CARDIAC CHANNELS--TARGETS OF DRUGS THAT AFFECT KINETICS
CARDIAC CHANNELS--TARGETS OF DRUGS THAT AFFECT KINETICS
批准号:
6191525
负责人:
DOROTHY A. HANCK
金额:
$29.69万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
2000
资助国家:
美国
项目状态:
已结题
起止时间:
2000-09-30 至 2004-07-31
中文摘要
描述(逐字摘自研究者摘要):拟定的实验是
目的是确定药物结合位点的结构相似性,
米贝拉地尔的通道类型(唯一高度特异性的T型Ca
目前已知的通道)和苯基烷基胺,
与米贝拉地尔竞争,并且其中一些结构信息是
可用于L型钙通道。将使用三个通道,T型
Ca通道α lH,作为米贝拉地尔的高亲和力靶点和某种程度上
维拉帕米的低亲和力靶点,电压门控Na通道,一个非常低的
对米贝拉地尔的亲和力靶点,但对维拉帕米的中等亲和力靶点,
和HERG,米贝拉地尔和维拉帕米的高亲和力靶。在每个
领域,实验提出了联合收割机定点诱变,
电生理学和分子建模。此外,实验
提出,将建立通道的具体或共同的影响动力学
控制这些药剂作为治疗药物的作用和功效。
英文摘要
DESCRIPTION (Verbatim from Investigator's Abstract): Experiments proposed are
aimed at determining structural similarities of drug binding sites between
channel types for mibefradil (the only highly specific agent for T-type Ca
channels known at the present time) and phenylalkylamines, the drug class that
competes with mibefradil, and for which some structural information is
available for L-type calcium channels. Three channels will be used, the T-type
Ca channel alpha lH, as a high affinity target for mibefradil and a somewhat
lower affinity target of verapamil, the voltage-gated Na channel, a very low
affinity target for mibefradil but a moderate affinity target for verapamil,
and HERG, a high affinity target for both mibefradil and verapamil. In each
area, experiments proposed combine site-directed mutagenesis,
electrophysiology, and molecular modeling. In addition, experiments are
proposed that will establish the channel specific or common effects on kinetics
that control the action and efficacy of these agents as therapeutic drugs.
期刊论文(0)
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会议论文
Drug therapy targeted to the voltage-gated sodium channel
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批准号:7682803
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项目类别:
-
资助金额:$70.48万
-
财政年份:2009
-
负责人:DOROTHY A. HANCK
-
依托单位:
Cardiac Channels: Targets of Drugs that Affect Kinetics
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批准号:7822235
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项目类别:
-
资助金额:$1.91万
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财政年份:2009
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负责人:DOROTHY A. HANCK
-
依托单位:
Drug therapy targeted to the voltage-gated sodium channel
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批准号:7923976
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项目类别:
-
资助金额:$71.15万
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财政年份:2009
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负责人:DOROTHY A. HANCK
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依托单位:
STRUCTURAL BASES OF T-TYPE CALCIUM CHANNEL FUNCTION
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批准号:6648432
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项目类别:
-
资助金额:$32.66万
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财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
CARDIAC CHANNELS--TARGETS OF DRUGS THAT AFFECT KINETICS
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批准号:6651146
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项目类别:
-
资助金额:$29.69万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
CARDIAC CHANNELS--TARGETS OF DRUGS THAT AFFECT KINETICS
-
批准号:6390884
-
项目类别:
-
资助金额:$29.69万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
CARDIAC CHANNELS--TARGETS OF DRUGS THAT AFFECT KINETICS
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批准号:6527645
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项目类别:
-
资助金额:$29.69万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
Cardiac Channels: Targets of Drugs that Affect Kinetics
-
批准号:7356037
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项目类别:
-
资助金额:$34.54万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
STRUCTURAL BASES OF T-TYPE CALCIUM CHANNEL FUNCTION
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批准号:6700442
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项目类别:
-
资助金额:$2.95万
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财政年份:2000
-
负责人:DOROTHY A. HANCK
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依托单位:
Structure-Function of the Cardiac Sodium Channel
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批准号:7392179
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项目类别:
-
资助金额:$36.15万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
Cardiac Channels: Targets of Drugs that Affect Kinetics
-
批准号:7568167
-
项目类别:
-
资助金额:$34.54万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
Cardiac Channels: Targets of Drugs that Affect Kinetics
-
批准号:7208193
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项目类别:
-
资助金额:$34.54万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
Cardiac Channels: Targets of Drugs that Affect Kinetics
-
批准号:7763878
-
项目类别:
-
资助金额:$34.54万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
STRUCTURAL BASES OF T-TYPE CALCIUM CHANNEL FUNCTION
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批准号:6200214
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项目类别:
-
资助金额:$29.71万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
STRUCTURAL BASES OF T-TYPE CALCIUM CHANNEL FUNCTION
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批准号:6390365
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项目类别:
-
资助金额:$29.71万
-
财政年份:2000
-
负责人:DOROTHY A. HANCK
-
依托单位:
STRUCTURAL BASES OF T-TYPE CALCIUM CHANNEL FUNCTION
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批准号:6527422
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项目类别:
-
资助金额:$29.71万
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财政年份:2000
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负责人:DOROTHY A. HANCK
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依托单位:
KINETICS OF CARDIAC SODIUM CHANNEL
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批准号:6109502
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项目类别:
-
资助金额:$29.65万
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财政年份:1999
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负责人:DOROTHY A. HANCK
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依托单位:
KINETICS OF CARDIAC SODIUM CHANNEL
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批准号:6272578
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项目类别:
-
资助金额:$28.83万
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财政年份:1998
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负责人:DOROTHY A. HANCK
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依托单位:
KINETICS OF CARDIAC SODIUM CHANNEL
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批准号:6241625
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项目类别:
-
资助金额:$26.34万
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财政年份:1997
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负责人:DOROTHY A. HANCK
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依托单位:
LENGTH-DEPENDENT PHENOMENA IN CARDIAC MUSCLE
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批准号:3049562
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项目类别:
-
资助金额:$0.04万
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财政年份:1983
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负责人:DOROTHY A. HANCK
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依托单位:
海外基金