Abstract：
:[14C]Guanidinium ion influx into Na+ channel preparations from mouse and rat cerebral cortex (purified synaptosomes, and synaptoneurosomes) was characterized and its properties were compared with those for 22Na+ influx. Tetrodotoxin-sensitive influx of [14C]guanidinium ion was stimulated by aconitine, veratridine, and batrachotoxin with a K0.5 of 7, 5 and 0.3 microM, respectively, the maximal influx being the same with all toxins. Scorpion venom shifted the activation curve of veratridine to the left, but did not increase the maximal influx. The potency of the local anesthetic drugs cocaine and tetracaine in inhibiting [14C]guanidinium ion influx depended upon the concentration of veratridine used to activate the Na+ channels. The mechanism of inhibition was of a competitive nature. Other local anesthetic drugs and cocaine congeners inhibited [14C]guanidinium ion influx with potencies very similar to those for inhibition of 22Na+ influx. The results show that [14C]guanidinium ion influx is a valid model for 22Na+ influx through voltage-dependent Na+ channels although there are some differences between the two influx assays. The guanidinium ion assay offers the convenience of the 14C isotope as compared with the strongly radiating 22Na+ isotope.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Reith MEdoi
10.1016/0922-4106(90)90245-ssubject
Has Abstractpub_date
1990-01-23 00:00:00pages
33-41issue
1eissn
0014-2999issn
1879-0712journal_volume
188pub_type
杂志文章abstract：:Levcromakalim was more potent at relaxing rat small mesenteric arteries with endothelium (EC50, 84+/-10 nM) than denuded vessels (EC50, 779+/-101 nM). The cannabinoid receptor antagonist SR 141716A (N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1H-pyrazole-3-carboxamide hydrochloride; 1 microM...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1997-11-27 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.03.053
更新日期：2011-06-25 00:00:00
abstract：:Renal adrenergic interactions of intravenously and intrarenal arterially administered angiotensin II were studied in the anesthetized rabbit. Systemic arterial blood pressure and left renal blood flow were monitored. Bolus doses of angiotensin II, 50 and 100 ng/kg given intravenously, caused an immediate reduction in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00357-q
更新日期：1995-09-25 00:00:00
abstract：:Propofol is generally used for the induction and maintenance of anesthesia in clinical procedures via activation of γ -aminobutyric acid A (GABAA) receptors. When administered at the clinical dose, propofol use is associated with movement disorders, including dystonia and ataxia, suggesting that propofol administratio...
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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更新日期：1995-12-29 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)01504-5
更新日期：1998-01-26 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)02016-8
更新日期：2003-08-22 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90307-6
更新日期：1975-06-01 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173087
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.06.090
更新日期：2008-09-11 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)02045-9
更新日期：2002-08-23 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90478-7
更新日期：1981-01-29 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90328-2
更新日期：1992-03-03 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00575-6
更新日期：2000-09-22 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90104-2
更新日期：1977-07-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90613-0
更新日期：1994-04-11 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：2006-02-17 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90167-x
更新日期：1983-08-05 00:00:00
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更新日期：1998-05-01 00:00:00
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journal_title：European journal of pharmacology
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更新日期：1993-06-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.06.035
更新日期：2014-10-05 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90145-v
更新日期：1990-01-03 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.04.030
更新日期：2012-06-15 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90125-9
更新日期：1975-02-01 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90569-x
更新日期：1994-01-24 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90216-4
更新日期：1979-12-07 00:00:00
abstract：:The influence of CGS 21680, an adenosine A2A receptor agonist, on striatal glutamate extracellular levels was tested in a microdialysis study in rats. CGS 21680 (10 mu M), infused intrastriatally through the microdialysis probe, greatly enhanced glutamate extracellular levels. These results show that striatal adenosin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00679-6
更新日期：1995-12-12 00:00:00
abstract：:Direct instillation of a recombinant human form of MMP-12 (rhMMP-12) in mice airways elicited an early inflammatory response characterized by neutrophil influx, cytokine release and gelatinase activation followed by a delayed response, mainly characterized by macrophage recruitment. As this experimental model of lung ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.11.070
更新日期：2007-03-15 00:00:00
abstract：:The acute effects of propranolol, 1 mg/kg i.v., were studied in chloralosed, vagotomized cats. The vascularly isolated but innervated calf muscles were perfused from another animal. In one group of experiments, the carotid baroreceptors were exposed to ambient arterial pressure. Here, propranolol caused a fall in hear...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90361-8
更新日期：1978-08-01 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
