Abstract：
:The effects of endothelin, a potent endogenous vasoconstrictor peptide, were examined in a range of vascular and non-vascular tissues. At concentrations that cause vasoconstriction in portal vein and aorta, the peptide strongly contracted rat uterus, trachea and vas deferens, but not guinea pig ileum. Nifedipine, a dihydropyridine calcium anatgonist, partially inhibited these contractions. Endothelin had no inotropic or chronotropic effect on the isolated rat heart. The peptide did not modulate secretion at the neuromuscular junction, from adrenal medullary cells or neutrophils, nor affect secretion or aggregation of platelets. The tissue responsiveness to endothelin was not the same as the tissue distribution of dihydropyridine receptors. This supports the idea that endothelin interacts with a specific receptor distinct from dihydropyridine sensitive calcium channels. The contractile effect of endothelin on non vascular smooth muscle suggests that the concept of endothelium dependent modulation of vascular smooth muscle tone may be extended to include epithelium dependent modulation of non vascular tissues.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Borges R,Von Grafenstein H,Knight DEdoi
10.1016/0014-2999(89)90716-4subject
Has Abstractpub_date
1989-06-20 00:00:00pages
223-30issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(89)90716-4journal_volume
165pub_type
杂志文章abstract：:3H-angiotensin binding sites have been studied in a particulate fraction prepared from rat adrenal glands. This binding is rapid and reversible, of high affinity (KD29 degrees C = 3-5 X 10(-9) M) and with demonstrable specificity for the angiotensin II octapeptide. The number of binding sites varies with endogenous an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90042-5
更新日期：1977-06-15 00:00:00
abstract：:Chronic Obstructive Pulmonary Disease (COPD) is a major incurable global health burden and is the 4th leading cause of death worldwide. It is believed that an exaggerated inflammatory response to cigarette smoke causes progressive airflow limitation. This inflammation, where macrophages, neutrophils and T lymphocytes ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.03.029
更新日期：2015-07-15 00:00:00
abstract：:[3H]Rauwolscine, a specific and potent alpha 2-antagonist radioligand, was used to characterize alpha 2-receptor binding in bovine cerebral cortex. [3H]Rauwolscine binding was reversible, stereospecific, and saturable. Association, dissociation, and saturation studies revealed one site interactions (k -1/k+1 = 1.2 nM,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90123-0
更新日期：1981-12-17 00:00:00
abstract：:We examined whether estrogen negatively modulates cannabinoid-induced regulation of food intake, core body temperature and neurotransmission at proopiomelanocortin (POMC) synapses. Food intake was evaluated in ovariectomized female guinea pigs abdominally implanted with thermal DataLoggers and treated s.c. with the ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.09.001
更新日期：2009-11-10 00:00:00
abstract：:It is well documented that cannabinoid receptor agonist WIN 55,212-2 had protective effect against cerebral ischemic injury. Our previous study indicated that WIN 55,212-2 pretreatment induced ischemic tolerance to focal cerebral ischemia in a dose-dependent manner. The aim of the present study was to investigate the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.07.024
更新日期：2010-10-25 00:00:00
abstract：:Natural purines like ATP, ADP and adenosine have crucial roles in platelet physiology. This knowledge has been significant in drug development and today ADP receptor antagonists are widely used for prevention of thrombotic events following myocardial infarction and ischaemic stroke. Recent studies have shown that a pu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172428
更新日期：2019-08-15 00:00:00
abstract：:The effects of phenoxybenzamine on alpha 1- and alpha 2-adrenergic receptor binding sites were examined directly using radioligand binding assays of the antagonist drugs [125I]BE 2254 and [3H]rauwolscine, respectively, in homogenates of rat cerebral cortex. Treatment with phenoxybenzamine caused an irreversible, dose-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90458-2
更新日期：1983-10-14 00:00:00
abstract：:Sham and electrolytic lesions of the dorsal, median, and dorsal + median raphe nuclei were made in different groups of rats. One week later, daily oral treatment with ethanol (5 g/kg p.o. for 25 days) was started. This treatment produced tolerance to the hypothermic and motor impairing (moving belt test) effects of et...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90079-6
更新日期：1982-06-04 00:00:00
abstract：:We examined the effects of (+/-)-(E)-4-ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide (FK409), a nitric oxide (NO) donor, on renal actions and norepinephrine overflow induced by renal nerve stimulation in anesthetized dogs, with or without N(G)-nitro-L-arginine (NOARG), a NO synthase inhibitor. Renal nerve stimulatio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01424-6
更新日期：1998-01-12 00:00:00
abstract：:The new dihydropyridine calcium channel antagonist S 11568 and its optical isomers, S 12967 and S 12968 (3 x 10(-6) to 10(-4) M), caused, unlike nifedipine (10(-4) M), equipotent and rapid endothelium-dependent relaxations and increased the content of cyclic GMP in rings of canine femoral arteries. These effects were ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90362-t
更新日期：1991-05-02 00:00:00
abstract：:Ketamine, a non-selective inhibitor of NMDA (N-methyl-D-aspartate) channels is used in anesthetic or sub-anesthetic doses to induce analgesia, amnesia, to suppress fear, anxiety and depression. Although the ketamine's effect on memory acquisition is known, its effects on other aspects of memory are controversial. Morr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.12.021
更新日期：2012-02-29 00:00:00
abstract：:The distribution of P2-purinoceptors in pre-capillary resistance vessels was studied in vitro, using Krebs perfused rabbit ears and in vivo, in autoperfused hindquarters, intestinal and renal vasculatures of pentobarbitone anaesthetised cats. ATP (10(-10)-10(-6) mol i.a.) caused dose-dependent vasodilatation which, in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90834-0
更新日期：1989-02-28 00:00:00
abstract：:In isolated heart muscle, the compound R56865 (N-[1-[4-(4-fluorophenoxy)butyl]-4-piperidinyl]-N-methyl-2- benzothiazolamine) has been shown to protect against intoxication by cardiac glycosides. We studied the influence of R56865 on various membrane currents in single isolated ventricular cardiomyocytes of the guinea-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90010-4
更新日期：1990-10-09 00:00:00
abstract：:Painful diabetic neuropathy is a common complication of diabetes mellitus, which often makes the patients suffer from severe hyperalgesia and allodynia. Thus far, the treatment of painful diabetic neuropathy remains unsatisfactory. Metformin, which is the first-line drug for type-2 diabetes, has been proved to attenua...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.06.010
更新日期：2015-10-05 00:00:00
abstract：:The effect of diazoxide, verapamil and compound D600 on calcium and isoproterenol dose-response relationships was investigated in isolated rabbit atrial preparations. All three agents shifted calcium dose-force relationships parallel and to the right. D600 acted as a competitive antagonist of calcium, as a plot of log...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90009-7
更新日期：1977-10-01 00:00:00
abstract：:Termination of signalling by G-protein-coupled receptors requires inactivation of the G alpha-subunits of heterotrimeric G-proteins and the re-association of G alpha- and G betagamma-subunits. Inactivation of G alpha-subunits is achieved by the hydrolysis of bound GTP by an intrinsic GTPase activity, which is consider...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.03.047
更新日期：2008-06-10 00:00:00
abstract：:We used male Wistar rats to determine the effects of lipopolysaccharide (LPS) on gastric secretion. After pylorus ligation, 24-h fasted rats received i.p. injections of different doses of LPS dissolved in sterile saline. The amounts of gastric acid and pepsin secreted were determined 2, 4 or 8 h after injection. Small...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90256-6
更新日期：1990-05-31 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：:A new analogue of ANF (atrial natriuretic factor), NNC 70-0270, was tested in various isolated artery preparations. In the rabbit aorta and renal artery NNC 70-0270 was compared with atriopeptin III and the relative inhibitory potency against noradrenaline-induced contractions (atriopeptin III = 1) was found to be 5 a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90764-h
更新日期：1991-11-19 00:00:00
abstract：:We investigated the effects of 7-nitroindazole, a specific inhibitor of neuronal nitric oxide (NO) synthase, on NO concentration and on blood flow in rat hippocampus after transient forebrain ischemia which was induced by 4-vessel occlusion for 10 min. NO concentration was measured directly by an NO-selective electrod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00555-5
更新日期：1999-09-10 00:00:00
abstract：:The dopamine transporter removes the neurotransmitter from the synapse, regulating dopamine availability. The transporter can be internalized and its function is blocked by cocaine and other ligands. Melittin inhibits dopamine transporter function and causes internalization of the recombinant transporter in stably tra...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.05.020
更新日期：2012-09-05 00:00:00
abstract：:Melatonin is of considerable interest for its regulatory influence on a variety of physiological processes including biological rhythms and neuroendocrine functions. We showed that melatonin potentiates sympathetic neurotransmission in the prostatic portion of the rat vas deferens, by increasing contractions in respon...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90696-3
更新日期：1994-05-12 00:00:00
abstract：:The ability of flunarizine to terminate ouabain-induced ventricular tachycardia was investigated in conscious dogs. These arrhythmias result from triggered activity based on delayed afterdepolarizations. Sustained ventricular tachycardia was induced by ouabain (48 +/- 6 micrograms/kg) and pacing in 13 animals with sur...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90780-2
更新日期：1989-06-08 00:00:00
abstract：:Several antimalarial drugs are known to produce a QT interval prolongation via a blockade of the rapidly activating delayed rectifier K+ current (IKr), encoded by the human-ether-a-go-go-related gene (hERG). We investigated the influence of lumefantrine and its major metabolite desbutyl-lumefantrine, as well as halofa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.11.003
更新日期：2004-01-19 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：:Statin therapy is used ubiquitously to reduce cholesterol levels, and recent studies have revealed statin use may be associated with a reduced risk of inflammatory bowel disease (IBD). A comprehensive assessment of the literature was performed to investigate whether statin use may influence the risk of new-onset IBD. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2020.173750
更新日期：2021-01-15 00:00:00
abstract：:The cyclic AMP efflux from rat neostriatal slices induced by simultaneous activation of D-1 (stimulatory) and D-2 (inhibitory) dopamine receptors with 30 microM dopamine was inhibited by morphine (0.3-3 microM), [D-Ala2, D-Leu5]enkephalin (DADLE, 0.03-0.3 microM) but not by [D-Pen2, D-Pen5]enkephalin (DPDPE, 0.03-0.3 ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90150-5
更新日期：1985-12-03 00:00:00
abstract：:This study shows that in spontaneously hypertensive rats (SHR) of 14-weeks-old, the sympathetically-induced, but not noradrenaline-induced tachycardic response are higher than age-matched Wistar normotensive rats. Furthermore, in SHR the sympathetically-induced tachycardic response was: (1) unaffected by moxonidine (3...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.08.017
更新日期：2016-11-15 00:00:00
abstract：:[3H]Idazoxan is a labelled ligand that is frequently used to study alpha 2-adrenoceptors in the central nervous system. In pig kidney membranes, [3H]idazoxan labelled high-affinity binding sites (Kd = 1.5 nM) that were not alpha 2-adrenoceptors and which recognized clonidine with low affinity. This new class of bindin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90503-7
更新日期：1989-01-31 00:00:00
abstract：:Recent studies suggested the involvement of the endocannabinoid pathway on insulin secretion in RINm5F cells or rat islets. Animal and clinical studies have reported beneficial effects of the selective cannabinoid 1 receptor antagonist rimonabant on glucose homeostasis. The aim of this study was to investigate the in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.05.024
更新日期：2009-08-15 00:00:00
