Abstract：
:The mechanism by which dibutyryl cyclic AMP (db-cAMP) induces vasodilatation was examined in isolated rat aorta. The contraction induced by norepinephrine (NE) was more sensitive to the inhibitory effect of db-cAMP than that induced by high K+, and the contraction induced by lower concentrations of each stimulant was more sensitive to db-cAMP than that induced by higher concentrations. Db-cAMP at 10 microM inhibited the increases in muscle tension and cytosolic Ca2+ level ([Ca2+]i) without changing the [Ca2+]i-tension relationship, suggesting that the inhibitory effect is mainly due to a decrease in [Ca2+]i. A higher concentration (300 microM) of db-cAMP inhibited muscle tension more strongly than [Ca2+]i suggesting that db-cAMP decreases Ca2+ sensitivity of contractile elements. In contrast, 10 microM verapamil inhibited the NE-stimulated [Ca2+]i more strongly than the NE-induced contraction. The verapamil-insensitive portion of the NE-stimulated [Ca2+]i and contraction was inhibited by db-cAMP, suggesting that db-cAMP and verapamil act by different mechanisms. In Ca(2+)-free solution, 1 microM NE induced transient increases in muscle tension and [Ca2+]i. The transient contraction was inhibited by 1 mM db-cAMP more strongly than [Ca2+]i. An activator of adenylate cyclase, forskolin, showed inhibitory effects similar to those of db-cAMP. The inhibitory effects of db-cAMP and forskolin were inversely proportional to [Ca2+]i before the addition of these inhibitors. These results suggest that db-cAMP inhibits smooth muscle contraction by decreasing [Ca2+]i and the Ca2+ sensitivity of contractile elements, and that both of these effects are stronger when [Ca2+]i is lower.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Abe A,Karaki Hdoi
10.1016/0014-2999(92)90385-hkeywords:
subject
Has Abstractpub_date
1992-02-18 00:00:00pages
305-11issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(92)90385-Hjournal_volume
211pub_type
杂志文章abstract：:The recovery of the muscarinic cholinergic receptor (mAChR) from its down-regulation by long-term exposure to ACh was investigated. This was done to obtain information about regulation of the mAChR. Exposure of guinea-pig vas deferens to 30 microM ACh for 24 h decreased the amount of mAChR to 30% of the initial level,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90417-0
更新日期：1985-02-26 00:00:00
abstract：:Our previous studies demonstrated the ability of exogenous agmatine to inhibit tolerance to and physical dependence on morphine in mice, rats and monkeys. The present study further evaluated the effect of agmatine on the psychological dependence induced by morphine in conditioned place preference assay. Agmatine (0.75...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.03.045
更新日期：2005-05-16 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：:Immunocytochemical and Co(2+) uptake studies revealed that in primary cultures of rat cortical neurones, the majority of neurones are gamma-aminobutyric acid (GABA) immunopositive and can express Ca(2+)-permeable alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors. By fura-2 microfluorimetry, it...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01296-7
更新日期：2002-03-01 00:00:00
abstract：:The aim of the present study was to find out the mechanism by which the inflammatory mediator, bradykinin, induces an increase of the cytosolic Ca(2+) concentration ([Ca(2+)](i)) in enteric neurons. For this purpose, ganglia in the isolated submucosa from rat colon were loaded with the Ca(2+)-sensitive dye, fura-2, an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.02.001
更新日期：2012-04-15 00:00:00
abstract：:Leukocytes can generate a substance that, when added to some partially purified human kininogen, is capable of forming kinins. The addition of endotoxin or polystyrene latex particles to the incubated leukocytes doubled the amount of kinin generated. Certain preparations of kininogen, however, failed to allow kinin fo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90137-5
更新日期：1975-08-01 00:00:00
abstract：:The kinetic and equilibrium binding properties of the 1,4-dihydropyridine activator [3H](-)-S-Bay K 8644 and the antagonist [3H](+)-PN 200-110 were determined in rat heart membrane particulate preparations at temperatures between 4 and 37 degrees C. The binding of [3H](-)-S-Bay K 8644 was temperature-dependent with a ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90064-o
更新日期：1991-10-14 00:00:00
abstract：:In this study the desensitizing power of increasing concentrations of resiniferatoxin applied topically to the bladder mucosa, and the irritating properties of the most effective desensitizing dose, were determined with the aid of the spinal expression of the proto-oncogene c-fos. Desensitization was assessed by the d...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00451-3
更新日期：1999-07-28 00:00:00
abstract：:Statins are the most common type of medicine used to treat hypercholesterolemia; however, they are associated with a low incidence of myotoxicity such as myopathy and rhabdomyolysis. The mechanisms for the adverse effects remain to be fully elucidated for safer chronic use and drug development. The results of our earl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.10.044
更新日期：2012-01-15 00:00:00
abstract：:To study the role of K(+) channels in the coronary and renal vascular response to vasopressin during diabetes mellitus, and whether there are gender differences in this role, we have examined the isometric response to this peptide of 2-mm-long arterial segments from male and female, normoglycemic and streptozotocin-in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01815-6
更新日期：2003-06-13 00:00:00
abstract：:A close relationship between the renin-angiotensin system and the pathophysiology of diabetic retinopathy has been suggested, several angiotensin II type 1 receptor (angiotensin AT1 receptor) antagonists being effective in animal models. Therefore, we examined the efficacy of an angiotensin AT1 receptor antagonist, ol...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.02.047
更新日期：2005-04-11 00:00:00
abstract：:Herein, we report an extensive investigation of the neuroprotective effects of the compound (Z)-alpha-[2-thiazol-2-yl)imidazol-4-yl]-N-tert-butylnitrone (S34176) and the prototypic nitrone alpha-phenyl-N-tert-butylnitrone (PBN), in different in vivo paradigms of neuronal degeneration. Administration of S34176 (75 mg/k...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.01.043
更新日期：2005-03-28 00:00:00
abstract：:Activated microglia that produce reactive nitrogen species (RNS), inflammatory factors, reactive oxygen species (ROS), and other neurovirulent factors may lead to the development of neurodegenerative diseases. Certain compounds can inhibit the activation of microglia. However, these mechanisms remain unclear. In the p...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.03.029
更新日期：2016-06-05 00:00:00
abstract：:We have assessed the utility of the Cytosensor microphysiometer for studying the pharmacology of recombinant CRF receptors. Chinese hamster ovary cells stably expressing the human CRF1 or CRF2 receptor were perfused in the Cytosensor with bicarbonate-free Hams F12 (pH 7.4) containing 0.2% bovine serum albumin. The ran...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00506-3
更新日期：1999-08-27 00:00:00
abstract：:This study was designed to investigate the effect and mechanism of allicin on hyperhomocysteinemia-induced experimental vascular endothelial dysfunction in rats. Fifty male Wistar rats were randomly divided into five groups: the normal control rats (NC), the high-methionine-diet rats (Met), the high-methionine-diet ra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.05.038
更新日期：2013-08-15 00:00:00
abstract：:The ligand preferences of recombinant NR1 homomeric and NR1-NR2 heteromeric NMDA receptors were examined by homogenate binding assay. The binding affinities for most ligands were similar to those reported for native NMDA receptors. The order of affinity for [3H]glutamate was NR1-NR2B > NR1-NR2A approximately NR1-NR2D ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90058-2
更新日期：1994-08-16 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
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172441
更新日期：2019-08-15 00:00:00
abstract：:Behaviors induced in mice by intrathecal injections of either N-methyl-D-aspartate (NMDA) or kainic acid are modulated by NH2-terminal fragments of substance P, such as substance P-(1-7). The action of substance P-(1-7) on kainic acid depends on sigma receptor activity. The present study was designed to test the hypot...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00199-9
更新日期：1996-06-13 00:00:00
abstract：:The acute administration of MDMA has been shown to promote glycogenolysis and increase the extracellular concentration of glucose in the striatum. In the present study the role of serotonergic and/or noradrenergic mechanisms in the MDMA-induced increase in extracellular glucose and glycogenolysis was assessed. The rel...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.07.004
更新日期：2010-10-10 00:00:00
abstract：:R-isovaline is a non-proteinogenic amino acid which produces analgesia in a range of nociceptive assays. Mediation of this effect by metabotropic receptors for γ-aminobutyric acid (GABA) and glutamate, demonstrated by previous work, may depend on the type of tissue or receptor system. The objective of this study was t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.08.005
更新日期：2016-11-15 00:00:00
abstract：:The kinetics of [3H]dexetimide dissociation from muscarine receptors in bovine cardiac left ventricular and tracheal smooth muscle membranes were studied in the absence and presence of three muscarine antagonists. It was found that [3H]dexetimide dissociation from cardiac muscarine receptors was monophasic and very fa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(89)90045-x
更新日期：1989-03-07 00:00:00
abstract：:The quantitative [14C]2-deoxyglucose autoradiographic technique was applied to the measurement of the cerebral metabolic effects of adenosine A1 and A2 receptor agonists and antagonists in adult rats. The adenosine A1 receptor agonist and antagonist, 2-chloro-N6-cyclopentyladenosine (CCPA) and 8-cyclopentyl-1,3-diprop...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90057-4
更新日期：1994-06-02 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：:Metabotropic glutamate receptors (mGlu receptors), with their unique signaling systems and pharmacological characteristics, have emerged as a new topic in excitatory amino acid research. Among them, the unique distribution of group II mGlu receptors, such as mGlu(2) and mGlu(3) receptors, and the involvement of these ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.12.041
更新日期：2010-08-10 00:00:00
abstract：:Using the ex vivo chick embryo retina to study the efficacy of antagonists in blocking the excitotoxic effects of excitatory amino acid agonists, we previously identified phencyclidine as the most powerful known anti-excitotoxin. Here we show that MK-801 is 5 times more powerful than phencyclidine as an anti-excitotox...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90552-8
更新日期：1987-09-23 00:00:00
abstract：:The human cholecystokinin B (CCKB) receptor has been isolated from a human temporal cortex cDNA library. Transient transfection of the receptor into COS-M6 cells resulted in high specific binding of 125I-sulphated CCK-8 labelled with Bolton and Hunter Reagent (KD = 31 pM). Competition experiments yielded the expected ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90117-1
更新日期：1994-06-15 00:00:00
abstract：:The cell adhesion molecules N-, VE- and OB-cadherin have been implicated as regulators of tumor growth and metastasis. We discuss evidence that N- and VE-cadherin play a key role in promoting blood vessel formation and stability, processes which are essential for tumor growth. Secondly, we describe the potential invol...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.05.033
更新日期：2009-12-25 00:00:00
abstract：:In many vascular smooth muscle cells, physiological and pharmacological agonists initiate oscillatory fluctuations in intracellular Ca(2+) to initiate and maintain vasoconstriction. These oscillations are supported by the underlying cellular ultrastructure, particularly the close apposition between the plasma membrane...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.11.055
更新日期：2010-03-10 00:00:00
abstract：:This review selectively explores some areas of pain research that, until recently, have been poorly understood. We have chosen four topics that relate to clinical pain and we discuss the underlying mechanisms and related pathophysiologies contributing to these pain states. A key issue in pain medicine involves crucial...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2013.01.069
更新日期：2013-09-15 00:00:00
abstract：:Soluble amyloid β-protein (Aβ) oligomers are primary mediators of synaptic dysfunction associated with the progression of Alzheimer's disease. Such Aβ oligomers exist dependent on their rates of aggregation and metabolism. Use of selective somatostatin receptor-subtype agonists have been identified as a potential mean...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.03.020
更新日期：2012-05-15 00:00:00
