Abstract:
:Nimodipine is a 1,4-dihydropyridine (DHP) calcium channel blocker which is used in the treatment of neurological deficits associated with subarachnoid hemorrhage. Small angle x-ray diffraction, differential scanning calorimetry, and equilibrium and kinetic binding techniques were used to study the interaction of nimodipine with bovine brain phosphatidylcholine (BBPC) membranes of varying cholesterol content. At concentrations (5 x 10(-10) M) near its Kd, the membrane partition coefficient of nimodipine was inversely related to the cholesterol to phospholipid (C:P) mole ratio in both model and native (rat synaptoneurosome) membranes. The nonspecific dissociation rate of nimodipine from BBPC was significantly slower at low C:P mole ratio (0.1:1) than at high C:P mole ratio (0.6:1). Calorimetric analysis showed that nimodipine decreased both the main phase transition temperature and cooperative unit size of melt for dimyristoyl phosphatidylcholine, dependent on membrane cholesterol content. Small angle x-ray diffraction analysis showed that nimodipine occupies a position in BBPC approx +/- 15 A from the center of the hydrocarbon core, near the hydrocarbon core/water interface. These data indicate that nimodipine is an amphiphilic molecule which rapidly washes out of and transports across membrane bilayers, facilitating its interactions with membranes and possibly its transport across the blood-brain barrier.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Herbette LG,Mason PE,Sweeney KR,Trumbore MW,Mason RPdoi
10.1016/0028-3908(94)90015-9subject
Has Abstractpub_date
1994-02-01 00:00:00pages
241-9issue
2eissn
0028-3908issn
1873-7064journal_volume
33pub_type
杂志文章abstract::The hypothesis that aberrant alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor activity contributes to epileptogenesis and neurodegeneration has prompted the search for AMPA receptor antagonists as potential therapeutics to treat these conditions. We describe the functional characterization of a...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(01)00170-8
更新日期:2002-02-01 00:00:00
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journal_title:Neuropharmacology
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更新日期:2010-01-01 00:00:00
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journal_title:Neuropharmacology
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更新日期:2008-12-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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journal_title:Neuropharmacology
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abstract::In several strains of mice: Swiss CD1, BALB, DBA2, C57, the mixed D1/D2 direct dopamine receptor agonist, apomorphine, elicited a marked and virtually similar hypothermic effect. By contrast, in C3H mice, this effect was obviously less and shorter. Similarly, the hypothermic effects of two direct D2 dopamine agonists ...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(92)90007-c
更新日期:1992-11-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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更新日期:2015-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:1989-04-01 00:00:00
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journal_title:Neuropharmacology
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更新日期:1983-02-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2004.02.007
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journal_title:Neuropharmacology
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更新日期:1993-09-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,评审
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journal_title:Neuropharmacology
pub_type: 杂志文章
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更新日期:1996-01-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(84)90202-8
更新日期:1984-03-01 00:00:00
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pub_type: 杂志文章,评审
doi:10.1016/j.neuropharm.2004.04.016
更新日期:2004-09-01 00:00:00
abstract::The function of 5-HT1A autoreceptors was examined by measuring the ability of the 5-HT1A receptor agonist 8-OH-DPAT to reduce 5-HT release in the striatum using in vivo microdialysis. 8-OH-DPAT reduced the release of 5-HT in the striatum. Chronic treatment with 8-OH-DPAT (1.0 mg/kg s.c.) for 7 days, but not 1 day, att...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(92)90110-b
更新日期:1992-10-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(98)00153-1
更新日期:1998-12-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(89)90112-3
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(97)00045-2
更新日期:1997-04-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2014.01.044
更新日期:2014-06-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2018.10.020
更新日期:2019-01-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/s0028-3908(99)00089-1
更新日期:2000-01-04 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(87)90247-4
更新日期:1987-08-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/0028-3908(95)00180-8
更新日期:1996-02-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2017.04.010
更新日期:2017-09-01 00:00:00
abstract::Zatosetron (13 mg or 0.19 mg/kg), a potent and selective 5-HT3 receptor antagonist was studied with a 30 min infusion in a crossover double-blind placebo-controlled trial for acute migraine therapy. Groups receiving zatosetron and placebo were demographically similar and zatosetron was well-tolerated in all patients w...
journal_title:Neuropharmacology
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1016/0028-3908(94)90082-5
更新日期:1994-03-01 00:00:00
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journal_title:Neuropharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.neuropharm.2018.10.002
更新日期:2018-12-01 00:00:00
abstract::Intrathecal (IT) injection of neostigmine (a cholinesterase inhibitor) has been reported to produce a significant anti-nociceptive effect in a number of inflammatory pain models. However, a potential anti-inflammatory effect of IT neostigmine in these models has not been investigated. In the present study, we have exa...
journal_title:Neuropharmacology
pub_type: 杂志文章
doi:10.1016/j.neuropharm.2004.12.024
更新日期:2005-09-01 00:00:00