罂粟碱对血管肾上腺素能神经中[3H]腺苷摄取可能具有的选择性抑制作用。

Possible selective inhibition of [3H]adenosine uptake by papaverine in vascular adrenergic nerves.

作者信息

Katsuragi T, Su C

出版信息

Eur J Pharmacol. 1982 Apr 8;79(1-2):111-5. doi: 10.1016/0014-2999(82)90581-7.

Abstract

The effect of the adenosine uptake inhibitors dipyridamole, papaverine and diazepam on the [3H]adenosine uptake was assessed using the rabbit pulmonary arterial segment. [3H]Adenosine uptake into the vascular segment was significantly diminished by dipyridamole (10(-6) -10(-5) M), papaverine (10(-5) -10(-4) M) or diazepam (5 x 10(-5) M) with potencies: dipyridamole greater than papaverine greater than diazepam. Dipyridamole (10(-6) M) or diazepam (5 x 10(-5) M) added 30 min before the incubation with [3H]adenosine reduced the high KCl-induced and epinephrine-induced [3H]purine effluxes equally, whereas papaverine (10(-5) M) selectively diminished the former efflux. KCl and epinephrine have been shown to act preferentially on the neuronal and extraneuronal sites, respectively. These results suggest that papaverine inhibits adenosine uptake into the vascular neuronal compartment, in preference to that into the extraneuronal compartment.

摘要

使用兔肺动脉段评估腺苷摄取抑制剂双嘧达莫、罂粟碱和地西泮对[³H]腺苷摄取的影响。双嘧达莫（10⁻⁶ - 10⁻⁵ M）、罂粟碱（10⁻⁵ - 10⁻⁴ M）或地西泮（5×10⁻⁵ M）可显著减少血管段对[³H]腺苷的摄取，效力为：双嘧达莫＞罂粟碱＞地西泮。在与[³H]腺苷孵育前30分钟加入双嘧达莫（10⁻⁶ M）或地西泮（5×10⁻⁵ M），可同等程度地降低高钾诱导和肾上腺素诱导的[³H]嘌呤流出，而罂粟碱（10⁻⁵ M）则选择性地减少前者的流出。已表明氯化钾和肾上腺素分别优先作用于神经元和非神经元部位。这些结果表明，罂粟碱优先抑制腺苷摄取进入血管神经元区室，而非进入非神经元区室。