Abstract：
:We hypothesized that uncompetitive NMDA glutamate receptor antagonists memantine (2,5-dimethyl-1-adamantanamine), and amino-alkyl-cyclohexane compounds: MRZ 2/579 (1-amino-1,3,3,5,5-pentamethylcyclohexane HCl), MRZ 2/600 (1-amino-1-ethyl-3,3,5,5-tetramethylcyclohexane HCl), and MRZ 2/615 (1-amino-1,3,5,5-tetramethyl-3-ethylcyclohexane HCl), all derivatives of amantadine (1-adamantanamine HCl), would inhibit the energy-dependent uptake of amantadine into rat renal tubules. All compounds displayed a concentration-dependent inhibition of amantadine uptake in the proximal and distal renal tubules. MRZ 2/579 showed a novel distal tubule selectivity of inhibition (P < 0.001). At a therapeutic amantadine concentration, bicarbonate-dependent transporter inhibition selectivity was observed with all compounds (P < 0.05) except MRZ 2/600, the only compound with a sterically bulky group next to the amino group of the cyclohexane ring structure. Steric hindrance around the ionized amino group of the cyclohexane ring appears to prevent bicarbonate-mediated organic cation transport. Furthermore, the distal tubule inhibition selectivity with MRZ 2/579 provides a novel tool to study the relative importance of organic cation transporters (OCTs) in proximal vs. distal renal tubules.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Fourie J,Escobar MR,Sitar DSdoi
10.1016/s0014-2999(02)02121-0keywords:
subject
Has Abstractpub_date
2002-09-27 00:00:00pages
1-10issue
1eissn
0014-2999issn
1879-0712pii
S0014299902021210journal_volume
452pub_type
杂志文章abstract：:Behavioral and biochemical techniques were used to compare the in vivo intrinsic efficacy of two new 2-(4-aminophenyl)-N, N-dipropylethylamine dopamine D(2) receptor agonists, 2-(4-amino-3-trifluoromethylphenyl)-N-N-dipropyl-ethylamine (NBF-203) and 2-(4-amino-3-bromo-5-trifluoromethylphenyl)-N-N-dipropylethylamine (N...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00158-8
更新日期：2000-04-14 00:00:00
abstract：:The aim of this study was to investigate the effect of cachexia induced by AH-130 cells on gastrointestinal motility in rats. We evaluated food intake, body weight variation, cachexia index, gastric emptying and in vitro gastric responsiveness of control or cachexia rats. In addition, we evaluated the effect of pretre...
journal_title：European journal of pharmacology
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abstract：:Molecular mechanisms responsible for diabetes-induced testicular dysfunction are not well understood. This study investigated oxidative stress, stage-dependent DNA base modification and expression of poly (ADP ribose) polymerase 1 (PARP1) in the testes of streptozotocin-induced diabetic rats. Hyperglycemia led to test...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.05.005
更新日期：2014-08-15 00:00:00
abstract：:Caffeine is the psychostimulant drug most consumed in the world. This drug is present in food, beverages and medicines marketed for individuals of all ages. In spite of this, caffeine effects on adolescents are poorly understood. The aim of this study was to evaluate the differences on caffeine-induced locomotor stimu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.03.052
更新日期：2011-06-25 00:00:00
abstract：:[N-methyl-Nle 28,31)]cholecystokinin-(26-33) (SNF 8702) is a highly selective ligand for the CCKB type of receptor present in the vertebrate central nervous system. Radioligand binding data showing that SNF 8702 binding affinity is reduced by the GTP analog guanylyl-imidodiphosphate suggest that SNF 8702 is an agonist...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(94)90079-5
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00395-2
更新日期：1995-09-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01452-0
更新日期：1998-01-19 00:00:00
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journal_title：European journal of pharmacology
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更新日期：2018-11-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2018-10-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)01287-6
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abstract：:Elevated fatty acid levels play a pathogenic role in the development of insulin resistance, associated with type 2 diabetes. Interventions with ability to ameliorate fatty acid-induced insulin resistance might be useful for the management of diabetes. Here, we explored the effect of the diastereomeric mixture of calop...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.10.049
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.12.043
更新日期：2010-08-10 00:00:00
abstract：:Gamma globin induction remains a promising pharmacological therapeutic treatment mode for sickle cell anemia and beta thalassemia, however Hydroxyurea remains the only FDA approved drug which works via this mechanism. In this regard, we assayed the γ-globin inducing capacity of Cis-vaccenic acid (CVA). CVA induced dif...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(95)00055-p
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.10.037
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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abstract：:The present study investigated the effects of systemic administration of the putative dopamine D3 receptor agonist 7-hydroxy-N,N-di-n-propyl-2-aminotetralin (7-OH-DPAT) on the acquisition and expression of morphine-induced place preference in male Wistar rats. Using a a 3-day schedule of conditioning it was found that...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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abstract：:Persistent hyperglycemia increases a systemic oxidative stress, causing the onset of vascular endothelial dysfunction and atherosclerosis. Diallyl trisulfide (DAT), a natural organosulfur compound in garlic, has been reported to have actions of dilating blood vessels and antibacteria, etc. In this study, models of obe...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.010
更新日期：2014-02-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90552-8
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01555-0
更新日期：1998-02-26 00:00:00
abstract：:An iron-free diet for 28 days caused a reduced level of iron in the blood. Iron deficient rats exhibited a lower level of motor activity and reversed circadian rhythms of thermoregulation and motor activity. The hypothermic effect of d-amphetamine was significantly reduced in iron deficient rats, and the magnitude of ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90048-0
更新日期：1981-09-24 00:00:00
abstract：:Neurotensin is a neuropeptide associated with basal ganglia dopaminergic neurons. Because levels of neurotensin in striatal tissue are differentially affected by low or high doses of methamphetamine, we employed microdialysis to assess the dose-dependent effects of methamphetamine on neurotensin release from the termi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.08.036
更新日期：2005-10-17 00:00:00
