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一种利血平样药物对[3H]去甲肾上腺素在细胞体和终末的释放及代谢的影响。

Effect of a reserpine-like agent on the release and metabolism of [3H]NA in cell bodies and terminals.

作者信息

Filinger E J

机构信息

Instituto de Investigaciones Farmacológicas (CONICET), Buenos Aires, Argentina.

出版信息

Gen Pharmacol. 1994 Sep;25(5):1039-43. doi: 10.1016/0306-3623(94)90116-3.

Abstract
  1. The reserpine-like agent, Ro4-1284 (2-hydroxy-2ethyl-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro- 11b-[H] benzo (a)quinolizine) releases [3H]noradrenaline ([3H]NA) from prelabelled superior cervical ganglion (cell bodies) and nictitating membrane (nerve endings) of the cat. 2. The potency of Ro 4-1284 29.0 microM was higher in the cell bodies than in the nerve endings. 3. In both tissues, exposure to the reserpine-like agent Ro 4-1284 induced a selective increase in the spontaneous outflow of [3H]DOPEG, while the [3H]OMDA metabolites to the release induced by Ro 4-1284 was very small. 4. The desamination is the preferential way of the metabolic inactivation of the [3H]NA released by the reserpine-like agent in both parts of the noradrenergic neuron.
摘要
  1. 利血平样药物Ro4-1284(2-羟基-2-乙基-3-异丁基-9,10-二甲氧基-1,2,3,4,6,7-六氢-11b-[H]苯并(a)喹嗪)能从预先标记的猫颈上神经节(细胞体)和瞬膜(神经末梢)释放[3H]去甲肾上腺素([3H]NA)。2. Ro 4-1284在细胞体中的效力(29.0微摩尔)高于神经末梢。3. 在这两种组织中,暴露于利血平样药物Ro 4-1284会导致[3H]多巴胺([3H]DOPEG)的自发流出选择性增加,而Ro 4-1284诱导释放的[3H]去甲氧基多巴胺([3H]OMDA)代谢产物非常少。4. 在去甲肾上腺素能神经元的两个部分,脱氨作用是利血平样药物释放的[3H]NA代谢失活的主要方式。

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