Abstract：
:The 8-substituted 9-ethyladenine derivatives: 8-bromo-9-ethyladenine (ANR 82), 8-ethoxy- 9-ethyladenine (ANR 94), and 8-furyl-9-ethyladenine (ANR 152) have been characterized in vitro as adenosine receptor antagonists. Adenosine is deeply involved in the control of motor behaviour and substantial evidences indicate that adenosine A(2A) receptor antagonists improve motor deficits in animal models of Parkinson's disease. On this basis, the efficacy of ANR 82, ANR 94, and ANR 152 in rat models of Parkinson's disease was evaluated. All compounds tested reversed the catalepsy induced by haloperidol. However, in unilaterally 6-hydroxydopamine-lesioned rats, only ANR 94 and ANR 152 potentiated l-dihydroxy-phenylalanine (l-DOPA) effect on turning behaviour and induced contralateral turning behaviour in rats sensitised to l-DOPA. Taken together the results of this study indicate that some 8-substituted 9-ethyladenine derivatives ameliorate motor deficits in rat models of Parkinson's disease, suggesting a potential therapeutic role of these compounds.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Pinna A,Volpini R,Cristalli G,Morelli Mdoi
10.1016/j.ejphar.2005.01.057keywords:
subject
Has Abstractpub_date
2005-04-11 00:00:00pages
157-64issue
2-3eissn
0014-2999issn
1879-0712pii
S0014-2999(05)00153-6journal_volume
512pub_type
杂志文章abstract：:Glucose is the primary energy fuel of life. A glucose transporter, the sodium-glucose transporter (SGLT), is receiving attention as a novel therapeutic target in disease. This review summarizes the physiological role of SGLT in cerebral ischemia, cancer, cardiac disease, and intestinal ischemia, which has encouraged a...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2018.01.003
更新日期：2018-03-05 00:00:00
abstract：:The role of flexibility of the alkyl side chain in the tetrahydrocannabinols to cannabinoid activity has been delineated in previous studies with side chain analogs of Delta(8)-tetrahydrocannabinol with double or triple bonds. This study investigated the site of antinociceptive action for these analogs through analysi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00259-4
更新日期：2000-06-02 00:00:00
abstract：:The in vivo pharmacological profiles of the selective tachykinin NK1 receptor agonists, [Sar9,Met(O2)11]substance P and GR 73632, were examined in gerbils. Both agonists induced a pronounced chromodacryorrhea following intravenous injection which was stereoselectively antagonised by the tachykinin NK1 receptor antagon...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90198-8
更新日期：1994-03-03 00:00:00
abstract：:The pre- and postsynaptic actions of the calcium entry facilitator Bay K 8644 were investigated in the rat isolated vas deferens. Bay K 8644 had no presynaptic effect on adrenergic neurotransmission in the epididymal portion. Bay K 8644 and alpha 1-adrenoceptor agonists potentiated, and the calcium entry blocker nifed...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90414-x
更新日期：1984-09-17 00:00:00
abstract：:Previous work has demonstrated that neuropeptide tyrosine (NPY), Y(1) receptor and Y(2) receptor are critical in modulation of pain after nerve injury. We hypothesized that NPY was important for nociception after surgical incision. As a model of postoperative pain, rats underwent a plantar incision in one hindpaw. Wes...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.10.036
更新日期：2013-01-05 00:00:00
abstract：:The beta-antagonistic effects of celiprolol were assessed in isolated guinea-pig preparations. The pA2 values obtained were 7.84 +/- 0.07, 7.79 +/- 0.06 and 6.45 +/- 0.11 against the positive chronotropic and inotropic effects in the atria and relaxant effects in the trachea induced by isoproterenol, respectively, ind...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90115-7
更新日期：1991-02-26 00:00:00
abstract：:The alpha7 (α7) nicotinic acetylcholine receptor is a therapeutic target for cognitive disorders. Here we describe 3-(3,4-difluorophenyl)-N-(1-(6-(4-(pyridin-2-yl)piperazin-1-yl)pyrazin-2-yl)ethyl)propanamide (B-973), a novel piperazine-containing molecule that acts as a positive allosteric modulator of the α7 recepto...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2017.01.037
更新日期：2017-03-15 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：:We previously reported that both nitric oxide (NO) generated from NO synthase by bombesin and NO generated from SIN-1 (NO donor) activate the brain cyclooxygenase (COX) (COX-1 for bombesin), thereby eliciting the secretion of both catecholamines (CA) from the adrenal medulla by brain thromboxane A(2)-mediated mechanis...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.01.005
更新日期：2012-03-15 00:00:00
abstract：:Recent studies in this laboratory have demonstrated the ability of acetylcholine receptor agonists to produce systemic arterial pressor responses through stimulation of spinal muscarinic receptors. In urethane-anesthetized rats a new surgical procedure was employed to permit microinjection of drugs into the cerebrospi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90039-k
更新日期：1993-12-21 00:00:00
abstract：:Clonidine and methysergide constrict the rabbit auricular artery by activating smooth muscle alpha-adrenoceptors. Clonidine inhibits and methysergide enhances responses to stimulation of the sympathetic nerves. Both drugs sensitise the artery to a variety of vasoconstrictor stimuli, although not to potassium chloride....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90264-8
更新日期：1976-03-01 00:00:00
abstract：:The administration of the synthetic and stable opioid peptide[D-Ala2,MePhe4,Met(O)5o1]enkephalin (FK 33-824) at the dose of 0.2 mg/kg i.v. induced a rise in plasma levels of prolactin in the rat, an effect which was prevented by 1 mg/kg i.v. of the opiate antagonist naloxone. A simultaneous i.v. injection of 20 microg...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90009-7
更新日期：1982-01-22 00:00:00
abstract：:The formation of epidural fibrosis adjacent to the dura mater is a complex multi-step process that is associated with a marked reduction in tissue cellularity and the excessive deposition of extracellular matrix components. Extensive epidural fibrosis is a major cause of post-laminectomy syndrome. Decorin strongly inh...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.12.017
更新日期：2014-02-05 00:00:00
abstract：:Infusion of tryptamine (1-4 mug/ml) through the pulmonary circulation of rat isolated lung perfused with Krebs solution caused release of a mixture of spasmogens contracting isolated smooth muscle preparations. One component of this mixture had biological activity comparable to E-type prostaglandins. Other components ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90238-7
更新日期：1976-02-01 00:00:00
abstract：:The tertiary nitrogen derivatives of two choline esters, chloroacetylcholine and acrylcholine, known to inhibit choline acetyltransferase (ChAc) in vitro, were tested for their effects in the whole animal, including peripheral and central cholinergic systems. These esters are N,N-dimethylaminoethyl chloroacetate (Cl-D...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(76)90357-5
更新日期：1976-11-01 00:00:00
abstract：:Characteristics of [3H]flunitrazepam ([3H]FLU) binding to cortical and cerebellar membrane receptors were examined following chronic (six days) administration of phenobarbital (PB) to C57B1 mice. Following PB treatment, the number of [3H]FLU binding sites (Bmax) was significantly reduced in both cerebral cortex and in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90497-7
更新日期：1984-08-17 00:00:00
abstract：:B cell antigen presentation, cytokine production, and antibody production are targets of pharmacological intervention in inflammatory and infectious diseases. Here we review recent pre-clinical evidence demonstrating that pharmacologically relevant levels of n-3 polyunsaturated fatty acids (PUFA) derived from marine f...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.03.100
更新日期：2016-08-15 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：:5-HT(1A) receptor activation by the very-high-efficacy, selective 5-HT(1A) receptor agonist F 13640 [(3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-([(5-methyl-pyridin-2-ylmethyl)-amino]-methyl)piperidin-1-yl]-methanone] was recently discovered to constitute a novel central mechanism of broad-spectrum analgesia that, remarkab...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01566-8
更新日期：2003-04-18 00:00:00
abstract：:It has been shown that G-protein coupled receptors have seven transmembrane alpha-helices, but the structural changes occurring in a G-protein coupled receptor as a response on agonist stimulus and the molecular events leading to blockade of the signal transduction by antagonists are not well understood. In the presen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00860-3
更新日期：2001-03-23 00:00:00
abstract：:We used two experimental models to prove that resveratrol (trans-3,4',5-trihydroxystilbene) reduces cardiac ischemic-reperfusion injury by means of a nitric oxide- and adenosine-dependent mechanism. (1). ACUTE EX VIVO: resveratrol (10 microM, 10 min) infusion in Langendorff-perfused normoxic rat hearts significantly i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01441-9
更新日期：2003-03-28 00:00:00
abstract：:Possible changes in noradrenergic function were investigated in rat frontal cerebral cortex after acute treatment (1, 2 h) with the GABAB agonist, baclofen. A single i.p. injection of d,l-baclofen 10 mg/kg both reduced noradrenaline (NA) biosynthesis in vivo (31%) and the endogenous concentration of normetanephrine (N...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90369-2
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abstract：:Renal hemodynamics were studied using an electromagnetic perivascular flow sensor in anesthetized rats injected i.v. with vehicle, 5 or 10 mg/kg body weight (b.w.) sulindac. No hemodynamic changes occurred with vehicle (n = 6), but mean arterial pressure was significantly decreased (by 15 mmHg) with sulindac (n = 12)....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)00178-7
更新日期：1997-07-09 00:00:00
abstract：:CP-96,345, a non-peptide, selective tachykinin NK1 receptor blocker and its inactive enantiomer, CP-96,344, inhibit ligand binding of phenylalkylamine but not dihydropyridine Ca2+ channel antagonists. Whether these Ca2+ channel antagonist properties of CP-96,345 and CP-96,344 can be expressed as cardiovascular effects...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90173-2
更新日期：1994-02-11 00:00:00
abstract：:We investigated the involvement of dopamine D1 and D2 receptor subtypes in the effects of GBR 12909, a selective dopamine uptake inhibitor, on latent learning in the performance of a water-finding task and on locomotor activity in mice. GBR 12909 (10 and 20 mg/kg) impaired latent learning, and this effect was countera...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90949-i
更新日期：1993-04-06 00:00:00
abstract：:Several phenyl-benzazepine compounds, putatively selective dopamine D1 receptor agonists, have been used to study the effects of dopamine D1 receptor stimulation in rodents and nonhuman primates. However, the dopamine receptor selectivities of these compounds have not been established in nonhuman primates. Accordingly...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00669-4
更新日期：1998-11-13 00:00:00
abstract：:The association of G-proteins with the T-cell-specific receptor structures CD3 and CD2 was investigated. High-affinity GTPase activity in membrane preparations of the human leukemic T-cell line Jurkat could be induced by the monoclonal antibodies OKT3 (anti-CD3) and OKT11 (anti-CD2). When combining maximally active co...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(90)90033-t
更新日期：1990-12-15 00:00:00
abstract：:[D-Met2,Pro5]enkephalinamide (DMPEA) strongly activated cardioinhibitory vagal efferents and elicited bradycardia when perfused through the cerebroventricular system of anaesthetized dogs. These effects were concentration-dependent but plateaued at an intraventricular concentration of 200 micrograms/ml. At this maxima...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90216-x
更新日期：1985-04-02 00:00:00
abstract：:Antinociceptive effects of various neuroleptics in animal acute pain-models have been described, mediated trough different pathways including the opioid system. In this study, we assessed the antinociceptive effects of the atypical neuroleptic drug amisulpride, which acts as a selective blocker of dopamine D2 and D3 r...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.08.049
更新日期：2003-10-08 00:00:00
abstract：:We investigated the effects of the platelet activating factor (PAF) receptor antagonists, SM-12502 ((+)-cis-3,5-dimethyl-2-(pyridyl)- thiazolidin-4-one hydrochloride), WEB-2086 (3-(4-(2-chlorphenyl)-9-methyl-6H-thieno(3,2-f)-(1,2,4)triazolo(4, 3- a)(1,4)diazepin-2-yl)-1-(4-morpholinyl)-1-propanone) and RP-48740 (3-(3-...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90037-x
更新日期：1994-11-15 00:00:00
