Abstract：
:The specific, irreversible binding of [3H]beta-funaltrexamine (beta-FNA) to mu opioid receptors in slices from the corpus striatum and midbrain region containing the ventral tegmentum area (VTA) was accomplished by incubation with [3H]beta-FNA followed by a washing procedure with 1 microM unlabeled naltrexone in the washing medium. Regional distribution studies of the specific, irreversible binding of [3H]beta-FNA revealed that slices of striatum and midbrain were richest in mu opioid receptors. Slices of cerebral cortex and medulla-pons had much lower amounts and the cerebellum had virtually no mu opioid receptors. Examination of the kinetics of the specific, irreversible binding of [3H]beta-FNA revealed that although the maximum binding of beta-FNA to striatal and midbrain slices of control and morphine tolerant/dependent mice did not differ, the rate at which beta-FNA associated with the receptor was increased in the slices from morphine tolerant/dependent animals. The increase in association probably occurred at the initial recognition step before alkylation takes place and is attributable to an increase in affinity of mu opioid receptors for beta-FNA in both the striatal and midbrain regions of morphine tolerant/dependent mice. This finding supports and expands earlier conclusions that the affinity of mu opioid receptors for opioid antagonists is increased during the development of opiate tolerance and dependence in mice.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Takahashi M,Portoghese PS,Takemori AEdoi
10.1016/0014-2999(88)90650-4subject
Has Abstractpub_date
1988-05-10 00:00:00pages
205-12issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(88)90650-4journal_volume
149pub_type
杂志文章abstract：:The effects of intra-amygdalar neuropeptide Y infusions were assessed in rats using the social interaction test. Neuropeptide Y administered into the central nucleus of the amygdala did not alter behavior, while injections into the basolateral nucleus of the amygdala produced an increased social interaction time. Furt...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00018-7
更新日期：1999-03-05 00:00:00
abstract：:We investigated the effects of 1-amino-5-bromouracil on the benzodiazepine-gamma-aminobutyric acid (GABA)A receptor complex to elucidate its central action. 1-Amino-5-bromouracil neither displaced nor enhanced [3H]muscimol, [35S]t-butylbicyclophosphorothionate (TBPS), or [3H]dehydroepiandrosterone sulfate binding to t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90278-x
更新日期：1994-12-12 00:00:00
abstract：:5-HT(1A) receptor activation by the very-high-efficacy, selective 5-HT(1A) receptor agonist F 13640 [(3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-([(5-methyl-pyridin-2-ylmethyl)-amino]-methyl)piperidin-1-yl]-methanone] was recently discovered to constitute a novel central mechanism of broad-spectrum analgesia that, remarkab...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01566-8
更新日期：2003-04-18 00:00:00
abstract：:Recently, it has been suggested that bumetanide, an inhibitor of the Na-K-2Cl co-transporter (NKCC1), may be useful in the treatment of central nervous system (CNS) disorders. However, from a physicochemical perspective, bumetanide may not cross the blood-brain barrier to the extent that is necessary for it to be an e...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.12.001
更新日期：2016-01-05 00:00:00
abstract：:Adenosine (10 micrograms kg-1 min-1, infused into the lumen of the left ventricle) and dipyridamole (0.25 mg kg-1 intravenously, a dose that potentiated markedly the fall in arterial pressure in response to bolus doses of adenosine) each reduced the number of extrasystoles which occurred during the first 30 minutes fo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90229-4
更新日期：1988-01-12 00:00:00
abstract：:The alpha7 (α7) nicotinic acetylcholine receptor is a therapeutic target for cognitive disorders. Here we describe 3-(3,4-difluorophenyl)-N-(1-(6-(4-(pyridin-2-yl)piperazin-1-yl)pyrazin-2-yl)ethyl)propanamide (B-973), a novel piperazine-containing molecule that acts as a positive allosteric modulator of the α7 recepto...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.01.037
更新日期：2017-03-15 00:00:00
abstract：:In incubation medium containing Na+ as the only cation, the specific binding of [3H]cocaine to a membrane preparation obtained from rat striatum reached a maximal level for 10 mM Na+, whereas higher concentrations decreased its affinity. The specific binding of [3H]cocaine was inhibited monophasically by GBR 12783, ma...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90188-0
更新日期：1994-07-15 00:00:00
abstract：:We studied the interaction of S-methylisothiourea (a selective inducible nitric oxide synthase inhibitor) with rofecoxib (a selective cyclooxygenase-2 inhibitor) and mefenamic acid (a non-selective cyclooxygenase inhibitor) in adjuvant-induced arthritis in female albino Wistar rats, applying the isobolographic analysi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.10.047
更新日期：2007-02-05 00:00:00
abstract：:Selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N- (methylsulfonyl)acetamide]) is a novel, orally available non-prostanoid prostacyclin receptor (IP receptor) agonist that has recently been approved for the treatment of pulmonary arterial hypertension (PAH). We examined the effect of the a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.057
更新日期：2017-01-15 00:00:00
abstract：:Ovarian cancer is the leading cause of death among gynecologic cancer patients. Although platinum-based chemotherapy as a frontline treatment for ovarian cancer has been widely used in clinical settings, its clinical efficacy is not satisfactory due to the resistance of ovarian cancer cells to apoptosis. Therefore, it...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173526
更新日期：2020-11-05 00:00:00
abstract：:Cocaine dependence continues to be a worldwide public health concern. Although the majority of individuals reporting cocaine use do so via the intranasal route, relatively few laboratory experiments have examined the reinforcing effects of cocaine administered intranasally. The purpose of this experiment was to measur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.06.055
更新日期：2010-10-10 00:00:00
abstract：:Mitochondria play a central role in cell biology not only as producers of ATP, but also in the sequestration of Ca(2+) and the generation of free radicals. They are also repositories of several proteins which regulate apoptosis. Perturbations in the normal functions of mitochondria will inevitably disturb cell functio...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0014-2999(02)01842-3
更新日期：2002-07-05 00:00:00
abstract：:alpha 2-adrenoceptor-mediated contractions of the rabbit saphenous vein were previously found to be inhibited by wortmannin, a protein kinase inhibitor which blocks receptor-dependent phospholipase D activation. Since other studies have indicated that receptor-dependent phospholipase D activation required activity of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00053-n
更新日期：1995-04-13 00:00:00
abstract：:The nature and specificity of the effect of histamine H1- and H2-receptor antagonists on the uptake of serotonin (5HT), norepinephrine (NE) and dopamine (DA) were studied in rat forebrain synaptosomes. Low concentrations (0.05-0.50 microM) of the H1-antagonist, pyrilamine, competitively inhibited 5HT uptake (Ki = 0.09...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90213-7
更新日期：1980-07-11 00:00:00
abstract：:Although a number of muscarinic agonists have been used in clinical trials for Alzheimer's Disease, many of these compounds are low in potency and have only limited intrinsic efficacy. The present study describes four non-quaternary oxadiazole based muscarinic agonists from a quinuclidine and a 1-azanorbornane series....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90006-r
更新日期：1990-10-09 00:00:00
abstract：:Transient ischemia was produced for 15 min by occlusion of the middle cerebral artery in halothane-anesthetized rats, and changes in the extracellular concentrations of neurotransmitter monoamines and amino acids were examined in the striatum. The occlusion produced marked increases in the extracellular concentrations...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.11.006
更新日期：2004-01-26 00:00:00
abstract：:The non N-methyl-D-aspartate (NMDA) receptor antagonists dinitroquinoxaline-2,3-dione (DNQX) and 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), both inhibit the visually driven response of sustained ganglion cells in the cat retina in vivo. In contrast to these findings, the potent NMDA receptor antagonist 3-[+/- )-2-ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90483-4
更新日期：1989-05-19 00:00:00
abstract：:Transient outward K+ current, Ito, contributes to cardiac action potential generation and is primarily carried by Kv4.3 (KCND3) channels. Two Kv4.3 isoforms are expressed in human ventricle and show differential remodeling in heart failure (HF). Lidocaine and mexiletine may be applied in selected patients to suppress ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173159
更新日期：2020-08-05 00:00:00
abstract：:The aim of this study has been to investigate the antiplatelet activity of a new series of thienylacylhydrazone derivatives analogous to the lead compound LASSBio-294 ((2-thienylidene) 3,4-methylenedioxybenzoylhydrazine). The antiplatelet effect was investigated in rabbit and human platelet rich plasma stimulated by a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.003
更新日期：2010-07-25 00:00:00
abstract：:Several studies have shown that glycine transporter 1 (GlyT1) inhibitors have anxiolytic actions. There are two types of glycine receptor: the strychnine-sensitive glycine receptor (GlyA) and the strychnine-insensitive glycine receptor (GlyB); however, which receptor is the main contributor to the anxiolytic actions o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.11.024
更新日期：2015-01-05 00:00:00
abstract：:The actions of 5-hydroxytryptamine have been studied in the chick biventer cervicis nerve--muscle preparation. At concentrations between 2.5 X 10(-3) and 3.7 X 10(-3) M, 5HT produced a transient increase in responses to indirect stimulation, but not to direct stimulation. At higher concentrations, 5HT produced a rever...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90095-4
更新日期：1977-07-15 00:00:00
abstract：:Pyrrolidine dithiocarbamate (PDTC) can form a complex with metal ions and then act as a proteasome inhibitor, which leads to tumor cell apoptosis, and could therefore be developed as an anticancer agent. In our efforts to find factors that induce PDTC-mediated apoptosis of tumor cells, the effect of serum concentratio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.09.048
更新日期：2010-12-15 00:00:00
abstract：:Inhibitory effects of the saponin fraction and its principal constituents, escins Ia, Ib, IIa, and IIb, from horse chestnuts on gastric emptying were investigated in mice loaded with a non-nutrient or nutrient meal. The saponin fraction and escins Ia-IIb inhibited gastric emptying of a 1.5% carboxymethyl cellulose sod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00035-7
更新日期：1999-03-05 00:00:00
abstract：:NP-252, a new dihydropyridine derivative, and nifedipine non-competitively inhibited contractile responses to KCl and responses to Ca2+ in Ca(2+)-free medium containing KCl in rabbit aorta and renal, mesenteric, coronary and basilar arteries, mesenteric veins and vena cava. The effects of NP-252 in these smaller arter...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90888-w
更新日期：1991-10-22 00:00:00
abstract：:Diabetic nephropathy is a progressive kidney disorder and is pathologically characterized by thickened glomerular and tubular basement membranes, accumulation of the extracellular matrix and increased mesangial hypertrophy. Growing evidence has suggested that diabetic nephropathy is induced by multiple factors, such a...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.04.017
更新日期：2015-08-05 00:00:00
abstract：:In guinea pig papillary muscle, the rate of electrical stimulation (0.1-2 Hz) strongly influenced the effects of the Anemonia sulcata toxin ATX II on action potential duration (APD) and contractile force. In the concentration range studied (10-8-10-7 M), ATX II always produced a larger prolongation in APD at low rates...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90632-x
更新日期：1982-04-23 00:00:00
abstract：:Increasing evidence displays that microRNAs (miRNAs) participate in the development of various human malignancies, including esophageal squamous cell carcinoma (ESCC). MicroRNA-33a-5p (miR-33a-5p) has recently been reported to function as a tumor suppressor in many human cancers. However, the expression and role of mi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172590
更新日期：2019-10-15 00:00:00
abstract：:The effects of capsaicin pretreatment on withdrawal responses of guinea-pig isolated ileum to [Met5]enkephalin (ME) and morphine and on the locomotor withdrawal response of guinea-pigs following a single dose of morphine, were investigated. In vitro treatment of ileum with capsaicin, 1.5 mumol/l for 1 h, did not signi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90257-9
更新日期：1988-12-06 00:00:00
abstract：:The interaction of 5 alpha-pregnane-3 alpha-ol-20-one (5 alpha 3 alpha P), a progesterone metabolite, with the GABAA receptor chloride channel complex was investigated at the pituitary level. In nanomolar concentrations this steroid potentiated the inhibitory effect of muscimol (a GABAA agonist) on prolactin release f...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90627-4
更新日期：1989-09-01 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
