Abstract：
:[3H]BAY U 3405 was used to characterize the effect of acidic and alkaline pH values on the binding of the thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor of human platelet membranes. The specific binding of [3H]BAY U 3405 largely increased upon acidification up to pH 5.8. Saturation binding studies revealed an increase in binding affinity without change in the number of binding sites. At pH 7.4 the Kd was 8.7 +/- 3.7 nM (Bmax = 6.6 +/- 0.6 pmol/mg protein) compared to 1.2 +/- 0.2 nM (Bmax = 6.1 +/- 0.6 pmol/mg protein) at pH 5.8. A more than 10-fold higher rate of association was observed at pH 5.8 compared to pH 7.4, while the rate of dissociation showed only minor changes. The kinetically derived dissociation constant was 1 nM (pH 5.8) and 9.6 nM (pH 7.4). The pH dependency of the binding of structurally different non-labelled ligands to the TXA2/PGH2 receptor was evaluated by inhibition studies at pH 5.8 and pH 7.4. BAY U 3405, daltroban, CTA2, and U 46619 showed significantly higher affinities at pH 5.8. In contrast, I-PTA-OH and GR 32191 had a higher affinity at pH 7.4. No significant difference was seen with SQ 29548 at the observed pH values. A second protonable group within the molecules I-PTA-OH, GR 32191, and SQ 29548 might be responsible for the observed differences.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Theis JG,Dellweg H,Perzborn E,Gross Rdoi
10.1016/0922-4106(92)90176-vkeywords:
subject
Has Abstractpub_date
1992-06-05 00:00:00pages
149-56issue
2eissn
0014-2999issn
1879-0712journal_volume
226pub_type
杂志文章abstract：:The family of facilitative glucose transporter (GLUT) proteins is responsible for the entry of glucose into cells throughout the periphery and the brain. The expression, regulation and activity of GLUTs play an essential role in neuronal homeostasis, since glucose represents the primary energy source for the brain. Br...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2004.02.041
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abstract：:We investigated protein kinase C participation in the contractile response to 5-hydroxytryptamine (5-HT), and in the interaction between 5-HT and endothelin-1, in aortas from control and diabetic rats. Diabetic rats display attenuated reactivity to 5-HT (i.e., approximately 47% of control maximum). The protein kinase ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00986-7
更新日期：1997-03-12 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90811-h
更新日期：1992-11-13 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00240-5
更新日期：2000-06-09 00:00:00
abstract：:Portulaca oleracea L. is used as a folk medicine in many countries because of its wide range of pharmacological effects. HM-chromanone, isolated from P. oleracea using bioassay-guided fractionation and HPLC, belongs to the homoisoflavonoid group and has been shown to exert several biological effects. In this study, we...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90355-5
更新日期：1989-08-03 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90582-4
更新日期：1983-04-08 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90495-2
更新日期：1982-03-26 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90603-3
更新日期：1982-06-16 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00891-7
更新日期：1999-02-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90551-z
更新日期：1991-03-26 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.10.064
更新日期：2008-02-02 00:00:00
abstract：:The present study describes the effect of sertindole, clozapine and haloperidol on the number of spontaneously active dopamine neurons in ventral tegmental area and substantia nigra pars compacta after daily oral treatment for 1, 2 or 3 weeks. In general, daily administration of high dosages (sertindole: 2.8 mumol/kg/...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90468-5
更新日期：1994-03-21 00:00:00
abstract：:The systemic administration of polyamines (s.c.) produced a dose-dependent motor depression. With high doses the depressant effect was long-lasting and the animals showed signs of toxicity. ED50 values for spermine, spermidine and putrescine were 38, 90 and 251 mg/kg respectively. The motor depression induced by the s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00786-8
更新日期：1996-12-30 00:00:00
abstract：:The effect of colchicine on jejunal adenylate cyclase activity, prostaglandin E2 (PGE2) and cAMP contents, the enzyme and mediators involved in intestinal fluid secretion was tested in rats. Four h after the intraperitoneal injection of colchicine (0.5 mg/100 g body wt.) mucosal PGE2 content, adenylate cyclase activit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90503-8
更新日期：1980-10-17 00:00:00
abstract：:The extracellular loops of the adrenoceptors present a potential therapeutic target in the design of highly selective adrenergic drugs. These regions are less conserved than the orthosteric binding site but have to date not been implicated in activation of adrenoceptors. A previously generated homology model identifie...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.03.034
更新日期：2014-06-15 00:00:00
abstract：:Cutaneous arteries show enhanced contraction in response to cooling, which is suggested to be mediated via α2C-adrenoceptors. We have previously shown that α1-adrenoceptors are also involved in the enhanced contraction in cooling conditions. In the present study, we aimed to identify the α1-adrenoceptor subtype involv...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.09.004
更新日期：2018-11-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2020.173561
更新日期：2020-11-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.09.045
更新日期：2013-12-05 00:00:00
abstract：:Receptor for advanced glycation end-products (RAGE) is involved in the pathogenesis of diabetic nephropathy. FPS-ZM1, a selective RAGE inhibitor, in combination with valsartan were investigated for their protective potentials on the renal markers of tubular injury in streptozotocin-induced diabetic rats. Rats were ass...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.10.035
更新日期：2019-01-05 00:00:00
abstract：:AY-22,241 (Actodigin) is a new rapid-acting semisynthetic cardiotonic steroid. In experiments on contractility of cat papillary muscle, Actodigin (2 times 10(-7) to 4 times 10(-6) M) produced a dose-dependent positive inotropic effect, a marked increase in the maximum rate of force development, and no change in restin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90316-7
更新日期：1975-05-01 00:00:00
abstract：:The histamine H₄ receptor mediates several histamine-induced cellular functions of leukocytes, including cell migration and cytokine production. Recent studies suggest that histamine signaling through the histamine H₄ receptor can also have anti-pruritic and anti-nociceptive functions. 1-(7-(2-amino-6-(4-methylpiperaz...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.11.027
更新日期：2012-01-30 00:00:00
abstract：:In vivo microdialysis was used to study the effects of the locally applied GABA B receptor antagonist 2-hydroxysaclofen and GABA B receptor agonist baclofen on the basal dopamine efflux as well as on the endomorphin-1- and endomorphin-2-induced dopamine efflux in the nucleus accumbens of freely moving rats. 2-Hydroxys...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.12.008
更新日期：2008-03-10 00:00:00
abstract：:Behavioral interactions between ethanol and GABA-mimetic and GABA antagonist drugs were evaluated by duration of narcosis and motor incoordination (inhibition of bar holding) in mice. Aminooxyacetic acid (AOAA), baclofen, and tetrahydroisoxazolopyridineol (THIP) (GABA mimetics) lengthened ethanol narcosis, while picro...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90607-6
更新日期：1983-04-22 00:00:00
abstract：:This study sought to determine the potential role of nitric oxide (NO) in N-methyl-D-aspartate (NMDA)-stimulated efflux of [14C] gamma-aminobutyric acid (GABA) and [3H]acetylcholine from striatal slices in vitro. In Mg2+-free buffer, NMDA-stimulated [14C]GABA and [3H]acetylcholine release were inhibited by the guanyla...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00636-0
更新日期：1998-10-23 00:00:00
abstract：:In the present study, the effects of dopamine receptor agonists and antagonists on naloxone-induced jumping in morphine-dependent mice were examined. Mice were rendered dependent as described in the methods section. Naloxone was injected to elicit jumping (as withdrawal sign). The first group received dopamine recepto...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02149-0
更新日期：2002-09-20 00:00:00
abstract：:Omeprazole, besides suppressing gastric acid, causes delayed gastric emptying, which may be associated with aggravated dyspeptic symptoms. Effects of omeprazole on small intestinal transit are unknown. In this study, we evaluated in mice if (a) omeprazole affects transit of a meal through the stomach and small intesti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.05.041
更新日期：2005-07-04 00:00:00
abstract：:The influence of decreased endogenous gamma-aminobutyric acid (GABA) concentration on benzodiazepine receptor function was studied in the brain of living baboons. Positron emission tomography and the radiotracer [11C]flumazenil combined with electroencephalography were used to determine the pharmacological properties ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)00004-6
更新日期：1997-02-19 00:00:00
abstract：:The hypothesis that K(+) channels and cell depolarization are involved in neuronal death and neuroprotection was tested in bovine chromaffin cells subjected to two treatment periods: the first period (preconditioning period) lasted 6 to 48 h and consisted of treatment with high K(+) solutions or with tetraethylammoniu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.08.084
更新日期：2006-12-28 00:00:00
