Abstract：
:Stimulation of [35S]GTPgammaS binding by serotonin (5-hydroxytryptamine, 5-HT) receptor ligands was characterized in rat hippocampal membranes. The optimized assay contained 30-50 microg protein, 300 microM GDP and 0.1 nM [35S]GTPgammaS, incubated at 37 degrees C for 20 min. At 10 microM, the 5-HT1A receptor agonist R(+)-8-hydroxy-2-(di-n-propylamino)tetralin [R(+)-8-OH-DPAT] stimulated GTPgammaS binding from 27.1 +/- 2.5 to 45.7 +/- 4.2 fmol/mg protein. Increasing the protein concentration did not affect the absolute difference between basal and maximal GTPgammaS binding nor the EC50, but decreased the percent stimulation. The non-selective agonists serotonin and 5-carboxamidotryptamine were 30-35% more efficacious, whereas the partial agonists buspirone and S(-)-8-hydroxy-2-(di-n-propylamino)tetralin stimulated GTPgammaS binding by 19 +/- 1 and 43 +/- 3%, respectively, compared to R(+)-8-OH-DPAT. Neither the 5-HT2 receptor agonist [(+/-)1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane HCl] (DOI) nor the 5-HT1A receptor antagonists WAY 100,635 (n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride) and spiperone altered basal GTPgammaS binding. WAY 100,635 abolished the effect of R(+)-8-OH-DPAT, but only reduced the effect of serotonin by 88 +/- 3%. Finally, methiothepin antagonized R(+)-8-OH-DPAT-stimulated GTPgammaS binding and reduced basal GTPgammaS binding by itself. The reduction was not affected by WAY 100,635. We have characterized a method to assess functional activity at 5-HT1A receptors in rat hippocampal membranes by measuring agonist-induced [35S]GTPgammaS binding.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Alper RH,Nelson DLdoi
10.1016/s0014-2999(97)01547-1subject
Has Abstractpub_date
1998-02-19 00:00:00pages
303-12issue
2-3eissn
0014-2999issn
1879-0712pii
S0014-2999(97)01547-1journal_volume
343pub_type
杂志文章abstract：:In cultured rat heart muscle cells, reversible long-term ATP depletion induces a decrease in beta-adrenoceptor density and a fall in isoproterenol- as well as forskolin-stimulated cAMP formation. However, isoproterenol-stimulated adenylyl cyclase activity in membrane preparations is not reduced after ATP depletion. Th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90104-p
更新日期：1991-11-13 00:00:00
abstract：:Intravenous baclofen (1 mg/kg) abolished or severely attenuated the high threshold late component (but not the low threshold early component of long duration (greater than 150 msec) discharges evoked in cat dorsal horn neurons by intense transcutaneous electrical stimulation. Baclofen similarly reduced the spontaneous...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90463-1
更新日期：1979-02-01 00:00:00
abstract：:We report positron emission tomography studies of beta-adrenoceptors in the human thorax with (S)-[(11)C]CGP12388 (4-(3-(2'-[(11)C]-isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one). Beta-adrenoceptors have previously been quantified using (S)-[(11)C]CGP12177 (4-(3-tert-butylamino-2-hydroxypropoxy)-2H-benzimida...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01499-6
更新日期：2001-12-21 00:00:00
abstract：:The pharmacological nature of nicotine-induced contraction in the rat basilar artery is poorly understood. The purpose of this study was to investigate the endothelium dependency and involvement of arachidonic acid metabolites in nicotine-induced contraction in the rat basilar artery. The rat basilar artery was remove...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.08.011
更新日期：2007-12-22 00:00:00
abstract：:Rheumatoid Arthritis is a chronic autoimmune disease with a complex disease pathogenesis leading to inflammation and destruction of synovial tissue in the joint. Several molecules lead to activation of immune pathways, including autoantibodies, Toll-Like Receptor ligands and cytokines. These pathways can cooperate to ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.03.085
更新日期：2016-05-05 00:00:00
abstract：:Inhibition of local cortisol regeneration from circulating cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the risk factors associated with the metabolic syndrome. Chronic modulation of glucocorticoid homeostasis may result in hypothalamic-pituitary-adrenal (HPA) axis s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.07.004
更新日期：2016-10-15 00:00:00
abstract：:Apolipoprotein B (ApoB) of low-density lipoprotein (LDL) causes endothelial dysfunction in the initial stage of atherogenesis. The present study was designed to explore the underlying molecular mechanisms involved. Rat mesenteric arteries were organ cultured in the presence of different concentrations of ApoB or LDL. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.008
更新日期：2014-02-15 00:00:00
abstract：:The effects of intra- and extraluminal capsaicin administration were evaluated in isolated perfused rat mesenteric bed. Capsaicin (10 nM-1 microM) produced a potent concentration-dependent relaxation of the tonic vasoconstriction induced by norepinephrine (1 microM) but not by high-K+ (60 mM). The capsaicin-induced re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90559-6
更新日期：1988-03-29 00:00:00
abstract：:The amyloid precursor protein (APP) has been mainly studied in its role in the production of amyloid β peptides (Aβ), because Aβ deposition is a hallmark of Alzheimer's disease. Although several studies suggest APP has physiological functions, it is still controversial. We previously reported that APP increased glial ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.09.015
更新日期：2011-01-10 00:00:00
abstract：:1,2,3,4-Tetrahydroisoquinoline (TIQ) is an exo- and endogenous amine naturally present in mammalian brain which displays antidepressant-like effect in various animal models: the forced swim test (FST) and chronic mild stress (CMS) paradigm in rats. To elucidate this action we compared the effects of TIQ with imipramin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.075
更新日期：2014-04-15 00:00:00
abstract：:(±)-3,4-Methylenedioxymethamphetamine (MDMA) is an illicit drug that evokes transporter-mediated release of serotonin (5-HT) in the brain. 5-HT transporter (SERT) proteins are also expressed in non-neural tissues (e.g., blood), and evidence suggests that MDMA targets platelet SERT to increase plasma 5-HT. Here we test...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.10.033
更新日期：2012-01-15 00:00:00
abstract：:The effects of delta9-THC and its ethanol vehicle on pilocarpine-induced parotid gland secretions were investigated in rats. Single doses of delta9-THC (1, 2.5, 5 and 10 mg/kg) or 95% ethanol were administered i.v. prior to pilocarpine stimulation of saliva. Total flow, alpha-amylase and cation content of the induced ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90071-6
更新日期：1976-12-01 00:00:00
abstract：:The effects of clonidine and dl-propranolol on negative pressure breathing-induced diuresis in chloralose-anaesthetized dog were studied. Clonidine (10 microgram/kg i.v.) suppressed the diuretic response, whereas dl-propranolol (1 mg/kg i.v.) was inactive. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90579-3
更新日期：1981-07-10 00:00:00
abstract：:Knockdown of spinal metabotropic glutamate 5 (mGlu5) receptor was shown to inhibit the development of intrathecal morphine antinociceptive tolerance. The present work was designed to evaluate the expression of spinal G-protein during morphine tolerance and knockdown of spinal mGlu5 receptor with antisense oligonucleot...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.11.024
更新日期：2014-01-15 00:00:00
abstract：:Previously reported work has provided evidence that arylazido aminopropionyl ATP (ANAPP3), a P2-receptor antagonist, blocks the effects of ATP and other purine analogs, in the urinary bladder of the cat. This antagonism appeared limited to those effects mediated by P2-receptors, such as contraction of the urinary blad...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90476-0
更新日期：1986-01-29 00:00:00
abstract：:In previous studies using Fos expression as a marker of neuronal activation, we showed that nitrous oxide (N(2)O) activates bulbospinal noradrenergic neurons in rats and that destruction of these neuronal pathways leads to loss of N(2)O antinociceptive action. Based on previous rat studies it has been proposed that th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01193-1
更新日期：2001-09-07 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
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90184-6
更新日期：1986-10-14 00:00:00
abstract：:The acetylcholine receptor agonists, acetylcholine (10(-5)-10(-4 M), carbachol (5 x 10(-6)-5 x 10(-5) M), bethanechol (5 x 10(-5)-5 x 10(-4) M) and dimethylphenylpiperazinium (DMPP, 10(-5) M) increased the short-circuit current (Isc) in the rat colon descendens by a tetrodotoxin (TTX)-sensitive mechanism. Blockade by ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90568-2
更新日期：1989-09-13 00:00:00
abstract：:Using a number of agonist and antagonist compounds, we attempted to characterize the responses and receptors involved in the effects of 5-hydroxytryptamine (5-HT) in the in situ blood perfused rat mesentery. An intra-arterial (i.a.) bolus injection of 5-HT increased mesenteric perfusion pressure in a dose-dependent wa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00444-1
更新日期：2000-08-04 00:00:00
abstract：:Existing antimuscarinic drugs for overactive bladder have high affinity for M(3)/M(1) muscarinic receptors and consequently produce M(3)/M(1)-mediated adverse effects including dry mouth, constipation, mydriasis and somnolence. TD-6301 is a M(2/4) muscarinic receptor-selective antagonist developed for the treatment of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.12.043
更新日期：2009-03-01 00:00:00
abstract：:Ro 40-5967 [(1S,2S)-2-[2[3-(2-benzamidopropyl]- methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl- methoxyacetate] is a new Ca2+ channel antagonist active at L-type channels. Radioligand binding studies in cardiac tissue show that Ro 40-5967 does not inhibit 1,4-dihydropyridine binding, but does in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00194-p
更新日期：1995-07-04 00:00:00
abstract：:Intracellular accumulation of Mn2+ augmented the contractions induced by norepinephrine and acetylcholine in the guinea pig isolated vas deferens. Contractions repeatedly induced by norepinephrine, acetylcholine, or a high concentration of K+ decreased depending on the incubation time in Ca(2+)-free medium. The rate o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00664-8
更新日期：1996-01-11 00:00:00
abstract：:The administration of the synthetic and stable opioid peptide[D-Ala2,MePhe4,Met(O)5o1]enkephalin (FK 33-824) at the dose of 0.2 mg/kg i.v. induced a rise in plasma levels of prolactin in the rat, an effect which was prevented by 1 mg/kg i.v. of the opiate antagonist naloxone. A simultaneous i.v. injection of 20 microg...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90009-7
更新日期：1982-01-22 00:00:00
abstract：:Cannabinoid CB(2) receptors have been implicated in antinociception in animal models of both acute and chronic pain. We evaluated the role both cannabinoid CB(1) and CB(2) receptors in mechanonociception in non-arthritic and arthritic rats. The antinociceptive effect of Delta(9)-tetrahydrocannabinol (Delta(9)THC) was ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.05.024
更新日期：2007-09-10 00:00:00
abstract：:We have reported that tacrolimus (FK506), an immunosuppressive drug, and diclofenac, a non-steroidal anti-inflammatory drug, possess different modes of neuroprotective action. FK506 suppresses only thapsigargin-induced apoptosis in neuroblastoma SH-SY5Y cells while diclofenac reverses tunicamycin-induced as well as th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.07.027
更新日期：2011-11-01 00:00:00
abstract：:To investigate the putative rewarding effects of atomoxetine, a non-stimulant medication for Attention-deficit/hyperactivity disorder (ADHD), we conducted conditioned place preference (CPP) tests in an animal model of ADHD, the spontaneously hypertensive rat (SHR). The effects of drug pre-exposure were also evaluated,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.05.057
更新日期：2011-09-30 00:00:00
abstract：:The biodistribution of S-(-)-4-(2-hydroxy-3-(1'-[18F]fluoroisopropyl)- aminopropoxy)carbazole ([18F]S-fluorocarazolol, a non-selective beta-adrenoceptor antagonist) was studied in rats (60 min after 18F injection when specific binding in peripheral organs was maximal). 18F uptake in brain, erythrocytes, heart and lung...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00636-l
更新日期：1995-01-16 00:00:00
abstract：:T-kinin and its putative carboxypeptidase product des-Arg(11)-T-kinin are members of the kinin family that are unique to the rat. Primary cultures of rat bladder smooth muscle cells were used to investigate the pharmacology of these peptides. Calcium imaging experiments showed that rat bladder smooth muscle cells resp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02102-7
更新日期：2002-08-23 00:00:00
abstract：:The increases in activity of hepatic thymidylate synthetase and of thymidine kinase, which catalyze the formation of thymidylate via the de novo and salvage pathways, respectively, were significantly suppressed during liver regeneration in rats which had been given alpha-adrenoceptor antagonists (phenoxybenzamine and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90380-2
更新日期：1985-08-27 00:00:00
abstract：:This study investigates the effects of benzodiazepine receptor inverse agonists on the locomotor and exploratory behaviour of mice when tested in a familiar environment. The weak partial inverse agonist Ro 15-3505 (0.3, 1, 3 mg/kg i.p.) significantly increased locomotion and hole-dipping in habituated mice. However, t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90701-5
更新日期：1992-10-20 00:00:00
