Abstract：
:The effect of various concentrations of 4 beta-phorbol dibutyrate, (4-beta PDBu) phorbol myristate acetate (PMA), and 4 beta-phorbol didecanoate (4 beta-PDD) were studied on the guinea-pig parenchymal strip. The order of potency, 4 beta-PDBu greater than PMA greater than 4 beta-PDD, was the inverse of their lipid solubility. 4 beta-PDBu, 10(-9)-10(-4) M, caused a powerful, slow, sustained contraction starting within 2-3 min and reaching maximum in approximately 45 min, the maximum being 170% of the maximum histamine contraction. The responses to PMA and 4 beta-PDD were slower and less marked. 4 alpha-Phorbol dibutyrate had no effect. These results differ from those reported for guinea-pig trachea. In calcium-free Krebs solution + EGTA (1 mM) the cumulative concentration-response curve to 4 beta-PDBu was still obtained but was slower and was diminished. A23187, ionomycin and vanadate also caused contraction, the respective concentration ranges being 10(-7)-10(-5), 10(-8)-10(-6) and 10(-6)-10(-3) M. When a low concentration of 4 beta-PDBu, which on its own produced no effect, was given with a low concentration of A23187, ionomycin or vanadate, marked synergism was seen. These results are consistent with the model of smooth muscle contraction in which it was proposed that the initial response to stimulation is mediated by both the trisphosphate/calcium and diacylglycerol/protein kinase C pathways, while the sustained response is mediated by the diacylglycerol/protein kinase C pathway, only.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Dale MM,Obianime AWdoi
10.1016/0014-2999(87)90407-9subject
Has Abstractpub_date
1987-09-02 00:00:00pages
23-32issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(87)90407-9journal_volume
141pub_type
杂志文章abstract：:Inhibition of inducible nitric oxide (NO) synthase during endotoxaemia may be of therapeutic value. We have previously shown that pretreatment of mice with adenosine receptor agonists 1 h before lipopolysaccharide administration results in a dose-dependent reduction of plasma nitrite and nitrate (NOx-) levels. This re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00677-2
更新日期：1996-12-05 00:00:00
abstract：:In male Swiss mice, muscimol produced myoclonic jerks. A 3 mg/kg (i.p.) dose induced this response in all of the mice tested and the peak response of 73 jerks per min was observed between 27 and 45 min. Increasing the brain serotonin levels by the administration of 5-hydroxytryptophan (80-160 mg/kg) in combination wit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90087-x
更新日期：1981-07-17 00:00:00
abstract：:Radioligand receptor binding techniques were used to characterize the effects of different structural types of antidepressant drugs on neurotransmitter receptors. The tricyclic antidepressants more or less potently inhibited the binding to rat brain preparations of several different radiolabelled ligands [3H]WB4101, [...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90172-2
更新日期：1981-03-26 00:00:00
abstract：:The toxicity of glutamate in neuronal cultures has been attributed in part to a mitochondrial dysfunction involving the permeability transition pore. The participation of the permeability transition pore in this process has been pharmacologically demonstrated by the use of cyclosporin A, which inhibits pore opening by...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00584-7
更新日期：2000-09-15 00:00:00
abstract：:Right ventricular kitten papillary muscles were incubated with dibutyryl adenosine 3',5'-monophosphate (dbcAMP) at varying concentrations as low as 1 X 10(-4)M. A positive inotropic effect was observed with all concentrations of dbcAMP. Concomitant administration of 5 X 10(-4)M monobutyryl guanosine 3',5'-monophosphat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90280-6
更新日期：1976-03-01 00:00:00
abstract：:In view of the scarce information about the analgesic mechanism of kappa-opioid receptor agonists, the objective of the present study was to determine whether nitric oxide (NO) is involved in the peripheral antinociception of bremazocine, a kappa-opioid receptor agonist. Three drugs all interfering with the L-arginine...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02275-6
更新日期：2002-11-01 00:00:00
abstract：:In the present study, the inhibitory effects of hesperetin (HSP) on human cardiac Kv1.5 channels expressed in HEK 293 cells and the ultra-rapid delayed rectifier K(+) current (Ikur) in human atrial myocytes were examined by using the whole-cell configuration of the patch-clamp techniques. We found that hesperetin rapi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.07.015
更新日期：2016-10-15 00:00:00
abstract：:In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin an aminopeptidase inhibitor of bacterial origin potently inhibited the hydrolysis of [3H][Leu5]enkephalin by slices from rat striatum with an IC50 value of about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90181-4
更新日期：1983-01-21 00:00:00
abstract：:Previous studies have shown that treatment of guinea-pig isolated vas deferens with the affinity label periodate-oxidized ATP (2',3'-dialdehyde ATP), results in two irreversible effects on biphasic contractile responses to ATP, i.e., potentiation of the P2X purinoceptor-mediated first phase and inhibition of the ecto-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00352-l
更新日期：1995-08-04 00:00:00
abstract：:The acetylcholine receptor agonists, acetylcholine (10(-5)-10(-4 M), carbachol (5 x 10(-6)-5 x 10(-5) M), bethanechol (5 x 10(-5)-5 x 10(-4) M) and dimethylphenylpiperazinium (DMPP, 10(-5) M) increased the short-circuit current (Isc) in the rat colon descendens by a tetrodotoxin (TTX)-sensitive mechanism. Blockade by ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90568-2
更新日期：1989-09-13 00:00:00
abstract：:Renal mesangial cells exposed to inflammatory cytokines produce high concentrations of nitric oxide (NO) which may exert cytotoxic actions. We report here that glomerular mesangial cells, endothelial cells and epithelial cells in culture are themselves targets for NO and undergo apoptotic cell death upon exposure to h...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00701-7
更新日期：1996-12-12 00:00:00
abstract：:The psychotropic actions of crude ginseng saponins, pure ginsenoside Rb1 (GS-Rb1) and ginsenoside Rg1 (GS-Rg1) obtained from the root of Panax ginseng, were evaluated from their effects on agonistic behavior in mice. A resident-intruder test situation was used. When the resident mouse was treated with crude ginseng sa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90305-6
更新日期：1988-02-09 00:00:00
abstract：:The present study was to investigate the neuroprotective efficacy and mechanism of Forsythoside B. Male Sprague-Dawley rats were subjected to middle cerebral artery occlusion for 1 h followed by reperfusion for 23 h. Rats received an intravenous bolus injection of Forsythoside B at 15 min after reperfusion. The result...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.055
更新日期：2010-08-25 00:00:00
abstract：:We have recently proposed that retinoic acid receptor (NR1B) is a promising target of neuroprotective therapy for intracerebral hemorrhage, since pretreatment of mice with an NR1B1/NR1B2 agonist Am80 attenuated various pathological and neurological abnormalities associated with the disease. In the present study we fur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.03.023
更新日期：2012-05-15 00:00:00
abstract：:Subplantar injection of 0.10 micrograms of serotonin in the rat resulted in a brief period (0-20 min) of increased pain sensitivity to an applied force (hyperalgesia) which preceded a longer period (40-120 min) of decreased pain sensitivity (hypoalgesia). The magnitude of each of these changes and the duration of the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90257-4
更新日期：1989-05-30 00:00:00
abstract：:Preclinical data, performed in a limited number of pain models, suggest that functional blockade of metabotropic glutamate (mGlu) receptors may be beneficial for pain management. In the present study, effects of 2-methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective mGlu5 receptor antagonist, were examined in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.11.005
更新日期：2004-12-15 00:00:00
abstract：:Alcuronium is known to stabilize allosterically the binding of the muscarinic antagonist N-methylscopolamine to muscarinic M2 receptors and thus to elevate the equilibrium binding of N-methylscopolamine in homogenized cardiac tissue. In order to check for a functional consequence of this effect, the action of alcuroni...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)00664-s
更新日期：1995-01-05 00:00:00
abstract：:The binding of atrial natriuretic peptide (ANP) to olfactory bulb, pituitary anterior lobe and thymus gland membranes was examined. [125I]ANP (rat, 99-126) bound specifically to the three types of membranes. However, the affinity for ANP receptor in olfactory bulb was much higher than those in either pituitary or thym...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90293-8
更新日期：1989-03-21 00:00:00
abstract：:Unexpectedly, it was observed that the P2-purinoceptor antagonist, suramin (10 microM to 1 mM), reversed the muscle paralysis caused by structurally unrelated non-depolarizing relaxants. Suramin competitively reversed the blocking action of pancuronium. Both the pre- and postsynaptic blockade of nicotinic receptors by...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90211-l
更新日期：1992-05-27 00:00:00
abstract：:Acute benzodiazepine administration has been reported to antagonize the effect of cholecystokinin both in the periphery and in the central nervous system. A two-week treatment with either diazepam (5 mg/kg per day) or flurazepam (15 mg/kg per day) markedly reduced the excitatory effect of microiontophoretically applie...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90703-0
更新日期：1988-06-22 00:00:00
abstract：:Chemopreventive non-steroidal anti-inflammatory drugs (NSAIDs) exhibit diverse pharmacological and biological activities mainly through their inhibitory effect on cyclooxygenase (COX). However, COX-independent mechanisms involving kinase inhibition have been proposed to explain certain therapeutic effects of NSAIDs. H...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.04.012
更新日期：2010-07-25 00:00:00
abstract：:The Na(+)/Ca(2+) exchanger (NCX) is involved in myocardial ischemia-reperfusion injuries. We examined the effects of 2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline (SEA0400), a potent and selective inhibitor of NCX, on myocardial ischemia-reperfusion injury models. In canine cardiac sarcolemmal vesicles an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02732-2
更新日期：2003-01-01 00:00:00
abstract：:Cancer cell lines derived from hepatocytes have an altered phenotype and they lack hepatocyte-specific functions. It is at least partly due to the under-expression of transcription factors such as hepatocyte nuclear factor 4α (HNF4α), steroid receptor co-activator 1 (SRC1) etc. Recently, a strategy of transient transf...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.07.049
更新日期：2011-11-01 00:00:00
abstract：:Airway remodeling in asthma is difficult to treat because of its complex pathophysiology that involves proinflammatory cytokines, as well as the arachidonic acid cytochrome P-450 (CYP) pathway; however, it has received little attention. In this study, we assessed the efficacy of a soluble epoxide hydrolase (sEH) on ai...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172874
更新日期：2020-02-05 00:00:00
abstract：:Diabetic cardiomyopathy (DCM) is one of the major cardiac complications in diabetic patients and a major reason for the death of diabetic patients. Obeticholic acid (OCA) is a semi-synthetic bile acid analogue. The objective of the present study was to investigate the possible cardio-protective effect of OCA against D...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.05.022
更新日期：2019-09-05 00:00:00
abstract：:The site of the analgesic action of AD-1211, the less active stereoisomer, and its pharmacological features were investigated. AD-1211, as well as pentazocine and morphine, blocked the reflex hypertension caused by injection of both bradykinin and bradykinin plus PGE1 into the splenic artery of dogs. In the rat or mou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90722-2
更新日期：1984-11-13 00:00:00
abstract：:Pentoxifylline, a methylxanthine derivative, has been widely used to improve erythrocyte deformability and capillary blood circulation in patients with claudication and cerebrovascular disorders as well as in animals with sepsis. Here, we investigate the effects of pentoxifylline on the hypotension, vascular hyporeact...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00265-4
更新日期：1999-05-28 00:00:00
abstract：:The interaction between endogenous nitric oxide (NO), elicited by administration of Escherichia coli lipopolysaccharide, and cyclooxygenase system, in ethanol-induced injury in rat gastric mucosa, was investigated. Administration of graded doses of lipopolysaccharide reduced the gastric mucosal injury in response to e...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00161-7
更新日期：1998-05-08 00:00:00
abstract：:The histamine H2-receptor antagonist cimetidine potently inhibited [3H]muscimol and enhanced [3H]flunitrazepam binding in membranes prepared from several brain regions in the rat, including the dorsal raphe nucleus. As further examined in cortical membranes, this effect on both GABA and benzodiazepine binding sites wa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90011-0
更新日期：1983-03-25 00:00:00
abstract：:The function of multidrug resistance-associated protein 2 (Mrp2) in the intestine and liver, as well as intestinal Mrp2 expression, was analyzed in CCl(4)-induced acute hepatic failure rats with hyperbilirubinemia. The plasma level of bilirubin glucuronides, endogenous Mrp2-substrates, was 26 microM at 24 h after CCl(...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.06.079
更新日期：2006-09-28 00:00:00
