Abstract：
:Cerebrocrast is a novel lipophilic dihydropyridine derivative with potential neuroprotective and antidiabetic properties. We have analyzed its interaction with L-type (CaV1.2b) and T-type (CaV3.1) calcium channels using a whole-cell patch clamp in HEK 293 cells. Cerebrocrast inhibited current flux through both CaV1.2b and CaV3.1 channels. In both cases, the drug was about 10-fold less effective than neutral dihydropyridines, but more efficient than the charged dihydropyridine amlodipine. IC50 values for the CaV1.2b channel were 586 +/- 96 nmol/L and 178 +/- 78 nmol/L at holding potentials of -80 mV and -50 mV, respectively. Approximately 50 micromol/L of cerebrocrast was needed to block 50% of the current amplitude in the CaV3.1 channel, but this inhibition was not facilitated by shifting the holding potential from -100 mV to -70 mV. Cerebrocrast did not alter current kinetics in either investigated channel, and the inhibition of calcium current was partly reversible or irreversible. In conclusion, the interaction of cerebrocrast with CaV3.1 lacked the typical characteristics of a state-dependent interaction, and voltage-dependent inhibition of CaV1.2b was consistent with partial interaction with the inactivated state of the channel.
journal_name
Can J Physiol Pharmacoljournal_title
Canadian journal of physiology and pharmacologyauthors
Drígelová M,Tarabová B,Duburs G,Lacinová Ldoi
10.1139/y09-086subject
Has Abstractpub_date
2009-11-01 00:00:00pages
923-32issue
11eissn
0008-4212issn
1205-7541pii
y09-086journal_volume
87pub_type
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y91-133
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y95-116
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doi：10.1139/cjpp-2016-0442
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y81-179
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y85-102
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y90-068
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/cjpp-77-1-8
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/cjpp-2015-0068
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章,评审
doi：10.1139/y91-101
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：
更新日期：1998-02-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y88-083
更新日期：1988-04-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/cjpp-2016-0194
更新日期：2018-06-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y88-078
更新日期：1988-04-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y86-225
更新日期：1986-10-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y93-086
更新日期：1993-08-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章,评审
doi：10.1139/cjpp-2014-0413
更新日期：2015-03-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/cjpp-2016-0676
更新日期：2018-01-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章,评审
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更新日期：2017-10-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章,评审
doi：10.1139/cjpp-2014-0468
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y91-110
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：
更新日期：1996-11-01 00:00:00
abstract：:Neural and paracrine agents, such as dopamine, epinephrine, and histamine, affect intestinal epithelial function, but it is unclear if these agents act on receptors directly at the enterocyte level. The cellular localization and villus-crypt distribution of adrenergic, dopamine, and histamine receptors within the inte...
journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y05-024
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y86-252
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/cjpp-2013-0318
更新日期：2014-04-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y79-191
更新日期：1979-11-01 00:00:00
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：
更新日期：2001-08-01 00:00:00
abstract：:Hyperglycemia in diabetes induces increased endothelin-1 (ET-1) production in the retina, kidney, and heart that may lead to hemodynamic impairment, permeability alteration, and increased extracellular matrix (ECM) protein production. Chronically elevated blood glucose levels may cause oxidative stress in these target...
journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/Y08-033
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journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章,评审
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abstract：:Norethandrolone (NE) and other androgenic steroids have been shown to be renotropic in various species and have also been reported to have salutary effects in patients with diminished renal function. Renal cortical slices prepared from rats pretreated with NE showed an increased capability to concentrate p-aminohippur...
journal_title：Canadian journal of physiology and pharmacology
pub_type： 杂志文章
doi：10.1139/y75-104
更新日期：1975-10-01 00:00:00
