Abstract:
:Peripheral type benzodiazepine receptors are differentially modified by arachidonate, diethylpyrocarbonate and thiol reagents, as evidenced by the finding that binding of a proposed agonist ([3H]R05-4864) and a proposed antagonist ([3H]PK 11195) to rat kidney mitochondrial membranes can be modified separately. (1) Arachidonate significantly lowered the affinity of the peripheral-type benzodiazepine receptor for R05-4864 and diazepam but did not alter the affinity for PK 11195 and only slightly altered for dipyridamole. In contrast, diethylpyrocarbonate inhibited [3H]PK 11195 binding by 43% while reducing [3H]R05-4864 binding only 16%. (2) Diethylpyrocarbonate treatment causes a reduction in affinity for both dipyridamole and PK 11195, did not change the affinities for R05-4864 and diazepam but increased the affinities for diuretics. PK 11195, R05-4864 and dipyridamole totally protected peripheral benzodiazepine receptors against inactivation by diethylpyrocarbonate. In contrast, diethylpyrocarbonate inactivation of [3H]PK 11195 binding was increased after preincubation of peripheral benzodiazepine receptors with metolazone. Arachidonate both lowers the affinity for [3H]R05-4864 and eliminated the ability of R05-4864 to protect peripheral benzodiazepine receptors against inactivation by diethylpyrocarbonate. (3) Among different thiol reagents, only dithiothreitol treatment resulted in 26 and 43% inhibition of [3H]PK 11195 and [3H]R05-4864 binding, respectively. These results indicate that the peripheral-type benzodiazepine receptor molecule possesses at least two different conformations or separate mutually exclusive sites for agonists and antagonists. Additionally, the interaction of the thiazide class of diuretics with peripheral-type benzodiazepine receptors seems to require binding sites on the receptor molecule in addition to those for specific agonist and antagonist, whereas dipyridamole appears to bind to the antagonist site or conformation.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Skowroński R,Beaumont K,Fanestil DDdoi
10.1016/0014-2999(87)90454-7subject
Has Abstractpub_date
1987-11-17 00:00:00pages
305-14issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(87)90454-7journal_volume
143pub_type
杂志文章abstract::Endothelin-1-(1-31) is a new bioactive 31-amino-acid-length peptide generated from big endothelin-1 by chymase or other chymotrypsin-type proteases with various pathophysiologic functions. In this study, we have detected the specific and monophasic binding of [125I]endothelin-1-(1-31) in porcine lung membranes. Compet...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(03)01454-7
更新日期:2003-03-28 00:00:00
abstract::G protein-coupled receptors (GPCRs) are a family of membrane receptors that regulate physiology and pathology of various organs. Consequently, about 40% of drugs in the market targets GPCRs. Heterotrimeric G proteins are composed of α, β, and γ subunits, and act as the key downstream signaling molecules of GPCRs. The ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2015.05.016
更新日期:2015-09-15 00:00:00
abstract::(5R)-5-hydroxytriptolide (LLDT-8) exhibits strong immunosuppressive activities in vitro and in vivo. Here, we investigated the effects of LLDT-8 on concanavalin A-induced hepatitis. Liver damage was evaluated by serum alanine transaminase (ALT) level and liver histology. The effects of LLDT-8 were determined by measur...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.03.013
更新日期:2006-05-10 00:00:00
abstract::The binding characteristics of [3H]gabapentin, the radiolabelled analogue of the novel anticonvulsant gabapentin (1-(aminomethyl)cyclohexaneacetic acid) were studied using purified synaptic plasma membranes prepared from rat cerebral cortex. In 10 mM HEPES buffer [3H]gabapentin bound to a single population of sites wi...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(93)90155-3
更新日期:1993-02-15 00:00:00
abstract::The effects on rat serum prolactin level of the two isomers constituting the racemic form of amisulpride were compared. (S-)-amisulpride induced hyperprolactinemia at lower doses (ED(50) = 0.09 +/- 0.01 mg/kg) than racemic- (ED(50) = 0.24 +/- 0.03 mg/kg) and (R+)-amisulpride (ED(50) = 4.13 +/- 0.05 mg/kg), in accord w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01990-8
更新日期:2002-07-19 00:00:00
abstract::The stable gastric pentadecapeptide BPC 157 (GEPPPGKPADDAGLV, M.W.1419), which was promising in inflammatory bowel disease (PL-10, PLD-116, PL-14736, Pliva) trials, protects against both acute and chronic alcohol-induced lesions in stomach and liver, but also, given peripherally, affects various centrally mediated dis...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2004.07.112
更新日期:2004-09-24 00:00:00
abstract::Choline displaced [3H]QNB binding from rat brain muscarinic receptors competitively, (Ki = 460 microM) but it was only 1/1000th as potent as ACh. Deanol was an extremely weak displacer of [3H]QNB binding while hemicholinium-3 was 50 times more potent than choline. Although brain levels of choline are well below its Ki...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90012-8
更新日期:1979-09-15 00:00:00
abstract::Diabetes mellitus is associated with an increased risk of cardiovascular disease. Endothelial dysfunction (i.e. decreased endothelium-dependent vasorelaxation) plays a key role in the pathogenesis of diabetic vascular disease. The present study was undertaken to determine whether diabetes induced by streptozotocin alt...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.01.063
更新日期:2006-03-27 00:00:00
abstract::In isolated rabbit aortae, imidazole (10(-4)M) caused a unique nonspecific potentiation of the contractile responses to prostaglandins, norepinephrine, 5-hydroxytryptamine, histamine and potassium only at low concentrations. Imidazole had no effect on the dose-response relationship for Ca2+ in the presence of potassiu...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90255-2
更新日期:1982-09-24 00:00:00
abstract::The effects of angiotensin II (AII) and angiotensin III (AIII) on mean arterial pressure (MAP) and mean circulatory filling pressure (MCFP), an index of total body venous tone, in the presence and absence of [Sar1,Ile8]AII in conscious rats were examined. The infusion of AII caused dose-dependent increases in MAP and ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90074-4
更新日期:1987-10-27 00:00:00
abstract::Pentobarbital anesthetized rats subjected to Noble-Collip drum trauma developed a shock state characterized by marked hypotension, increases in plasma cathepsin D (9.6-fold), free amino-nitrogen (4.0-fold), and myocardial depressant factor (5.2-fold) activities, and a survival time of 1.90 +/- 0.23 h. Following the in...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90487-q
更新日期:1990-06-21 00:00:00
abstract::Adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), adenosine, adenine and inosine were injected intradermally into the backs of human volunteers. ATP, ADP and AMP evoked weal and flare responses in the skin in a dose dependent manner. The rank order of potency was ATP greater tha...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(81)90110-2
更新日期:1981-12-17 00:00:00
abstract::Nitric oxide (NO) and prostacyclin (PGI(2)) are two of the most important vasodilators produced by endothelial cells, the regulation of NO on PGI(2) production has not been fully clear yet. Polyaspartoyl.L-arginine (PDR) is an L-arginine residue-rich compound with inhibitory effects of platelet aggregation and thrombo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.11.003
更新日期:2008-12-28 00:00:00
abstract::Our recent study has shown that the intracerebroventricular administration of d-serine, an endogenous and selective agonist for the glycine site of the N-methyl-d-aspartate receptor, alone or in combination with morphine, leads to the potentiation of antinociception on the tail-flick response. Although there is a vari...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2008.02.068
更新日期:2008-05-31 00:00:00
abstract::We investigated the effects of methylnaltrexone on morphine-induced inhibition of smooth muscle-strip contraction in isolated guinea-pig ileum and human small intestine. The longitudinal muscle-strip was immersed in a temperature-controlled (37 degrees C) bath containing a physiological solution of 95% O2 and 5% CO2 w...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00018-g
更新日期:1995-03-24 00:00:00
abstract::The intrathecal injection of a variety of selective kappa-opioid receptor ligands did not result in significant inhibition of thermal nociceptive tail flick responses in rats. In contrast, these compounds dose dependently inhibited pressure nociceptive responses. Cross-tolerance studies revealed that the kappa-opioid ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(87)90223-8
更新日期:1987-06-04 00:00:00
abstract::The adenosine-receptor modulation of noradrenaline release was compared in prostatic and epididymal portions of rat vas deferens. In both portions, tritium overflow elicited by electrical stimulation (100 pulses/8 Hz) was reduced by the adenosine A(1) receptor agonist, N(6)-cyclopentyladenosine, and enhanced by the no...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(02)01906-4
更新日期:2002-07-12 00:00:00
abstract::A cDNA clone coding for the guinea pig leukotriene B4 (BLT) receptor has been isolated from a lung cDNA library. The guinea pig BLT receptor has an open reading frame corresponding to 348 amino acids and shares 73% and 70% identity with human and mouse BLT receptors, respectively. Scatchard analysis of membranes prepa...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(99)00514-2
更新日期:1999-09-10 00:00:00
abstract::Serotonin 1A receptor agonists have attracted much interest recently as potential therapeutic agents for levodopa-induced motor complications, such as dyskinesia and motor fluctuations. The effects of piclozotan (SUN N4057) on a rat model of advanced Parkinson's disease were investigated. Parkinsonian rats, unilateral...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2010.09.013
更新日期:2010-12-15 00:00:00
abstract::This study showed the effects of baclofen on endogenous excitatory (Glu and Asp) and non-excitatory (Tau, Gly and Ala) amino acid release. (A) Release was stimulated by K+ 30 mM in rat frontal cortex slices in vitro (evoked release in ng/g tissue per 5 min): 3739 +/- 215 (Asp), 3429 +/- 357 (Glu), 763 +/- 181 (Tau), 9...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(92)94813-b
更新日期:1992-11-24 00:00:00
abstract::The therapeutic efficacy of antidepressant drugs that inhibit the reuptake of serotonin (5-hydroxytryptamine, 5-HT) may be enhanced by blocking their indirect activation of 5-HT(1A) autoreceptors, which mediate feedback inhibition of serotonergic neuronal activity. In this study, we examined the effects of venlafaxine...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00622-1
更新日期:2000-09-15 00:00:00
abstract::Sibutramine was formerly marketed as an anti-obesity agent. The current study investigated the relationships between monoamine reuptake site occupancy for sibutramine and both its antidepressant-like efficacy and thermogenic effects. Sibutramine's effects on locomotor activity (LMA) and food intake were also evaluated...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2014.03.024
更新日期:2014-08-15 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::SCH 23390 (R(+)-7-chloro-8-hydroxy-2,3,4,5-tetrahydro-3-methyl-1-phenyl-1H-3 -benzazepine) is a potent, relatively selective antagonist of the D-1 dopamine receptor ( Iorio et al., J. Pharmacol. Exp. Ther. 226, 462). Because SKF 75670, the 7-OH analogue of SCH 23390, is a partial D-1 agonist, we conclude that the 7-Cl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(84)90324-8
更新日期:1984-04-13 00:00:00
abstract::We have characterized the tachykinin NK(2) receptor-mediated contraction and vectorial ion transport responses in the muscularis mucosae and mucosa of the rat isolated distal colon, respectively. The tachykinin NK(2) receptor-selective antagonist nepadutant (c([(beta-D-GlcNAc)Asn-Asp-Trp-Phe-Dpr-Leu]c(2beta-5beta))) p...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(01)00836-6
更新日期:2001-03-01 00:00:00
abstract::Extracellular fluid levels of excitatory amino acids (glutamate, Glu; and aspartate, Asp) in the locus coeruleus and the behavioral signs during naloxone-precipitated withdrawal from kappa-opioid receptor agonists, butorphanol and (5 alpha, 7 alpha, 8 beta) -(+)-N-methyl-N-[7-(1-pyrrolidinyl)-1-oxaspiro[4,5]dec-8-yl]-...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(96)00569-9
更新日期:1996-10-31 00:00:00
abstract::In the present study, the development of tolerance to the motor impairing effects of gamma-hydroxybutyric acid (GHBA) and ethanol was compared (Experiment 1). Rats were required to perform a motor coordination task daily shortly after ethanol (3.5 g/kg) and GHBA (1.0 g/kg) administration for 9 consecutive days. Tolera...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(94)00687-3
更新日期:1995-02-06 00:00:00
abstract::No effective chemopreventive agent has been approved against hepatocellular carcinoma (HCC) to date. Since HCC is one of the hypervascular solid tumors, blocking angiogenesis represents an intriguing approach to HCC chemoprevention. The aim of the current study was to examine the combined effect of the anti-angiogenic...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.11.022
更新日期:2014-01-15 00:00:00
abstract::Apoptosis or programmed cell death has been suggested as an important mode of neurodegeneration in Alzheimer's disease pathogenesis. The present study explored the neuroprotective effect of 2-ethoxy-4,5-diphenyl-1,3-oxazine-6-one (EDPOO) against H(2)O(2)-induced cell death in rat pheochromocytoma (PC12) cells. We foun...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2011.02.028
更新日期:2011-05-11 00:00:00
abstract::Aspirin (acetylsalicylic acid), the oldest synthetic drug, was originally used as an anti-inflammatory medication. Being an irreversible inhibitor of COX (prostaglandin-endoperoxide synthase) enzymes that produce precursors for prostaglandins and thromboxanes, it has gradually found several other applications. Sometim...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2019.172762
更新日期:2020-01-05 00:00:00