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通过一种与胺在组织中扩散相关的方法所确定的,神经元和非神经元摄取在兔主动脉中3H-(-)去甲肾上腺素失活过程中的作用。

The role of neuronal and extraneuronal uptake in the inactivation of 3H-(--)noradrenaline in the rabbit aorta determined by a method relating with amine diffusion in the tissue.

作者信息

Henseling M

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1983 Nov;324(3):163-8. doi: 10.1007/BF00503889.

Abstract

Apparent coefficients of diffusion for 3H-noradrenaline and 14C-sorbitol were determined in the different layers of the rabbit aorta; uptake1 and uptake2 were inhibited. For 3H-noradrenaline, a value of 6.3 . 10(-7) cm2 . s-1 was obtained in intact aorta and a similar one in intima-media, while that in adventitia was three times higher than in intact aorta. The apparent coefficient was the same for 3H-noradrenaline and 14C-sorbitol in adventitia. However, the values were slightly higher for 3H-noradrenaline than for 14C-sorbitol in intact aorta and in intima-media. Thus, the distribution of sorbitol did not exactly reflect the distribution of noradrenaline in these two preparations, even when both uptake mechanisms were inhibited. When either uptake1 or uptake2 was intact, about 60% of the 3H-noradrenaline (0.12 mumol . 1(-1) was inactivated on its way through the vessel wall (intact aorta). This indicated that each mechanism was equieffective in removing noradrenaline from the extracellular fluid either in the adventitia (uptake1) or intima-media (uptake2). Similarly, when noradrenaline left the extracellular space by diffusion, about the same amount of noradrenaline was inactivated neuronally and extraneuronally. However, under classical incubation conditions, neuronal inactivation of 3H-noradrenaline was three to five times higher than extraneuronal one. This difference reflected the rapid access of noradrenaline to the neurones rather than the capacity of the neuronal and extraneuronal uptake sites to remove the amine from the extracellular fluid in the different layers of the aortic wall.

摘要

测定了3H-去甲肾上腺素和14C-山梨醇在兔主动脉不同层的表观扩散系数;摄取1和摄取2均受到抑制。对于3H-去甲肾上腺素,完整主动脉中的值为6.3×10(-7) cm2·s-1,内膜-中膜中的值与之相似,而外膜中的值比完整主动脉中的高3倍。外膜中3H-去甲肾上腺素和14C-山梨醇的表观系数相同。然而,在完整主动脉和内膜-中膜中,3H-去甲肾上腺素的值略高于14C-山梨醇的值。因此,即使两种摄取机制均受到抑制,山梨醇的分布也不能准确反映去甲肾上腺素在这两种制剂中的分布。当摄取1或摄取2完整时,约60%的3H-去甲肾上腺素(0.12 μmol·L-1)在穿过血管壁(完整主动脉)的过程中失活。这表明每种机制在从外膜(摄取1)或内膜-中膜(摄取2)的细胞外液中去除去甲肾上腺素方面具有同等效力。同样,当去甲肾上腺素通过扩散离开细胞外空间时,神经元内和神经元外失活的去甲肾上腺素量大致相同。然而,在经典孵育条件下,3H-去甲肾上腺素的神经元内失活比神经元外失活高3至5倍。这种差异反映了去甲肾上腺素快速进入神经元,而不是神经元和神经元外摄取位点从主动脉壁不同层的细胞外液中去除胺的能力。

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