当前位置： SCI文献检索 > LIFE SCIENCES期刊下所有文献 > Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker.

Mechanism underlying the block of human Cav3.2 T-type Ca2+ channels by benidipine, a dihydropyridine Ca2+ channel blocker.

Abstract：

AIMS:Benidipine, a dihydropyridine Ca(2+) channel blocker, has been reported to block T-type Ca(2+) channels; however, the mechanism underlying this effect was unclear. In this study, we characterized the mechanism responsible for this blocking activity. Furthermore, the blocking activity was compared between two enantiomers of benidipine, (S, S)- and (R, R)-benidipine. MAIN METHODS:Human Ca(v)3.2 (hCa(v)3.2) T-type Ca(2+) channels stably expressed in the human embryonic kidney cell line, HEK-293, were studied in whole-cell patch-clamp recordings and Ca(2+) mobilization assay. KEY FINDINGS:In whole-cell patch-clamp recordings, benidipine blocked hCa(v)3.2 T-type Ca(2+) currents elicited by depolarization to a comparable extent as efonidipine. The block was dependent on stimulation frequency and holding potential, but not test potential. Benidipine significantly shifted the steady-state inactivation curve to the hyperpolarizing direction, but had no effect on the activation curve. Benidipine prolonged the recovery from inactivation of hCa(v)3.2 T-type Ca(2+) channels without any effect on the kinetics of activation, inactivation, or deactivation. In the Ca(2+) mobilization assay, benidipine was more potent than efonidipine in blocking Ca(2+) influx through hCa(v)3.2 T-type Ca(2+) channels. (S, S)-Benidipine was more potent than (R, R)-benidipine in blocking hCa(v)3.2 T-type Ca(2+) currents, but there was no difference in blocking the Ca(2+) influx. SIGNIFICANCE:We have characterized the blocking activity of benidipine against hCa(v)3.2 Ca(2+) channels and revealed the difference between the two enantiomers of benidipine. The blocking action of benidipine could be mediated by stabilizing hCa(v)3.2 Ca(2+) channels in an inactivated state.

journal_name

Life Sci

journal_title

Life sciences

authors

Inayoshi A,Sugimoto Y,Funahashi J,Takahashi S,Matsubara M,Kusaka H

doi

10.1016/j.lfs.2011.03.019

subject

Has Abstract

pub_date

2011-05-09 00:00:00

pages

898-907

issue

19-20

eissn

0024-3205

issn

1879-0631

pii

S0024-3205(11)00156-1

journal_volume

88

pub_type

杂志文章

相关文献

LIFE SCIENCES文献大全
  • Radioenzymatic analysis of neurotransmitters.

    abstract：:Since the late 1960's, radioenzymatic assays have gradually come to replace the less sensitive and less specific spectrofluorometric and bioassay procedures previously used to determine many of the neurotransmitters. These assays provide the means to measure picogram quantities of most of these substances, and have en...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(87)90185-8

    authors： Philips SR

    更新日期：1987-08-17 00:00:00

  • Dysregulated ion channels and transporters activate endoplasmic reticulum stress in rat kidney of fetal growth restriction.

    abstract：AIMS:The mechanisms underlying the fetal origin of renal disease remains unknown. This study aimed to investigate the profiles of ion channel and transporter proteins in the fetal kidney in fetal growth restriction (FGR)rats, and to explore their association with the fetal origin of renal disease. MAIN METHODS:An FGR ...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2020.118276

    authors： Guo Y,Lu Y,Wang J,Zhu L,Liu X

    更新日期：2020-10-15 00:00:00

  • Vitamin D levels in multiple sclerosis patients: Association with TGF-β2, TGF-βRI, and TGF-βRII expression.

    abstract：AIM:A variety of evidence suggests that vitamin D can prevent the development of multiple sclerosis (MS). TGF-β pathway genes also play important roles in MS. Here, we aim to study whether vitamin D affects TGF-β pathway gene expression and Expanded Disability Status Scale (EDSS) scores in MS patients. MAIN METHODS:A ...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2015.05.017

    authors： Shirvani-Farsani Z,Behmanesh M,Mohammadi SM,Naser Moghadasi A

    更新日期：2015-08-01 00:00:00

  • Modification of the effects of 7-OH-DPAT, a dopamine D3-receptor agonist, on morphine-induced hyperlocomotion by diabetes.

    abstract：:We examined the effect of 7-OH-DPAT on spontaneous locomotor activity that is enhanced in diabetic mice. 7-OH-DPAT (0.1-30 mg/kg, s.c.) dose-dependently decreased the enhanced spontaneous locomotor activity in diabetic mice, but not in nondiabetic mice. When mice were pretreated with of 7-OH-DPAT (0.1 mg/kg), morphine...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(96)00363-3

    authors： Kamei J,Saitoh A

    更新日期：1996-01-01 00:00:00

  • HOTAIRM1 suppresses cell proliferation and invasion in ovarian cancer through facilitating ARHGAP24 expression by sponging miR-106a-5p.

    abstract：AIMS:Ovarian cancer (OC) is the most lethal gynecologic malignant tumors all over the world. HOX antisense intergenic RNA myeloid 1 (HOTAIRM1) has been reported as an important regulator in multiple tumors. However, the functions of HOTAIRM1 in OC and its possible molecular mechanisms remain unclear. MAIN METHODS:qRT-...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2020.117296

    authors： Chao H,Zhang M,Hou H,Zhang Z,Li N

    更新日期：2020-02-15 00:00:00

  • Calcium-activated and voltage-dependent potassium conductances in clonal pituitary cells.

    abstract：:Voltage clamp recordings of GH3/B6 pituitary cells reveal the presence of non linear steady state membrane properties at the level of the resting potential (about -41 mV). Clamping the cells to potentials more depolarized than -60 mV is associated with a potential dependent increase in membrane conductance and membran...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(82)90475-1

    authors： Dufy B,Barker JL

    更新日期：1982-05-31 00:00:00

  • Neurotoxic esterase: gel filtration and isoelectric focusing of carboxylesterases solubilized from hen brain.

    abstract：:Carboxylesterase activity (EC 3.1.1.1) of hen brain including neurotoxic esterases NTEA and NTEB is solubilized from lyophilized lipid-extracted brain material by the use of n-octylglucoside. The solubilized enzymes are subjected to free isoelectric focusing, six carboxyl - esterase activity peaks are obtained. By gel...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(84)90082-1

    authors： Chemnitius JM,Haselmeyer KH,Zech R

    更新日期：1984-03-19 00:00:00

  • Sorbitol accumulation in heart: implication for diabetic cardiomyopathy.

    abstract：:Sorbitol levels in heart were determined in streptozotocin-induced diabetic rats. Significantly higher levels were found in hearts of diabetic rats compared to normal rats. The findings are compatible with either significantly higher de novo synthesis of sorbitol in heart than is generally believed or uptake of circul...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(89)90016-7

    authors： Nakada T,Kwee IL

    更新日期：1989-01-01 00:00:00

  • Aggregation of human blood platelets in the presence of the pyridoindole stobadine.

    abstract：:The antiarrhythmic and cardioprotective drug stobadine, possessing antioxidant and neuroprotective properties, was studied as to its in vitro effect on aggregation of human blood platelets. Pretreatment of platelets with stobadine for 30 s inhibited stimulated platelet aggregation in a dose-dependent way. Depending on...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(99)00460-9

    authors： Jancinová V,Nosál R,Danihelová E

    更新日期：1999-01-01 00:00:00

  • Effects of aortic coarctation on aortic antioxidant enzymes and NADPH oxidase protein expression.

    abstract：:Abdominal aortic coarctation above the renal arteries leads to severe hypertension above the stenotic site and provides a model for simultaneous testing of the effects of increased and decreased pressure and consequently shear stress in the same animal. The effects of increased pressure, per se, on oxidative stress an...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2004.10.014

    authors： Sindhu RK,Roberts CK,Ehdaie A,Zhan CD,Vaziri ND

    更新日期：2005-01-07 00:00:00

  • NMDA receptor antagonists enhance 5-HT2 receptor-mediated behavior, head-twitch response, in mice.

    abstract：:The purpose of this study was to characterize behavioral interactions between glutamatergic and serotonergic 5-HT2 receptors. Both competitive (AP-5 [D-2-amino-5-phosphovalerate] and D-CPP [3-(2carboxypiperazine-4yl)-propylphosphonate]) and noncompetitive (MK-801 [dizocilpine], ketamine, dextrorphan and dextromethorph...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(98)00519-0

    authors： Kim HS,Park IS,Park WK

    更新日期：1998-01-01 00:00:00

  • miR424-5p functions as an anti-oncogene in cervical cancer cell growth by targeting KDM5B via the Notch signaling pathway.

    abstract：AIMS:Aberrant expression of miRNAs exert the critical roles in carcinogenesis, including cervical cancer. Recent study corroborated the down-regulation of miR424-5p in uterine cervix adenocarcinoma. This research aimed to investigate the function and underlying mechanisms of miR424-5p in cervical cancer cell growth. M...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2017.01.006

    authors： Zhou Y,An Q,Guo RX,Qiao YH,Li LX,Zhang XY,Zhao XL

    更新日期：2017-02-15 00:00:00

  • Ionizing radiation induces opioid-mediated analgesia in male mice.

    abstract：:The effects of exposure to ionizing radiation on the nociceptive thresholds of CF-1 mice were examined. Significant increases in thermal response latencies, indicative of analgesia were observed after exposure to either high or low doses of radiation. However, the onset of analgesia occurred significantly more rapidly...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(84)90352-7

    authors： Teskey GC,Kavaliers M

    更新日期：1984-10-08 00:00:00

  • Protective role of AGK2 on thioacetamide-induced acute liver failure in mice.

    abstract：AIMS:The aim of the present study was to investigate the protective effects of AGK2 as a selective SIRT2 inhibitor on thioacetamide (TAA)-induced acute liver failure (ALF) in mice and its potential mechanism. MAIN METHODS:All male C57BL/6 mice were separated into control, TAA, AGK2 + TAA, and AGK2 groups. The histolog...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2019.05.061

    authors： Jiao FZ,Wang Y,Zhang WB,Zhang HY,Chen Q,Shi CX,Wang LW,Gong ZJ

    更新日期：2019-08-01 00:00:00

  • Endothelin-1 and -2: two amino acids matter.

    abstract：AIMS:Endothelin-1 (ET-1) and endothelin-2 (ET-2; Trp(6)Leu(7)ET-1) are expressed by different cell types, but are considered to display identical pharmacological properties on endothelin receptors. We studied agonist-dependent aspects of endothelin(A) (ET(A))-receptor function and the importance of amino acids 6 and 7 ...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2012.02.011

    authors： Compeer MG,Suylen DP,Hackeng TM,De Mey JG

    更新日期：2012-10-15 00:00:00

  • Aging and sex influence the permeability of the blood-brain barrier in the rat.

    abstract：:The aim of the present study was to investigate the existence of aging- and sex-related alterations in the permeability of the blood-brain barrier (BBB) in the rat, by calculating a unidirectional blood-to-brain transfer constant (Ki) for the circulating tracer [14C]-alpha-aminoisobutyric acid. We observed that: a) th...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(90)90157-m

    authors： Saija A,Princi P,D'Amico N,De Pasquale R,Costa G

    更新日期：1990-01-01 00:00:00

  • Distribution of parathyroid hormone-sensitive adenylate cyclase in isolated rabbit renal cortex microvessels and glomeruli.

    abstract：:The effect of the synthetic amino-terminal fragment of bovine parathyroid hormone, bPTH-(1-34), on the adenylate cyclase of microvessels and glomeruli isolated from rabbit kidney cortex was studied in the presence and absence of guanosine triphosphate (GTP). bPTH-(1-34) stimulated the vascular and glomerular adenylate...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(84)90034-1

    authors： Helwig JJ,Schleiffer R,Judes C,Gairard A

    更新日期：1984-12-24 00:00:00

  • Sexual activity decreases oxytocin receptor densities in the thymus.

    abstract：:Sexual interactions have multiple effects on oxytocin systems in the brain. In the present study we observed that allowing estrogen-progesterone treated ovariectomized rats to be mounted ten times by a male significantly decreased the density (beta max) of thymic oxytocin receptors. Animals were ovariectomized and aft...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(93)90467-h

    authors： Caldwell JD,Walker CH,Pedersen CA,Mason GA

    更新日期：1993-01-01 00:00:00

  • Gossypol ameliorates liver fibrosis in diabetic rats induced by high-fat diet and streptozocin.

    abstract：:11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitors have been shown to treat type 2 diabetes (T2D). Since gossypol is an 11β-HSD1 inhibitor, the objective of the present study was to treat T2D and T2D-related liver fibrosis in rat model using low-dose gossypol. T2D was induced by feeding with high fat diet plus i...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2016.02.044

    authors： Chen G,Wang R,Chen H,Wu L,Ge RS,Wang Y

    更新日期：2016-03-15 00:00:00

  • Analgesic action of nicotine on tibial nerve transection (TNT)-induced mechanical allodynia through enhancement of the glycinergic inhibitory system in spinal cord.

    abstract：:The activation of cholinergic pathways by nicotine elicits various physiological and pharmacological effects in mammals. For example, the stimulation of nicotinic acetylcholine receptors (nAChRs) leads to an antinociceptive effect. However, it remains to be elucidated which subtypes of nAChR are involved in the antino...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2006.08.011

    authors： Abdin MJ,Morioka N,Morita K,Kitayama T,Kitayama S,Nakashima T,Dohi T

    更新日期：2006-12-03 00:00:00

  • Alteration of Mrp2 and P-gp expression, including expression in remote organs, after intestinal ischemia-reperfusion.

    abstract：:The present study was carried out in order to identify the changes in expression of multidrug resistance-associated protein (Mrp) 2 and P-glycoprotein (P-gp) in the intestine and remote organs after intestinal ischemia-reperfusion (I/R). Mrp2 expression in the jejunum and liver was decreased at 6 h after I/R. This dec...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2008.04.019

    authors： Ogura J,Kobayashi M,Itagaki S,Hirano T,Iseki K

    更新日期：2008-06-20 00:00:00

  • Effects of catechins on vascular tone in rat thoracic aorta with endothelium.

    abstract：:The effects of eight catechin derivatives on vascular tone in rat thoracic aorta were examined. Catechin derivatives (10 microM) potentiated the contractile response to phenylephrine in endothelium-intact arteries. The potentiations produced by EGCg and EGC were almost absent in endothelium-denuded arteries and abolis...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(02)02080-5

    authors： Sanae F,Miyaichi Y,Kizu H,Hayashi H

    更新日期：2002-10-11 00:00:00

  • Cross tolerance between morphine and beta-endorphin in the in vivo vasodilating effect in the hamster cheek pouch.

    abstract：:The relative potencies of the in vivo vasodilating effect on the arterioles of the hamster cheek pouch of morphine and beta-endorphin decreased significantly after chronic morphine injection, indicating the existence of tolerance to morphine and cross tolerance between morphine and beta-endorphin. The apparent pA2 val...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(83)90140-6

    authors： Koo A,Wong TM

    更新日期：1983-01-31 00:00:00

  • Effects of diazepam and cyclohexyladenosine on open-field behavior in rats perinatally exposed to caffeine.

    abstract：:Adult rat offspring earlier exposed to maternally ingested caffeine during both gestation and lactation were observed in an open field following acute administration of diazepam or cyclohexyladenosine. While both drugs reduced measures of locomotion and emotional reactivity, caffeine-exposed rats showed evidence of gr...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(96)80009-9

    authors： Fisher CE,Hughes RN

    更新日期：1996-01-01 00:00:00

  • Tissue uptake of ketamine and norketamine enantiomers in the rat: indirect evidence for extrahepatic metabolic inversion.

    abstract：:Ketamine, used clinically as an intravenous analgetic and dissociative anaesthetic agent, is a racemate with both pharmacokinetic and pharmacodynamic enantioselectivity. S-ketamine has been found have a higher clearance and greater potency than R-ketamine as well as a greater therapeutic index. We performed a study in...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(01)01287-5

    authors： Edwards SR,Mather LE

    更新日期：2001-09-14 00:00:00

  • Estrogen dependence of the renal vasodilatory effect of nicotine in rats: role of α7 nicotinic cholinergic receptor/eNOS signaling.

    abstract：AIMS:We recently reported that acute exposure to nicotine vasodilates the renal vasculature of male rats via facilitation of endothelial nitric oxide synthase (eNOS). In this study, we investigated whether this effect of nicotine is sexually dimorphic and the role of estrogen in modulating the nicotine effect. MAIN ME...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/j.lfs.2010.11.009

    authors： el-Mas MM,el-Gowilly SM,Gohar EY,Ghazal AR,Abdel-Rahman AA

    更新日期：2011-01-17 00:00:00

  • Effect of opioid peptides and potassium on the release of vasoactive intestinal polypeptide and thyrotropin releasing hormone from perifused rat hypothalami.

    abstract：:Opioid peptides have been demonstrated to stimulate prolactin secretion, and it has been postulated that this is mediated, at least in part, by an effect on hypothalamic prolactin releasing and release-inhibiting factors and neurotransmitters. The aim of this study was to investigate the effect of opioid peptides and ...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(87)90314-6

    authors： Burns G,Baker DJ,Brown BL,Dobson PR

    更新日期：1987-03-09 00:00:00

  • Involvement of Na+ and Ca2+ channel activation and resultant nitric oxide synthesis in glutamate-mediated hypoxic injury in rat cerebrocortical slices.

    abstract：:The role of Na+ and Ca2+ channels in glutamate-mediated hypoxic injury was investigated in slices of the rat cerebral cortex. Hypoxic injury was determined by mitochondrial reduction of 3-(4,5-dimethyl-2-thiazol)-2,5-diphenyltetrazolium bromide after exposure of brain slices to 30-min of hypoxia/glucose deprivation fo...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/s0024-3205(00)00814-6

    authors： Oka M,Itoh Y,Ukai Y

    更新日期：2000-09-29 00:00:00

  • The role of oxygen free radicals in the development of chronic renal failure.

    abstract：:This study examined whether there is increased production of oxygen free radicals during chronic renal failure. Rats subjected to 3/4 nephrectomy and sham operated controls were killed after 3 weeks. Lipid extracts of plasma and renal tissue were examined by HPLC and kidney specimens were also analyzed by EPR spectros...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(92)90548-4

    authors： Trachtman H,Wilson D,Rao PS

    更新日期：1992-01-01 00:00:00

  • FSH bioactivity is strongly enhanced by kinetic incubation of pre-antral hamster follicles.

    abstract：UNLABELLED:Isolation of meiotic arrested oocytes from mammalian ovaries involves a resumption of the meiosis. Studying the effect of FSH on this process it was found that doses up to of 0.1 IU/ml did not maintain the meiotic arrest in hamster oocytes in pre-antral follicles during static incubation conditions. However,...

    journal_title：Life sciences

    pub_type： 杂志文章

    doi：10.1016/0024-3205(94)90045-0

    authors： Goverde HJ,van de Venne WP

    更新日期：1994-01-01 00:00:00