Abstract：
:It has been shown that analgesics such as morphine, lidocaine and clonidine increase the release of spinal acetylcholine. Acetylcholine may therefore play an important role in the regulation of spinal pain threshold. Since behavioral as well as in vitro studies have shown a clear involvement of GABA (gamma-amino butyric acid) receptors in the regulation of spinal nociceptive mechanisms, the present study focused on the role of GABA receptors for spinal acetylcholine release control. GABA receptor agonists and antagonists were infused via a spinal microdialysis probe and acetylcholine release was measured. The GABA(A) receptor agonist muscimol decreased acetylcholine release and the antagonist bicuculline increased acetylcholine release. The GABA(B) receptor agonist baclofen decreased acetylcholine release whereas the antagonist saclofen did not change acetylcholine release. The results suggest that both GABA receptor subtypes have an inhibitory role on spinal dorsal horn acetylcholine release and that the GABA(A) receptors are tonically regulating acetylcholine release.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kommalage M,Höglund AUdoi
10.1016/j.ejphar.2005.08.035keywords:
subject
Has Abstractpub_date
2005-11-21 00:00:00pages
69-73issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(05)00887-3journal_volume
525pub_type
杂志文章abstract：:We studied the effects of the tyrosine kinase inhibitors genistein and tyrphostin and the tyrosine phosphatase inhibitors sodium orthovanadate and phenylarsine oxide on endotoxin-mediated induction of nitric oxide (NO) synthase in rat aorta and its effects on vascular contractility. Genistein (i.p. 10 mg/kg) inhibited...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01311-3
更新日期：1997-10-29 00:00:00
abstract：:Ryanodine at nanomolar concentrations suppressed the earlier of two contraction components which can be produced in guinea-pig papillary muscles, in the presence of noradrenaline (3 microM) at a low contraction frequency (0.2 Hz). However, test contractions elicited shortly after a steady state contraction showed an u...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90437-2
更新日期：1988-01-19 00:00:00
abstract：:The novel antiepileptic drug levetiracetam has been shown to reverse anxiogenic effects of benzodiazepine withdrawal in mice tested in an elevated plus-maze without altering the behaviour of normal mice in this model. This could suggest that the effect of levetiracetam is dependent upon the level of stress/anxiety of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01724-2
更新日期：2003-05-23 00:00:00
abstract：:The effect of morphine on the capsaicin-induced cough reflex was studied in mu 1-opioid receptor-deficient CXBK mice. There was no significant difference between the morphine-induced antitussive effect in CXBK mice and C57BL/6 mice, a progenitor strain. Furthermore, the antitussive effects of morphine in both the CXBK...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90553-t
更新日期：1993-08-10 00:00:00
abstract：:The goal of these investigations was to study the role of tachykinin NK2 receptors in neonatal spinal cords using the selective NK2 receptor agonist [beta-Ala8]neurokinin A-(4-10) and the new NK2 receptor antagonist GR 94800. Experiments were performed with superfused hemisected rat and gerbil spinal cords. Dorsal roo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90053-1
更新日期：1994-06-02 00:00:00
abstract：:With some latency, ouabain (10(-6)--10(-5) M) induced a long-lasting contractile response of the isolated vas deferens of the guinea-pig. The ouabain-induced contraction was potentiated by pretreatment with tropolone, whereas it was prevented by pretreatment with cocaine, bretylium, reserpine or phentolamine. The resp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90121-8
更新日期：1978-02-15 00:00:00
abstract：:CysLT1 receptors are known to be involved in the pathogenesis of asthma. However, the functional roles of CysLT2 receptors in this condition have not been determined. The purpose of this study is to develop an experimental model of CysLT2 receptor-mediated LTC4-induced lung air-trapping in guinea pigs and use this mod...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.036
更新日期：2017-01-05 00:00:00
abstract：:Given the differences in the dopamine neurotransmission between the shell and the core of the nucleus accumbens, as well as the differential involvement of these two domains in oral behaviour of rats, it was decided to determine whether or not dopamine D1 and/or dopamine D2 receptors differentially direct oral behavio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00428-n
更新日期：1995-11-03 00:00:00
abstract：:Binding of the radioligand [125I]iodoclonazepam to three different areas of rat brain (cerebellum, hippocampus and striatum) has been characterised. In all three regions binding is rapid, saturable and of high affinity (cerebellum Bmax = 1.49 +/- 0.3 pmol/mg of protein, Kd = 0.39 +/- 0.06 nM; hippocampus Bmax = 1.5 +/...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90484-8
更新日期：1991-04-03 00:00:00
abstract：:The present study was designed to characterize the vasopressin receptor subtype involved in the vasopressin-induced activation of the central sympatho-adrenomedullary outflow using urethane-anesthetized rats. Intracerebroventricularly (i.c.v.) administered vasopressin (0.1, 0.2 and 0.5 nmol/animal) dose-dependently el...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02652-3
更新日期：2002-12-13 00:00:00
abstract：:The choleretic action of 3-(2,4,5-triethoxybenzoyl)propionic acid (AA-149) was studied in anesthetized dogs. AA-149 produced a dose-dependent increase of the bile flow with both i.v. and intrajejunal administration of doses 1 mg/kg and higher. Biliary clearance of 14C-erythritol showed that AA-149 stimulated canalicul...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90050-x
更新日期：1978-03-01 00:00:00
abstract：:Abnormal proliferation and hypertrophy of vascular smooth muscle (VSMC), as the main structural component of the vasculature, is an important pathological mechanism of hypertension. Recently, increased levels of arginine vasopressin (AVP) and copeptin, the C-terminal fragment of provasopressin, have been shown to corr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.10.023
更新日期：2016-12-05 00:00:00
abstract：:To investigate the effect of a single and multiple administration of lysergic acid diethylamide (LSD) on cerebral metabolism of dopamine and serotonin, male Wistar rats were treated with low and high doses (0.1 and 2.0 mg/kg i.p.) of LSD and the levels of dopamine, 3,4-dihydroxyphenylacetic acid, homovanillic acid, 3-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01025-x
更新日期：1997-07-30 00:00:00
abstract：:Antidepressant drugs are currently one of the most prescribed medications. In addition to treatment resistance and side effects of antidepressants, their clinical use is further complicated by antidepressant discontinuation syndrome (ADS). ADS is a common problem in patients following the interruption, dose reduction,...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2018.04.003
更新日期：2018-06-15 00:00:00
abstract：:Heparin is a natural polymer widely used in medicine especially during the treatment of cardiovascular diseases since it is a potent blood anticoagulant. In case of emergency, e.g., massive hemorrhage, the anticoagulant activity of heparin has to be quickly stopped by the administration of a heparin reversing agent. C...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.04.037
更新日期：2012-07-05 00:00:00
abstract：:(5R,6R)-6-(3-Propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[ 3.2.1]octane (PTAC) is a selective muscarinic receptor ligand. The compound exhibits high affinity for central muscarinic receptors with partial agonist mode of action at muscarinic M(2) and M(4) and antagonist mode of action at muscarinic M(1), M(3) and M(5...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00442-8
更新日期：2000-08-25 00:00:00
abstract：:Nanomolar concentrations of atropine have been considered up to now to be selective for blockade of muscarinic receptors for acetylcholine. A collateral finding indicated to us that these low concentrations of atropine could also target the neuronal nicotinic receptors. We report here a detailed study on this novel pr...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.01.057
更新日期：2006-03-27 00:00:00
abstract：:SB203580 is the prototypical p38 MAPK inhibitor; however it cannot be used clinically due to liver toxicity. We developed a structural analogue of SB203580 - ML3403 - with equal in vitro and ex vivo p38alpha MAPK inhibition as SB203580, but with reduced activity towards liver cytochrome P450 enzymes. In addition, we d...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.02.037
更新日期：2010-06-10 00:00:00
abstract：:Previous studies have shown that sertindole (1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl]ethyl ]-2 imidazolidinone), an atypical antipsychotic drug that is a potent 5-HT2A and dopamine D2 receptor antagonist, preferentially affects mesocorticolimbic rather than mesostriatal dopamine neurons. Usin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00936-4
更新日期：1999-02-12 00:00:00
abstract：:Goniothalamin, a natural occurring styryl-lactone, is a novel compound with putative anticancer activities. In the present study, the mechanism of action of goniothalamin was further investigated in human breast cancer MDA-MB-231 cells. Goniothalamin treatment of cells significantly induced cell cycle arrest at G(2)/M...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.08.047
更新日期：2005-10-17 00:00:00
abstract：:The aim of the present investigation was to evaluate the antidiabetic activity of cycloart-23-ene-3beta, 25-diol (called as B2) isolated from stem bark of Pongamia pinnata in streptozotocin-nicotinamide induced diabetic mice. Diabetes was induced in mice by injecting streptozotocin (200mg/kg, i.p.) after 15 min nicoti...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2010.01.019
更新日期：2010-04-25 00:00:00
abstract：:A sensitive high pressure liquid chromatography (HPLC) method was used to measure acetylcholine release from canine bronchial tissue in response to electrical stimulation. Indomethacin enhanced the efflux of acetylcholine, an effect that was reversed by the addition of prostaglandin E2 (PGE2). Prostaglandin D2 (PGD2) ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90451-2
更新日期：1989-08-29 00:00:00
abstract：:Most virus infections induce cycloxygenase-2 (COX-2) expression and subsequent prostaglandin E(2) (PGE(2)) production in cells, an inflammatory response that might be detrimental to virus replication and pathogenesis. This response in dengue virus infection remains to be elucidated. Triptolide and tetrandrine, compoun...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.04.056
更新日期：2008-07-28 00:00:00
abstract：:The aim of this work was to investigate the effect of P-glycoprotein modulators on human extraneuronal monoamine transporter (EMT)-mediated transport. The experiments were performed using a cell line from human embryonic kidney (HEK293 cells) stably transfected with pcDNA3hEMT (293(hEMT)), or with pcDNA3 alone (293(co...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01055-x
更新日期：2001-06-22 00:00:00
abstract：:Calcium channel blockers appear to reduce the cardiac toxicity of cocaine and some stimulant-induced behaviors. The present experiment was designed to test whether the internal state induced by cocaine is altered by the calcium antagonist nimodipine. Substitution tests with the calcium agonist BAY K 8644 were also con...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)94072-6
更新日期：1990-09-04 00:00:00
abstract：:On exposure to triphosphatic nucleotides vas deferens DDT1 MF-2 smooth muscle cells responded with an outward K+ current as measured with the whole-cell patch clamp configuration. The rank order of potency was: ATP greater than UTP greater than TTP greater than CTP = GTP. The responses evoked by these agonists were bl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90048-9
更新日期：1992-05-14 00:00:00
abstract：:Recombinant vaccinia viruses harboring the human dopamine D4 receptor cDNA containing two 48 base pair-repeats (D4.2) or the rat dopamine D2 short (D2s) receptor cDNA were used to infect rat-1 fibroblasts. Heterologous expression of both dopamine receptors was demonstrated in binding assays. The affinity constants of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(95)90011-x
更新日期：1995-06-23 00:00:00
abstract：:Beat-to-beat alternations of the cardiac monophasic action potential, known as electrical alternans, were studied at drug concentrations that have known arrhythmogenic outcomes. Electrical alternans were elicited from the heart of anesthetized guinea pigs, both in the absence and presence of drugs that inhibit the del...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.12.028
更新日期：2004-02-20 00:00:00
abstract：:A previous report showed that transforming growth factor-beta1 (TGF-beta1) can induce heme oxygenase-1 (HO-1) expression, attenuate cellular injury, and maintain tissue homeostasis. In this study, we investigated the involvement of phosphoinositide-3-OH-kinase (PI3K)/Akt and the nuclear factor-kappaB (NF-kappaB) signa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.01.025
更新日期：2007-04-10 00:00:00
abstract：:The effects of amiloride on contraction evoked by perivascular nerve stimulation were studied in a ring preparation of rat mesenteric artery. The contraction evoked by nerve stimulation was abolished by tetrodotoxin or prazosin. Amiloride depressed the nerve-induced contraction concentration dependently. Noradrenaline...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00879-5
更新日期：1997-02-05 00:00:00
