Abstract：
:We investigated whether tolerance develops to the vasorelaxant effects of a new vasodilator, (+-)-(E)-4-ethyl-2-[(E)-hydroxy-imino]-5-nitro-3-hexenamide (FK409), in isolated canine coronary artery strips and to its hypotensive effect in rats, and whether FK409 activates soluble guanylate cyclase isolated from vascular tissues in the absence of L-cysteine. No tolerance to FK409 (0.46 nM to 0.46 microM or 1-1000 micrograms/kg, i.v.) or cross-tolerance between FK409 and glyceryl trinitrate was demonstrated in in vitro and in vivo experiments, whereas the tolerance to glyceryl trinitrate (0.44 nM to 4.4 microM or 1-1000 micrograms/kg, i.v.) was marked in both conditions. In addition, FK409 (0.1-10 microM) activated soluble guanylate cyclase without L-cysteine, but glyceryl trinitrate (1-100 microM) required the addition of L-cysteine (5 mM) for the activation of the enzyme. The results suggest that FK409 may be advantageous compared to tolerance-producing nitrates currently in clinical use, and that this property of FK409 is probably due to its independence of a sulfhydryl group donor.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Isono T,Sato N,Yamamoto T,Sawada T,Yamazaki S,Miura S,Furuichi A,Ozaki R,Koibuchi Y,Ohtsuka Mdoi
10.1016/0014-2999(94)90333-6subject
Has Abstractpub_date
1994-08-01 00:00:00pages
163-8issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(94)90333-6journal_volume
260pub_type
杂志文章abstract：:Using a batch method for incubation of hippocampal slices, we have examined the effects of 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (RU24969) and (m-trifluoromethylphenyl)piperazine (TFMPP) on release of endogenous 5-hydroxytryotamine (5-HT). Release of 5-HT from slices was enhanced by RU24969 and TFMPP ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94111-a
更新日期：1990-11-06 00:00:00
abstract：:We have investigated the effect of inhaled HOE 140, a novel bradykinin B2 receptor antagonist, against bradykinin- and vagal stimulation-induced airway microvascular leakage and bronchoconstriction in anesthetized guinea-pigs. Lung resistance was measured for 6 min after challenge, followed by measurement of extravasa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90393-x
更新日期：1994-01-14 00:00:00
abstract：:The effect of systemic administration of the nonselective dopamine receptor agonist apomorphine on efflux of serotonin (5-hydroxytryptamine, 5-HT) in striatum and hippocampus of freely moving rats was examined using in vivo microdialysis. 5-HT efflux was increased by a moderate dose of apomorphine sufficient for a pos...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00321-5
更新日期：1998-06-26 00:00:00
abstract：:We studied the relationships between arachidonic acid (AA) metabolism and contractile responses to Na arachidonate (NaA) and the prostaglandins (PGs) in mesenteric arteries isolated from sham-operated and totally pancreatectomized dogs. PGE2 and PGF2 alpha produced a similar dose-dependent relaxation of mesenteric art...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90480-1
更新日期：1984-08-17 00:00:00
abstract：:Morphine produces a state dependent learning. The hippocampus is involved in this kind of learning. Gap junctions (GJs) are involved in some of the effects of morphine and exist in different areas of the hippocampus. We investigated the effects of blocking GJ channels of the hippocampal CA1 area, by means of pre-test ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.10.040
更新日期：2014-12-15 00:00:00
abstract：:Capsaicin (1-3 microM) and electrical stimulation of mesenteric nerves in the presence of hexamethonium and guanethidine antidromically stimulate extrinsic sensory nerve fibers to produce a specific slow depolarizing response of myenteric neurons and a contractile response of muscles in the isolated guinea-pig ileum, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90092-v
更新日期：1993-06-11 00:00:00
abstract：:In the present study, the P2Y receptor(s) mediating the effects of the pyrimidines UTP and UDP on phospholipase C activation in the mouse neuroblastoma x rat glioma hybrid cell line NG108-15 was investigated. Reverse Transcriptase-Polymerase Chain Reaction (RT-PCR) analysis detected transcripts for the P2Y(6) and P2Y(...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00845-7
更新日期：2001-03-01 00:00:00
abstract：:AMN082 is a selective metabotropic glutamate mGlu7 receptor agonist reported to exhibit antidepressant activity. Considering that excessive glutamate release is involved in the pathogenesis of depression, the effect of N,N'-dibenzyhydryl-ethane-1,2-diamine dihydrochloride (AMN082) on glutamate release in rat cerebroco...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.01.038
更新日期：2018-03-15 00:00:00
abstract：:We assessed the intrinsic activity of the purported selective muscarinic M1 receptor agonist SR 95639A (morpholinoethylamino-3-benzocyclohepta-(5,6-c)-pyridazine) in inducing several receptor-mediated signals. Our results indicate that SR 95639A lacks the ability to activate phosphoinositide hydrolysis in rat cerebral...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90126-g
更新日期：1992-10-01 00:00:00
abstract：:The concentration of blood glucose was measured in rats after administration of a number of drugs characterized as dopamine agonists. Compounds that cause release of dopamine, or agents that block the reuptake of dopamine, did not elevate blood glucose. Some direct dopamine receptor stimulants (lergotrile, bromocripti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90234-0
更新日期：1983-06-03 00:00:00
abstract：:To elucidate the mechanism of age-related changes in the cardiovascular function stimulated with angiotensin II, we examined the effects of angiotensin II on the coronary flow, production of nitric oxide (NO) and prostacyclin, and on the cardiac function in the Langendorff-perfused young and aged rats' hearts. Angiote...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00575-0
更新日期：1999-10-01 00:00:00
abstract：:In isolated strips of human urinary bladder detrusor muscle, ATP, alpha, beta-methylene ATP and P1,P6-diadenosine hexaphosphate caused concentration-dependent contractions. ATP was less potent than the two synthetic purine compounds and gave smaller maximum responses. Responses to ATP, P1,P6-diadenosine hexaphosphate ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90881-9
更新日期：1989-12-12 00:00:00
abstract：:We investigated the acute and chronic effects of alpha 2-adrenoceptor and muscarinic receptor agonists on dihydropyridine-sensitive voltage-dependent Ca2+ channels in spinal cord-dorsal root ganglion cocultures. Clonidine and oxotremorine inhibited the voltage-dependent Ca2+ influx (42 +/- 2% and 35 +/- 6% with 100 mi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(93)90060-m
更新日期：1993-01-04 00:00:00
abstract：:The administration of a small dose of apomorphine (50 micrograms/kg s.c.) induced repeated episodes of yawning in male rats. Short-term (3 days) treatment with 17 beta-estradiol antagonized apomorphine-induced yawning in male rats. Moreover, apomorphine induced yawning much less effectively in female than in male rats...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90418-7
更新日期：1984-09-17 00:00:00
abstract：:Mastoparan activated membrane-bound guanylate cyclase and potentiated the effect of atrial natriuretic factor (ANF) and ATP on guanylate cyclase activity in rat lung membranes. Mastoparan is a cationic, amphiphilic tetradecapeptide with an amidated carboxyl terminus. It takes the alpha-helical conformation upon intera...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(93)90196-g
更新日期：1993-11-15 00:00:00
abstract：:Endothelin-1 (ET-1) is reported to be the most powerful constrictor of blood vessels known. Atrial natriuretic factor is a potent relaxor of contracted vessels. This study examined the potential interaction between these vasoactive peptides on rabbit aortic rings. ET-1 contracted the rings in a dose-dependent manner w...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94168-w
更新日期：1990-12-04 00:00:00
abstract：:Learning and memory in the brain likely occur through activity-dependent, long-lasting changes in synaptic transmission. Two opposite activity-dependent synaptic modifications have been identified so far, long-term potentiation and long-term depression. In many brain areas including hippocampal CA1 and neocortex, the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2007.11.084
更新日期：2008-05-06 00:00:00
abstract：:In the brain, various neurotransmitters such as noradrenaline and GABA regulate peripheral sympathetic functions. Previously, it has been reported that both β-adrenoceptor activation and GABAB receptor activation in the brain are involved in the elevation of plasma noradrenaline levels. However, it is unknown whether ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.01.029
更新日期：2019-04-05 00:00:00
abstract：:Mitomycin C (MMC) is known to reduce epidural fibrosis, but the underlying mechanisms have not yet been elucidated. Aberrant miR-200b expressions have been reported in multiple types of fibrotic tissues from many diseases. The aim of this study was to clarify the mechanism by which MMC induces fibroblasts apoptosis an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2015.08.002
更新日期：2015-10-15 00:00:00
abstract：:The purpose of the current study was to assess neuropeptidergic alterations during a phase of the drug addiction cycle associated with drug craving as compared to a time period when the drug had been recently self-administered. Male Wistar rats were allowed to self-administer cocaine, heroin or saline for 6 h for 5 co...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00874-7
更新日期：1999-01-22 00:00:00
abstract：:Intracellular recording was used to study the effect of uncouplers of oxidative phosphorylation on miniature endplate potentials (m.e.p.p.s) in skeletal muscles from dystrophic mice and their clinically normal littermates. Control m.e.p.p. frequency in muscles from dystrophic mice was not significantly different from ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90637-1
更新日期：1988-02-16 00:00:00
abstract：:Atherosclerosis is a leading cause of death worldwide. It is a complex chronic inflammatory disease involving interactions between vascular, circulating and immune cells. B cells play an important role in chronic inflammation producing antibodies and regulating T and natural killer (NKT) cell activation. The role of B...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2017.09.002
更新日期：2017-12-05 00:00:00
abstract：:Acid-sensing ion channels (ASICs) are involved in numerous physiological and pathological processes in the central nervous system. Development of pharmacological tools capable to inhibit or potentiate these channels is important for our knowledge about roles of ASICs in the neuronal network and can be promising for tr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.06.013
更新日期：2016-10-05 00:00:00
abstract：:Recent evidence suggests that polydatin (PD), a resveratrol glucoside, may have beneficial actions on the cardiac hypertrophy. Therefore, the current study focused on the underlying mechanism of the PD anti-hypertrophic effect in cultured cardiomyocytes and in progression from cardiac hypertrophy to heart failure in v...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.11.012
更新日期：2015-01-05 00:00:00
abstract：:The action of antidepressants on cell proliferation (bromodeoxyuridine (BrdU) or [3H]thymidine incorporation) was studied in the adult rat hippocampus in vivo and in neural precursors (immature rat cerebellar granule cells) in vitro. In vivo, prolonged (21 days) but not acute (single) intraperitoneal treatment with fl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00904-3
更新日期：2001-01-05 00:00:00
abstract：:Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive loss of memory and cognitive deficit. The observed amnesia in the early stages of AD is suggested to be a retrieval problem, rather than encoding and consolidation deficit. According to the cholinergic hypothesis of AD, scopolamine i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.12.007
更新日期：2018-01-15 00:00:00
abstract：:It has been suggested that administration of a cannabinoid CB(1) (SR141716A ¿N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1-H-pyrazole-3-carboxamide) and CB(2) (SR144528 ¿N-[(1S)-endo-1, 3, 3-trimethyl bicyclo ¿2.2.1 heptan-2-yl]-5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-pyr azo le- 3-ca...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00226-0
更新日期：2000-05-19 00:00:00
abstract：:Fenfluramine + phentermine was a widely used combination for weight loss. Fenfluramine and phentermine are believed to act via serotonin and catecholamines, respectively. To what extent these drugs interact has not been well-established. We compared the anorectic efficacy of a range of doses of the combination (using ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00235-6
更新日期：1999-06-04 00:00:00
abstract：:Anti-tumor activity of bakuchiol, an analogue of resveratrol, was investigated on human lung adenocarcinoma A549 cell line. MTT assay revealed that IC(50) of bakuchiol at 72h was 9.58+/-1.12 micromol/l, much lower than that of resveratrol (33.02+/-2.35 micromol/l). Bakuchiol but not resveratrol elevated intracellular ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.06.025
更新日期：2010-09-25 00:00:00
abstract：:The effects of intraperitoneal injections of two opioid antagonists on plasma corticosterone levels in stressed mice was investigated. The effects of the mu-opioid receptor antagonist naloxone was dependent on the dose used. Low doses (0.5 and 1 mg/kg) potentiated the elevation of plasma corticosterone observed in sal...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90042-6
更新日期：1984-05-18 00:00:00
