MINORITY SCHOOL FACULTY DEVELOPMENT AWARD
MINORITY SCHOOL FACULTY DEVELOPMENT AWARD
批准号:
3088265
负责人:
STANLEY L EVANS
金额:
$5.64万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1985
资助国家:
美国
项目状态:
已结题
起止时间:
1985-12-01 至 1990-11-30
关键词:
antihypertensive agents blood flow measurement blood pressure centrifugation chemical structure function disease /disorder prevention /control dopamine receptor drug design /synthesis /production drug screening /evaluation hypertension laboratory mouse laboratory rat peripheral blood vessel phenylethylamines scintillation counter trace elements ultrasound blood flow measurement
中文摘要
刺激突触前外周多巴胺受体(DA2)产生
交感神经抑制导致低血压。突触后外周
多巴胺受体(DA1)激活亚服务器的血管扩张和利尿作用。
外周高特异性激动剂的设计与合成
多巴胺受体已经进化成一种控制
高血压。N,N-二正丙基多巴胺的外周作用
多巴胺受体导致血压和心脏减少
速度刺激了类似化合物的合成。潜力
这些取代(芳烷基)苯乙胺的临床应用
当前感兴趣的话题。
这项研究项目建议(A)合成和表征一系列
苯乙胺的N-芳烷基衍生物和相关化合物,(B)
评估这些化合物对外周多巴胺的有效性
使用局部血流测量的受体(脉冲多普勒
流量计)和(C)进一步表征外周血中的多巴胺
使用化学探针(即重金属)的受体。综合方案
发展将是这项调查的主要主题。区域血液
流量测量将在清醒和麻醉的动物身上进行。
外周多巴胺受体活性。化学探测法
接收器还将使用区域血流测量技术。这个
拟议的研究具有重要意义,因为它可能提供一系列新的
抗高血压药物和有关外周血细胞的更多信息
多巴胺受体。
英文摘要
Stimulation of presynaptic peripheral dopamine receptors (DA2) produces
sympathoinhibition resulting in hypotension. Postsynaptic peripheral
dopamine receptor (DA1) activation subserver's vasodilation and diuresis.
The design and synthesis of highly specific agonists for peripheral
dopamine receptors have evolved into a new approach for the control of
hypertension. The action of N, N-di-n-propyldopamine on peripheral
dopamine receptors resulting in reduced blood pressure and reduced heart
rate has stimulated the synthesis of similar compounds. The potential
clinical application of these substituted (aralkyl) phenethylamines is a
topic of current interest.
This research project proposes to (a) synthesize and characterize a series
of N-aralkyl derivatives of phenethylamine and related compounds, (b)
evaluate the effectiveness of these compounds on peripheral dopamine
receptors utilizing regional blood flow measurements (pulsed Doppler
flowmeter) in rats and (c) further characterize the peripheral dopamine
receptors using chemical probes (i.e., heavy metals). Synthetic scheme
development will be a major thrust of this investigation. Regional blood
flow measurements will be performed in conscious and anesthetized animals
for peripheral dopamine receptor activity. Chemical probing of the
receptors will also use the regional blood flow measurement technique. The
proposed research is significant because it may provide new series of
antihypertensive agents and additional information about peripheral
dopamine receptors.
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会议论文
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批准号:3088266
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项目类别:
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资助金额:$5.62万
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负责人:STANLEY L EVANS
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依托单位:
MINORITY SCHOOL FACULTY DEVELOPMENT AWARD
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批准号:3088267
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项目类别:
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资助金额:$6.07万
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负责人:STANLEY L EVANS
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依托单位:
MINORITY SCHOOL FACULTY DEVELOPMENT AWARD
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批准号:3088263
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项目类别:
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资助金额:$5.21万
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财政年份:1985
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负责人:STANLEY L EVANS
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依托单位:
MINORITY SCHOOL FACULTY DEVELOPMENT AWARD
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批准号:3088264
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项目类别:
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资助金额:$5.44万
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财政年份:1985
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负责人:STANLEY L EVANS
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依托单位:
海外基金