists. CGP 54062 has an IC50 in a GABAB binding test of 0.013 microM which is roughly 2500-fold lower than one of the most potent blockers known so far, CGP 35348 (IC50 = 34 microM). CGP 46381 and CGP 36742 have IC50s of 4.9...

journal_title：European journal of pharmacology

authors： Olpe HR,Steinmann MW,Ferrat T,Pozza MF,Greiner K,Brugger F,Froestl W,Mickel SJ,Bittiger H

更新日期：1993-03-23 00:00:00

abstract：:There is increasing evidence in support of an important role played by neurotensin (NT), a tridecapeptide originally found in bovine hypothalamus, in regulation of cardiovascular system. Elevated systemic levels of NT may contribute to pathogenesis of acute circulatory disoders, and predict the risk for cardiovascular...

journal_title：European journal of pharmacology

authors： Osadchii OE

更新日期：2015-09-05 00:00:00

abstract：:Ovarian cancer is the major cause of cancer death among female genital malignancies, and requires developing novel therapeutic measures. Immune escape and acquisition of tolerance by tumor cells are essential for cancer growth and progression. An immunoregulatory enzyme indoleamine 2,3-dioxygenase (IDO) overexpression...

journal_title：European journal of pharmacology

authors： Kobayashi A,Tanizaki Y,Kimura A,Ishida Y,Nosaka M,Toujima S,Kuninaka Y,Minami S,Ino K,Kondo T

更新日期：2015-11-05 00:00:00

abstract：:Increasing costs, much time consumption and high risk of failure associated with the process of de novo development of new anticancer drugs have prompted the pharmaceutical industry to seek alternative strategies that may facilitate and accelerate the whole process. In particular, the repurposing strategy, known also ...

journal_title：European journal of pharmacology

authors： Antoszczak M,Markowska A,Markowska J,Huczyński A

更新日期：2020-01-05 00:00:00

abstract：:The significance of neuropeptide Y Y(2) receptors in sympathetic nonadrenergic transmission was investigated using the novel selective antagonist BIIE0246 ((S)-N2-[[1-[2-[4-[(R,S)-5,11-dihydro-6(6h)-oxodibenz[b,e]azepin-11-yl]-1-piperazinyl]-2-oxoethyl]cyclopentyl]acetyl]-N-[2-[1,2-dihydro-3,5 (4H)-dioxo-1,2-diphenyl-...

journal_title：European journal of pharmacology

authors： Malmström RE,Lundberg JO,Weitzberg E

更新日期：2002-03-29 00:00:00

abstract：:The effects of (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'- trifluoromethylpropiophenone monohydrochloride (NK433), a novel centrally acting muscle relaxant, on masticatory muscle reflexes were investigated in rats. NK433 inhibited the monosynaptic tonic vibration reflex of the masseter muscle and the polysynaptic tonic pe...

journal_title：European journal of pharmacology

authors： Ozawa Y,Komai C,Sakitama K,Ishikawa M

更新日期：1996-02-29 00:00:00

abstract：:Although convulsions due to local anesthetic systemic toxicity are thought to be due to inhibition of GABA(A) receptor-linked currents in the central nervous system, the mechanism of action remains unclear. We therefore examined the effects of local anesthetics on gamma-aminobutyric acid (GABA)-induced currents using ...

journal_title：European journal of pharmacology

authors： Sugimoto M,Uchida I,Fukami S,Takenoshita M,Mashimo T,Yoshiya I

更新日期：2000-08-11 00:00:00

abstract：:The effects of 4-aminopyridine (4-AP) on basal and glucose-induced insulin secretion and on plasma glucose concentrations were investigated in vivo in intact mice and in mice subjected to surgical adrenalectomy plus chemical sympathectomy induced by 6-hydroxydopamine. In normal intact mice, an i.v. injection of 4-AP, ...

journal_title：European journal of pharmacology

authors： Ahrén B,Leander S,Lundquist I

更新日期：1981-09-11 00:00:00

abstract：:Blockade of sodium channels located in the sinoatrial node can slow diastolic depolarisation rate, recorded in vitro. The objective was therefore to determine whether these blockers could slow heart rate in vivo. The heart rate was firstly measured in spontaneously beating, isolated rat heart atria in the presence of ...

journal_title：European journal of pharmacology

authors： Létienne R,Vié B,Le Grand B

更新日期：2006-01-20 00:00:00

abstract：:The present study was undertaken to investigate vascular function in hypercholesterolemic rabbits and also to characterize the effects of pioglitazone on it. Rabbits were fed normal, 0.5% cholesterol chow, or 0.5% cholesterol chow plus 300 ppm pioglitazone for 5 or 10 weeks. The tension of isolated renal artery rings ...

journal_title：European journal of pharmacology

authors： Moroe H,Fujii H,Honda H,Arai K,Kanazawa M,Notoya Y,Kogo H

更新日期：2004-08-30 00:00:00

abstract：:We have investigated, by using the whole-cell patch-clamp technique, the Ca2+ channel antagonist properties of eliprodil in cultured cerebellar granule cells which are known to express L-, N-, P- as well as Q- and R-type Ca2+ channels. Eliprodil maximally antagonized 50% of the voltage-dependent Ba2+ current with an I...

journal_title：European journal of pharmacology

authors： Biton B,Godet D,Granger P,Avenet P

更新日期：1997-04-04 00:00:00

abstract：:The treatment of rat thymocytes with 10 microM terfenadine resulted in a significant increase in DNA fragmentation. The DNA fragmentation induced by terfenadine was dependent on its concentration and incubation time. In terfenadine-treated cells, the translocation of phosphatidylserine from the inside of plasma membra...

journal_title：European journal of pharmacology

authors： Enomoto R,Komai T,Yoshida Y,Sugahara C,Kawaguchi E,Okazaki K,Kinoshita H,Komatsu H,Konishi Y,Lee E

更新日期：2004-08-02 00:00:00

abstract：:We have demonstrated that activation of ATP-sensitive potassium (K(ATP)) channels can attenuate sympathetic hyperinnervation. Sildenafil, a phosphodiesterase-5 inhibitor, has been shown to provide a preconditioning-like cardioprotective effect via opening of K(ATP) channels. The aim of this study was to investigate wh...

journal_title：European journal of pharmacology

authors： Lee TM,Chen CC,Chung TH,Chang NC

更新日期：2012-09-05 00:00:00

abstract：:Agomelatine is an antidepressant with a novel mechanism of action. It is a melatonergic agonist for MT1 and MT2 receptors and a serotonin (5-HT2C) receptor antagonist. Agomelatine has been suggested not to have adverse effects on sexual functions. However, the effects of chronic agomelatine administration on reproduct...

journal_title：European journal of pharmacology

authors： Canpolat S,Ulker N,Yardimci A,Bulmus O,Ozdemir G,Sahin Z,Ercan Z,Serhatlioglu I,Kacar E,Ozcan M,Turk G,Ozkan Y,Atmaca M,Yilmaz B,Kelestimur H

更新日期：2016-01-05 00:00:00

abstract：:Several effects of bacterial endotoxins involve an opioid pathway and neuropeptide FF is an endogenous peptide known to modulate opioid activity, mainly in the central nervous system. The aim of this study was to investigate in rats the role of central neuropeptide FF receptors in intestinal motor disturbances and bod...

journal_title：European journal of pharmacology

authors： Million M,Fioramonti J,Zajac JM,Buéno L

更新日期：1997-09-03 00:00:00

abstract：:The main purpose of this study was to compare in vitro pharmacological properties of human αCGRP (CGRP) and a recently discovered metabolically stable CGRP analogue, SAX, in isolated rat and human artery segments. In rat, CGRP and SAX induced similar vasodilatory responses in isolated mesenteric artery with the potenc...

journal_title：European journal of pharmacology

authors： Sheykhzade M,Abdolalizadeh B,Koole C,Pickering DS,Dreisig K,Johansson SE,Abboud BK,Dreier R,Berg JO,Jeppesen JL,Sexton PM,Edvinsson L,Wootten D,Sams A

更新日期：2018-06-15 00:00:00

abstract：:The beta-carboline FG 7142 was studied alone and in combination with Ro 15-1788, CGS 8216 and lorazepam in squirrel monkeys trained to respond under a fixed-interval (FI) schedule of food presentation. FG 7142 (0.3-5.6 mg/kg i.v.) produced dose-related decreases in the rate of FI responding, effects opposite to those ...

journal_title：European journal of pharmacology

authors： Wettstein JG

更新日期：1989-04-25 00:00:00

abstract：:Effects of (2RS, 3SR)-2-aminomethyl-2,3,7,8-tetrahydro-2,3,5,8, 8-pentamethyl-6H-furo-[2,3-e] indol-7-one hydrochloride (UK-1745), a novel cardiotonic drug with beta-adrenoceptor blocking property and antiarrhythmic activity, on the action potentials of isolated papillary muscles and the membrane currents of single ve...

journal_title：European journal of pharmacology

authors： Uemura H,Sakamoto N,Nakaya H

更新日期：1999-11-03 00:00:00

abstract：:An enhanced vasoconstrictor activity of cutaneous arteries participates in the reduction of skin blood flow induced by cooling stimulation. Raynaud's phenomenon, which is characterized by intense cooling-induced constriction of cutaneous arteries, is more common in women during the period from menarche to menopause. W...

journal_title：European journal of pharmacology

authors： Serizawa I,Iwasaki N,Ishida H,Saito SY,Ishikawa T

更新日期：2017-02-15 00:00:00

abstract：:We have assessed the capacity of two novel inhibitors to block cytokine-induced nitric oxide (NO) synthesis by macrophages and vascular smooth muscle cells, as well as NO production by the constitutive enzyme in central nervous system tissue. NG-Cyclopropyl-L-arginine selectively inhibited Ca2+/calmodulin-dependent NO...

journal_title：European journal of pharmacology

authors： Lambert LE,French JF,Whitten JP,Baron BM,McDonald IA

更新日期：1992-05-27 00:00:00