Abstract：
:In a medium containing 100 mM NaCl and 10 mM MgCl2, the binding of antagonists to rat myocardial muscarinic receptors is well described by the simple Langmuir isotherm. However, in low ionic strength media, while a small proportion of the sites (23%) display a small (2-3 fold) increase in antagonist affinity, the majority demonstrate a substantial (ca. 10-fold) decrease. This reduction is reversed by micromolar concentrations of guanylylimidodiphosphate and other GTP analogues, with consequent abolition of the heterogeneity of the receptor population induced by low ionic strength. Millimolar concentrations of Mg2+ but not other cations strongly potentiate this action of the guanine nucleotides.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Hulme EC,Berrie CP,Birdsall NJ,Burgen ASdoi
10.1016/0014-2999(81)90085-6subject
Has Abstractpub_date
1981-07-17 00:00:00pages
137-42issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(81)90085-6journal_volume
73pub_type
杂志文章abstract：:Adenosine added to isolated electrically driven preparations of human ventricular heart muscle antagonized the positive inotropic effect of isoprenaline (mean EC50 19 mumol 1(-1), n = 9). Similar effects were observed with the adenosine receptor agonist (-)-N6-phenylisopropyladenosine (mean EC50 0.5 mumol 1(-1), n = 7...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90170-0
更新日期：1985-10-22 00:00:00
abstract：:Of eleven aporphine analogues tested on striatal adenylate cyclase only (-)-apomorphine and (+/-)-N-n-propyl-norapomorphine (+/-(NPA)) were effective in stimulating the cyclase from rat brain. Inactive compounds included (+/-)-isoapomorphine, (-)-1,2-dihydroxyaporphine and (+/-)-10-hydroxy-N-n-propylnoraporphine. (+)-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90302-2
更新日期：1976-01-01 00:00:00
abstract：:The effects of intracisternal injections of [Lys8]vasopressin and [Arg8]vasopressin (25, 50, 100, 200 mU/kg) and related compounds oxytocin (25, 50, 100, 200 mU/kg), felypressin (25, 50, 100, 200 mU/kg) and vasotocin (100, 200, 400, 800 ng/kg) on the acute neurogenic pressor responses to afferent vagal stimulation (5,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90009-3
更新日期：1985-11-19 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
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.07.049
更新日期：2011-11-01 00:00:00
abstract：:The role of pertussis toxin-sensitive G proteins on the alpha 2-adrenoceptor and mu-opioid receptor-mediated inhibition of the efferent function of capsaicin-sensitive neurones was investigated in guinea-pig atria pretreated with guanethidine. In the presence of atropine, CGP 20712A (2-hydroxy-5-(2-[hydroxy-3-(4-[(1-m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90444-9
更新日期：1992-06-17 00:00:00
abstract：:Translational research for neurodegenerative disease depends intimately upon animal models. Unfortunately, promising therapies developed using mouse models mostly fail in clinical trials, highlighting uncertainty about how well mouse models mimic human neurodegenerative disease at the molecular level. We compared the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.03.021
更新日期：2015-07-15 00:00:00
abstract：:Carbachol produces both negative and positive inotropy in rat left atria. It is not clear whether these two effects are mediated by two separate cell surface muscarinic receptors or a single receptor interacting with two coupling proteins in the cell membrane. Pirenzepine, known to selectively block some biochemical m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94095-f
更新日期：1990-11-20 00:00:00
abstract：:It has been shown that G-protein coupled receptors have seven transmembrane alpha-helices, but the structural changes occurring in a G-protein coupled receptor as a response on agonist stimulus and the molecular events leading to blockade of the signal transduction by antagonists are not well understood. In the presen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00860-3
更新日期：2001-03-23 00:00:00
abstract：:The effect of local administration of big endothelin-1 (1-38, big ET-1) has been investigated on blood flow in the skin of anaesthetised rats, measured by 133Xe clearance. The local effects of big ET-1 and big endothelin-3 (1-41, big ET-3) have also been determined on microvessel diameter by intravital microscopy of t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90056-n
更新日期：1993-03-23 00:00:00
abstract：:The present work is aimed at evaluating the protective effect of eugenol against in vitro nicotine-induced toxicity in murine peritoneal macrophages, compared with N-acetylcysteine. Eugenol was isolated from Ocimum gratissimum and characterized by HPLC, FTIR, (1)H NMR. To establish most effective protective support, w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.09.019
更新日期：2009-11-25 00:00:00
abstract：:Precipitated withdrawal in rats chronically exposed to delta 9-tetrahydrocannabinol, the major psychoactive principle of the marijuana plant, was unequivocally demonstrated for the first time using a selective antagonist, SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1(2,4- dichloro-phenyl)-4-methyl-1H-pyrazole ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00447-s
更新日期：1995-08-25 00:00:00
abstract：:Cytochrome P450 2J2 (CYP2J2) is highly expressed in human tumors and carcinoma cell lines, and has been implicated in the pathogenesis of human cancers. The aim of this study was to identify a compound that could inhibit the activity of CYP2J2, and to examine its anticancer activity. To identify CYP2J2 inhibitors, 10 ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.07.047
更新日期：2015-10-05 00:00:00
abstract：:The effects of propofol, pentobarbital, alphaxalone, etomidate and diazepam on t-[35S]butylbicyclophosphorothionate ([35S]TBPS) binding to membrane preparations from rat cerebral cortex were studied in the absence of gamma-aminobutyric acid (GABA). Addition of low concentrations (3-10 microM) of propofol to washed mem...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90172-4
更新日期：1994-04-15 00:00:00
abstract：:Kappa- and mu-opioid binding site affinities of the kappa-selective ligand U62066 and its optical isomers, (+)-U63639 and (-)-U63640 were compared with those of the structurally related ligand PD117302 and its respective isomers, (+)-PD123497 and (-)-PD123475. The relative efficacies of each compound were also establi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90512-8
更新日期：1989-12-07 00:00:00
abstract：:The middle ear epithelium functions to maintain a fluid-free middle ear cavity. Dysfunction of the middle ear epithelial ion and fluid transport is implicated in the pathogenesis of fluid collection in the middle ear cavity, characteristic of otitis media with effusion. The efficacy of steroid therapy for the treatmen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.11.012
更新日期：2009-01-14 00:00:00
abstract：:The stress-induced hyperthermia procedure, in which effects of drugs on basal (T(1)) and stress-induced body temperature (T(2)) are measured, predicts anxiolytic drug effect. Serotonergic drugs alter these responses and here, we studied the role of 5-HT(1A) receptors in stress-induced hyperthermia by using 5-HT(1A) re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.08.058
更新日期：2006-11-21 00:00:00
abstract：:The effects of dopamine (DA) and of two selective DA DA1 agonists (SKF 38393 and SKF 82526) on adenylate cyclase activity were studied with human kidney cortex membrane preparations. DA elicited a dose-related stimulation of adenylate cyclase activity with an EC50 of 60 microM. The selective DA DA1 antagonist SCH 2339...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90667-x
更新日期：1988-05-10 00:00:00
abstract：:Physiological experiments suggest that the angiotensin AT1 receptor type predominates in rat vas deferens. Membrane binding experiments, using 125I-[Sarl,Ile8]angiotensin II, confirm the presence of angiotensin AT1 receptors and the absence of angiotensin AT2 receptors in this tissue. Angiotensin II and the angiotensi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00380-x
更新日期：1998-06-26 00:00:00
abstract：:Endogenous D-serine is known to modulate glutamatergic transmission via interaction with the glycine site of N-methyl-D-aspartate (NMDA) receptors. D-serine is synthesized by racemization of L-serine using an enzymatic reaction catalyzed by serine racemase. Although much attention has been focused on the role of D-ser...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.09.011
更新日期：2012-12-05 00:00:00
abstract：:The effects of the new 3,4-disubstituted furoxan, CHF 2206, on vascular tone, platelet aggregation and platelet cyclic 3',5'-guanosine monophosphate (cGMP) levels were investigated. The compound was a potent inhibitor of rabbit aortic ring contraction induced by norepinephrine, the stable prostaglandin F2 alpha analog...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90077-9
更新日期：1994-04-01 00:00:00
abstract：:In the Brattleboro rat with diabetes insipidus vasopressin V2 receptor mRNA and the mRNA of various adenylyl cyclase (AC) isoforms are moderately reduced compared with those of normal rats. In the present study renal vasopressin V2 receptor mRNA was modestly higher (by 34%), as was expression of AC 5, 6 and 9 mRNAs (u...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01461-1
更新日期：1998-01-02 00:00:00
abstract：:Trans-dehydrocrotonin has antiulcerogenic and antitumor activities. A complex of beta-cyclodextrin with dehydrocrotonin was developed to improve the delivery of dehydrocrotonin. Complex in solid state was evaluated using X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermal gravimetric analysis (TG...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.01.016
更新日期：2005-03-07 00:00:00
abstract：:The efficacy of a combinational prophylactic regimen on the lethality, convulsions, and loss of morphological and functional integrities of the brain induced by an organophosphate soman was investigated in rats. The rats were implanted subcutaneously with osmotic minipumps containing the combinational prophylactic reg...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.10.034
更新日期：2004-11-28 00:00:00
abstract：:Rats were injected with 15 mg/kg (i.p.) mianserin or vehicle (saline) for 4, 10 or 21 days and 5-HT2 receptor binding and mRNA levels measured. Treatment with mianserin induced a substantial decrease in 5-HT2 radioligand binding (44-59% decrease; P less than 0.05 vs. control). No changes in the amount of 5-HT2 or, as ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90093-w
更新日期：1991-06-19 00:00:00
abstract：:Clearance of apoptotic cells, so-called efferocytosis, by alveolar macrophages (AMs) is important for lung homeostasis and is impaired in pulmonary inflammatory diseases, such as chronic obstructive pulmonary disease and asthma. Carbocisteine, a mucoregulatory drug, corrects the contents of fucose in airway mucus and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.12.026
更新日期：2012-02-29 00:00:00
abstract：:The ability of flunarizine to terminate ouabain-induced ventricular tachycardia was investigated in conscious dogs. These arrhythmias result from triggered activity based on delayed afterdepolarizations. Sustained ventricular tachycardia was induced by ouabain (48 +/- 6 micrograms/kg) and pacing in 13 animals with sur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90780-2
更新日期：1989-06-08 00:00:00
abstract：:5-methoxy-N,N-dimethyltryptamine (5-MeODMT) produced a dose-dependent decrease in the discharge rate of serotonin-containing neurons in the dorsal raphe nucleus of freely moving cats. This ranged from a 15% decrease at 10 microgran/kg, i.m., to a virtual complete depression of activity at 250 microgram/kg. 5-MeODMT's ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90406-0
更新日期：1979-02-15 00:00:00
abstract：:Quick stretching of a helical strip of dog basilar artery at a rate of 10 cm/s to 140% of the slack length of the muscle evoked a delayed contraction. A small amount of hemolysate (0.01-0.2 mg/ml as hemoglobin), which increased the basal tone by 10-15% of the maximum contracture produced by 80 mM K+, potentiated the s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90814-5
更新日期：1989-10-04 00:00:00
abstract：:This study shows that in spontaneously hypertensive rats (SHR) of 14-weeks-old, the sympathetically-induced, but not noradrenaline-induced tachycardic response are higher than age-matched Wistar normotensive rats. Furthermore, in SHR the sympathetically-induced tachycardic response was: (1) unaffected by moxonidine (3...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.08.017
更新日期：2016-11-15 00:00:00
abstract：:The effects of inosine on sinus rate and atrial contractile force were investigated using the isolated and blood-perfused canine atrium which was perfused with arterial blood from a donor dog. Injected inosine (100-3000 micrograms) consistently induced positive chronotropic and inotropic effects. However, the larger d...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90174-0
更新日期：1980-10-31 00:00:00
