Abstract：
:Oxymetazoline was recognized with nanomolar affinity by 5-HT1A, 5-HT1B and 5-HT1D binding sites and mimicked the effects of 5-hydroxytryptamine with about the same potency and intrinsic activity as the endogenous amine in the corresponding functional tests. At 5-HT1C receptors, oxymetazoline behaved as a mixed agonist-antagonist. Clonidine had minimal activity. Methiothepin antagonized the effects of oxymetazoline (7.4 less than pKB less than 8.8). Thus, oxymetazoline is a full and potent agonist at 5-HT1A, 5-HT1B and 5-HT1D receptors and a partial agonist at 5-HT1C receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Schoeffter P,Hoyer Ddoi
10.1016/0014-2999(91)90432-psubject
Has Abstractpub_date
1991-04-17 00:00:00pages
213-6issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(91)90432-Pjournal_volume
196pub_type
杂志文章abstract：:The effect of the anti-allergic drug azelastine, 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepine-4-yl)-1-(2H)-phth alazione), on airway hyperresponsiveness induced by immunologically stimulated pulmonary alveolar macrophages was investigated in canine bronchial segments under isometric conditions in vitro. Macroph...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00114-z
更新日期：1995-05-15 00:00:00
abstract：:Serotonin(1A) (5-HT(1A)) receptors are involved in anxiety. This study focuses on the role of genetic factors on the anxiety-related effects of 5-HT(1A) receptor stimulation using both a within subject design. The effects of 5-HT(1A) receptor activation were studied in high- and low-anxiety mice (129S6/SvEvTac (S6) an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.04.037
更新日期：2004-06-21 00:00:00
abstract：:The functional role of P2X7 receptor (P2X7R) inhibition in cancer-induced bone pain has been highly contradictory. Whereas knockout studies have suggested pro-nociceptive effects, pharmacological studies suggest anti-nociceptive or no effect. The discrepancy is likely linked to the highly polymorphic nature of the P2X...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.12.032
更新日期：2019-02-15 00:00:00
abstract：:Ca2+-handling disturbances play an important role in the genesis of myocardial ischemia/reperfusion (I/R) injury. Ischemic preconditioning (IPC) is a powerful strategy to induce tolerance against subsequent ischemic episodes. IPC signaling pathways may be triggered by Ca2+ ion. Since Na+/Ca2+ exchanger 1 (NCX1) partic...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.045
更新日期：2017-01-05 00:00:00
abstract：:Recent successes as a pharmacological adjunct to exposure therapy has focused attention on the therapeutic potential of the glycine(B) receptor partial agonist, D-cycloserine (DCS), in certain clinical anxiety disorders. Although widely believed to reflect a facilitation of extinction learning, previous research with ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.08.005
更新日期：2010-11-10 00:00:00
abstract：:The Kd values of the multiple agonist binding sites in cardiac muscarinic receptors (mAChR) and pD2 values for negative inotropic actions were determined independently and their relation was examined. The guinea-pig cardiac mAChR is known to have three agonist binding sites (super-high (SH), high (H) and low (L) affin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90293-6
更新日期：1985-12-17 00:00:00
abstract：:Detailed antagonist competition curves for [3H]prazosin-labelled binding sites in rat cerebral cortex membranes reveal anomalous binding characteristics. Dihydroergocryptine and indoramine compete in a steep, monophasic manner while WB4101 and phentolamine exhibit shallow competition curves. Computer-assisted analysis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90432-7
更新日期：1985-02-26 00:00:00
abstract：:Infusion of arachidonic acid through the guinea pig lung or the cat spleen causes a release of thromboxane A2 and prostaglandins, as measured by bioassay. After incubation of human platelets with arachidonate similar metabolites are formed, as demonstrated chromatographically. Infusion of imidazole (50-75 microgram/ml...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90104-2
更新日期：1977-07-15 00:00:00
abstract：:We have investigated the effect of 2(4-((2-carboxymethyl)phenyl)ethylamino)-5'-N-ethylcarboxamidoadenosine (CGS 21680), a potent and selective agonist at adenosine A2A receptors, on pulmonary inflammation induced by allergen challenge in the ovalbumin-sensitised, Brown Norway rat. Aerosol administration of ovalbumin (...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01305-5
更新日期：2002-03-08 00:00:00
abstract：:Recombinant human tumor necrosis factor alpha (TNF alpha) decreases social exploration and induces weight loss in mice in a dose- and time-dependent manner (2.5-40 micrograms/mouse). To assess the role of interleukin-1 (IL-1) in these effects, mice pretreated with IL-1 receptor antagonist (IL-1ra, 500 micrograms/mouse...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90184-r
更新日期：1991-12-17 00:00:00
abstract：:The effects of N-(aminoiminomethyl)-1, 4-dimethyl-1H-indole-2-carboxamide methanesulfonic acid (SM-20550), a novel potent Na(+)/H(+) exchanger, and nicorandil, a K(+) channel opener with nitrate-like activity, were studied in a myocardial ischemia and reperfusion injury model. Anesthetized rabbits underwent occlusion ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00610-5
更新日期：2000-09-15 00:00:00
abstract：:Evidence suggests that insulin has direct, potent and physiologically relevant vasodilatory effects. This has led to the hypothesis that in states of insulin resistance, insulin's vasodilatory effects may be blunted leading to an increase in vascular tone and blood pressure. To examine this proposition we studied the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)00104-0
更新日期：1997-03-19 00:00:00
abstract：:Recent reports have provided evidence for a new concept that in small resistance arteries α1D-adrenoceptor-mediated contraction is intimately linked to pannexin-1 (Px1) hemichannels that open to allow the release of ATP, from the smooth muscle effector cell, that acts back on P2Y purinoceptors to cause contraction. Th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.01.024
更新日期：2015-03-05 00:00:00
abstract：:Cancer stem cell therapy is becoming a focal point for oral squamous cell carcinoma (OSCC). They can be regulated by tumor glucose metabolism, whereas the regulation is not fully investigated in OSCC. Herein, we studied the synergistic anti-tumor effect of a LIN28 inhibitor C1632 and hypoglycemic medication metformin ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173757
更新日期：2021-01-15 00:00:00
abstract：:The influence of inflammatory cells on airway reactivity was investigated on arachidonic acid-induced relaxations of guinea-pig trachea and on arachidonic acid metabolism in guinea-pig tracheal epithelial cells. The presence of either eosinophils or neutrophils (1.0 x 10(7) cells/ml), from bronchoalveolar lavage, decr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00736-4
更新日期：1996-12-19 00:00:00
abstract：:The effects of intracellular and extracellular application of bretylium tosylate on outward potassium current and fast inward Na+ current have been studied in single ventricular cells of chick embryo (18-day-old) using the whole-cell voltage clamp technique. Extracellular superfusion with bretylium (3 x 10(-4) M) decr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90535-3
更新日期：1988-07-14 00:00:00
abstract：:Dipeptidyl peptidase-4 (DPP-4) inhibitors improve glycemic control in patients with type 2 diabetes by increasing plasma active glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide levels. However, the effects of chronic DPP-4 inhibition on in vivo beta-cell function are poorly characterize...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.04.018
更新日期：2008-07-07 00:00:00
abstract：:The analgesic activity of dothiepin (an antidepressant interacting with serotonin receptors) was studied (double-blind) in humans. A significant increase in nociceptive flexion reflex threshold and subjective pain threshold was observed after a 14-day dothiepin treatment. The effects of dothiepin on diffuse noxious in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90175-h
更新日期：1993-10-12 00:00:00
abstract：:Methotrexate is a disease modifying anti-rheumatic drug that is widely used for the treatment of rheumatoid arthritis. Nimesulide is a non-steroidal anti-inflammatory drug which is frequently used as adjuvant therapy for symptomatic alleviation of rheumatoid arthritis. In this study, we have evaluated the potential in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.07.006
更新日期：2010-10-10 00:00:00
abstract：:The pharmacological treatment of mood and anxiety disorders has for long relied on the serendipitous findings of monoaminergic and benzodiazepine drugs more than 50 years ago. These treatments, however, are therapeutically insufficient and even though more recently developed drugs are particularly improving side effec...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2008.01.057
更新日期：2008-05-13 00:00:00
abstract：:More recently, arsenic trioxide (ATO), was integrated into acute promyelocytic leukemia (APL) treatment, showing high efficacy and tolerability in patients with both ATRA-sensitive and ATRA-resistant APL. ATO could induce apoptosis at relatively high concentrations (0.5 to 2.0 micromol/L) and partial differentiation a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.04.040
更新日期：2014-08-05 00:00:00
abstract：:L-Glutamic acid and kainic acid injected into the cisterna magna of dogs, produced a dose-dependent increase in blood pressure and a decrease in heart rate. In contrast, intravenous injection of both compounds was ineffective. The hypertension was probably due to an increase in sympathetic tone as guanethidine prevent...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90055-4
更新日期：1979-11-23 00:00:00
abstract：:Electrical field stimulation of the isolated adventitial and intima-medial layers of rabbit aorta preloaded with 3H-noradrenaline elicited a 3H outflow. The initial 3H outflow from adventitia was independent of external Ca2+ concentration. Each of the subsequent 3H outflows was mainly Ca2+ sensitive. All stimulation-i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90156-4
更新日期：1976-10-01 00:00:00
abstract：:The anti-arrhythmic action of 2,3-cis-1,2,3,4-tetrahydro-5-[(2-hydroxy-3-tert-butylamino)propoxy]2,3-naphthalenediol (nadolol) was evaluated and compared with that of propranolol in several experimental models of cardiac arrhythmias. Both nadolol and propranolol antagonized isoproterenol-induced tachycardia and ouabai...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90296-x
更新日期：1976-01-01 00:00:00
abstract：:Small-conductance calcium-activated potassium channels (K(Ca)2) generating the medium afterhyperpolarization seen after an action potential modulate the neuronal integration signal. The effects of two K(Ca)2 channel blockers, apamin, specific to K(Ca)2.2 and K(Ca)2.3 channels, and lei-Dab7, which binds to K(Ca)2.2 cha...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.05.019
更新日期：2008-07-28 00:00:00
abstract：:Cats, sedated and paralyzed, showed a significant increase in body temperature after intravenous injection of morphine while animals with additional spinal blockade (C3) from injection of 2% lidocaine solution, did not. The results suggest that motor activity is not necessary for morphine-induced hyperthermia in the c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90113-9
更新日期：1978-06-01 00:00:00
abstract：:Protective effects of OP-2507 [15-cis-(4-propylcyclohexyl)-16,17,18,19,20-pentanor-9-deoxy -9 alpha, 6-nitrilo-PGF1 methyl ester] against cerebral anoxia and edema were investigated in a variety of experimental models in mice and rats. OP-2507 given s.c. or p.o. led to a consistent and dose-dependent prolongation of s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90706-5
更新日期：1986-04-29 00:00:00
abstract：:Pulmonary hypertension is a progressive disease of various origins that is associated with right ventricular dysfunction. In the present study, the protective effect of diosgenin was investigated in monocrotaline-induced pulmonary hypertension in rats. Pulmonary hypertension was induced by a single subcutaneous inject...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.07.026
更新日期：2014-10-05 00:00:00
abstract：:Racemic baclofen, (-)-baclofen and muscimol depressed all spontaneously firing locus coeruleus neurons tested in a slice preparation. Racemic phaclofen (100 microM; 1 mM) moderately antagonized the effects of racemic baclofen without antagonizing those of muscimol. Bicuculline (10, 30, 100 microM) potently antagonized...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90061-1
更新日期：1988-04-27 00:00:00
abstract：:The selectivity of the potent dopamine D-2 agonist 2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetralin (N-0437) was examined in a series of in vivo and in vitro pharmacological models. In radioligand binding assays, N-0437 showed high potency (Ki = 0.69 nM) and selectivity for D-2 receptors as compared to its potency...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90783-2
更新日期：1988-03-01 00:00:00
