HYPOTHALAMUS AND NARCOTIC EFFECTS
HYPOTHALAMUS AND NARCOTIC EFFECTS
批准号:
3207438
负责人:
HEMENDRA N BHARGAVA
金额:
$13.93万
依托单位国家:
美国
项目类别:
财政年份:
1987
资助国家:
美国
项目状态:
已结题
起止时间:
1987-01-01 至 1989-12-31
关键词:
analgesics benzodiazepines blood chemistry brain metabolism chordate locomotion dopamine receptor dosage drug addiction antagonist drug administration routes drug adverse effect drug metabolism drug tolerance drug withdrawal hormone inhibitor hypophysectomy hypothalamic hormones hypothalamus hypothermia laboratory mouse laboratory rat morphine naloxone narcotics neuropeptide receptor neuropeptides opioid receptor peptide hormone analog radioimmunoassay thyrotropin releasing hormone
中文摘要
潜在长效和口服有效的化合物的类似物的作用
下丘脑肽激素,特别是促黑素释放的肽激素
抑制因子(MIF)和促甲状腺激素释放激素(TRH)对
急性(镇痛、体温过低等)和慢性影响(耐受性和
阿片类药物,特别是吗啡的身体依赖性),将是
在小鼠和大鼠中进行了研究。 耐受和身体依赖
吗啡将通过吗啡丸粒植入程序诱导。
将通过测量反应(例如镇痛剂,
体温过低、僵硬等)不同剂量的吗啡
植入安慰剂颗粒的动物。 身体依赖的程度将
通过确定体温过低,身体
突然和纳洛酮诱导戒断期间的体重减轻等,以及
在纳洛酮诱导期间出现刻板跳跃、湿狗抖动等
戒断 多肽修饰阿片的机制
将通过检查
多巴胺(D1和D2)、阿片(Mu,Delta)
和Kappa)、MIF和TRH。 这将通过3 H-配体的结合来研究
到从整个大脑和大脑区域制备的膜。 此外该
吗啡长期给药对大鼠脑内
脑啡肽(通过放射免疫测定)和
将测定脑啡肽降解酶。 由于我们的研究
实验室首次证明,
阿片受体激动剂抑制3 H-TRH与其受体的结合,
大脑,进一步的研究将进行内源性和
Mu、Delta和Kappa阿片受体的外源性配体,以了解
这些互动。 这些研究可能不仅有助于理解
下丘脑肽在吗啡慢性作用中的作用,但可能
也导致了抑制鸦片成瘾的药物的开发,
治疗阿片类药物引起的痛苦戒断综合征
英文摘要
The effect of potentially long acting and orally effective analogs of
hypothalamic peptide hormones, particularly of melanotropin release
inhibiting factor (MIF) and thyrotropin releasing hormone (TRH) on the
acute (analgesia, hypothermia, etc.) and chronic effects (tolerance and
physical dependence) of opiates, particularly of morphine, will be
investigated in mice and rats. Tolerance to and physical dependence on
morphine will be induced by the morphine pellet implantation procedure.
Tolerance will be assessed by measuring the responses (e.g. analgesic,
hypothermic, cataleptic, etc.) to varying doses of morphine in morphine and
placebo pellet implanted animals. The degree of physical dependence will
be measured by determining the intensity of signs like hypothermia, body
weight loss, etc. during abrupt and naloxone-induced withdrawal and of
stereotyped jumping, wet dog shakes, etc. during naloxone-induced
withdrawal. The mechanism by which the peptides modify opiate
tolerance-dependence process will be investigated by examining the
functions of brain receptors for dopamine (D1 and D2), opiate (Mu, Delta
and Kappa), MIF and TRH. This will be studied by the binding of 3H-ligands
to membranes prepared from whole brain and brain regions. In addition, the
effect of chronic administration of morphine on the concentration of
enkephalins (to be determined by radioimmunoassay) and the activity of
enkephalin degrading enzymes will be determined. Since studies in our
laboratory have demonstrated for the first time that tifluadom, a Kappa
opiate receptor agonist inhibits the binding of 3H-TRH to its receptors in
the brain, further studies will be carried out with endogenous and
exogenous ligands for Mu, Delta, and Kappa opiate receptors to understand
these interactions. These studies may lead not only to understanding of
the role of hypothalamic peptides in the chronic action of morphine but may
also lead to the development of drugs that inhibit opiate addiction and
manage the opiate induced distressing withdrawal syndrome.
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SYNTHESIS AND BIOACTIVITY OF POTENTIAL DELTA ANTAGONISTS
-
批准号:2121671
-
项目类别:
-
资助金额:$12.66万
-
财政年份:1994
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
SYNTHESIS AND BIOACTIVITY OF POTENTIAL DELTA ANTAGONISTS
-
批准号:2121672
-
项目类别:
-
资助金额:$13.16万
-
财政年份:1994
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
SYNTHESIS AND BIOACTIVITY OF POTENTIAL DELTA ANTAGONISTS
-
批准号:2121669
-
项目类别:
-
资助金额:$12.36万
-
财政年份:1994
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
OPIOID ACTIONS AND NEUROPEPTIDES
-
批准号:2115954
-
项目类别:
-
资助金额:$9.95万
-
财政年份:1992
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
OPIOID ACTIONS AND NEUROPEPTIDES
-
批准号:3069502
-
项目类别:
-
资助金额:$9.76万
-
财政年份:1992
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
OPIOID ACTIONS AND NEUROPEPTIDES
-
批准号:2115956
-
项目类别:
-
资助金额:$9.83万
-
财政年份:1992
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
OPIOID ACTIONS AND NEUROPEPTIDES
-
批准号:2115955
-
项目类别:
-
资助金额:$9.86万
-
财政年份:1992
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
OPIOID ACTIONS AND NEUROPEPTIDES
-
批准号:2115952
-
项目类别:
-
资助金额:$8.97万
-
财政年份:1992
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS & NARCOTIC EFFECTS
-
批准号:3207440
-
项目类别:
-
资助金额:$10.53万
-
财政年份:1987
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS & NARCOTIC EFFECTS
-
批准号:3207434
-
项目类别:
-
资助金额:$10.16万
-
财政年份:1987
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS & NARCOTIC EFFECTS
-
批准号:3207441
-
项目类别:
-
资助金额:$10.94万
-
财政年份:1987
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS AND NARCOTIC EFFECTS
-
批准号:3207439
-
项目类别:
-
资助金额:$15.39万
-
财政年份:1987
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS AND NARCOTIC EFFECTS
-
批准号:3207431
-
项目类别:
-
资助金额:$13.45万
-
财政年份:1987
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
HYPOTHALAMUS AND NARCOTIC EFFECTS
-
批准号:3207437
-
项目类别:
-
资助金额:$9.25万
-
财政年份:1980
-
负责人:HEMENDRA N BHARGAVA
-
依托单位:
海外基金