1992
DOI: 10.1111/j.1528-1157.1992.tb02358.x
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Dihydropyridine Calcium Antagonists in Mice: Blood and Brain Pharmacokinetics and Efficacy Against Pentylenetetrazol Seizures

Abstract: Dihydropyridine calcium antagonists are candidate anticonvulsants, but little is known of their penetration into brain. Nifedipine (NFD) and nimodipine (NMD) pharmacokinetics were compared in mouse blood and brain, and their activity against pentylenetetrazol (PTZ) was assessed. After intraperitoneal (i.p.) injection, both dihydropyridines achieved peak blood and brain concentrations in 5 min. Estimated blood and brain elimination half-lives (t1/2) of NMD (16.7 and 22.4 min) were slightly longer than those of … Show more

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Cited by 48 publications
(44 citation statements)
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“…As no effect on extinction was noted at this concentration, we increased the dose up to 1 mg/kg to reach nifedipine brain concentrations that should be within the range of those reached after i.p. injections (see Materials and Methods) at the beginning of the experiment (Larkin et al 1992). Proper cannula placement was confirmed both histologically and functionally, by applying BayK (70 µg/µL) at the end of the experiment, resulting in dystonic behavior within 1-2 min after injection.…”
Section: Discussionmentioning
confidence: 99%
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“…As no effect on extinction was noted at this concentration, we increased the dose up to 1 mg/kg to reach nifedipine brain concentrations that should be within the range of those reached after i.p. injections (see Materials and Methods) at the beginning of the experiment (Larkin et al 1992). Proper cannula placement was confirmed both histologically and functionally, by applying BayK (70 µg/µL) at the end of the experiment, resulting in dystonic behavior within 1-2 min after injection.…”
Section: Discussionmentioning
confidence: 99%
“…Doses were adjusted to reach CNS concentrations within a range similar to i.p. injections based on previously determined pharmacokinetic parameters (Larkin et al 1992). Figure 5, B, D, and F, illustrates that fear acquisition prior to injection was similar in the two groups, later assigned to vehicle and the drug group.…”
Section: Effect Of Intracerebroventricular (Icv) Nifedipine Adminimentioning
confidence: 98%
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“…Mice were injected subcutaneously 50 min prior to behavioral testing (10 mL/kg). Drug dose and pretreatment time were chosen based on studies conducted in our laboratory (Cain et al 2002;Barad et al 2004) and on previous reports of systemic administration in rodents (Janicki 1988;Larkin 1992). …”
Section: Drugmentioning
confidence: 99%
“…In addition to these, clinical studies have also been performed in epileptic patients to investigate the effects of nifedipine. They have failed to confirm its efficacy in epilepsy, but EEGs suggested a small improvement with higher dose nifedipine (26,27).…”
Section: Yilmaz I Et Al: Nifedipine and Hippocampal Neuron Numbermentioning
confidence: 99%