STRIATAL D2 ACETYLCHOLINE INTERACTIONS - PET STUDIES OF THE VESAMICOL RECEPTOR

STRIATAL D2 ACETYLCHOLINE INTERACTIONS - PET STUDIES OF THE VESAMICOL RECEPTOR
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DOI:
10.1097/00001756-199309150-00006
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发表时间:
1993-09-30
期刊:
影响因子:
1.7
通讯作者:
WIDEN, L
WIDEN, L
中科院分区:
医学4区
文献类型:
--
作者:
INGVAR, M;STONEELANDER, S;WIDEN, L

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本文用正电子发射计算机断层扫描(PET)研究了[F-18]NEFA(一种氨基苯甲酰氨基酚)在灵长类动物脑内的局部分布。结合是立体选择性的,可以被阻断,但不能被vesamicol取代。使用[H-3]ABV的体外放射自显影证实了晚期的区域分布模式,纹状体>皮质>小脑,并且与已知的胆碱能神经支配模式一致。用sigma 1或D1拮抗剂预处理不影响纹状体摄取,而D2拮抗剂显著增加了摄取。这与已知的对D2受体阻断的纹状体中乙酰胆碱周转的诱导一致,并证明掺入的[F-18]-(-)-NEFA的量受到靶神经元中胆碱能活性的影响。
THE regional cerebral distribution of [F-18]NEFA, an aminobenzovesamicol (ABV), was studied in primates with PET. The binding was stereoselective and could be blocked but not displaced with vesamicol. The regional distribution pattern at late times, striatum > cortex > cerebellum, was corroborated by in vitro autoradiography using [H-3]ABV and is consistent with known patterns of cholinergic innervation. Pretreatment with sigma1 or D1 antagonists did not affect the striatal uptake, whereas D2 antagonists markedly augmented the uptake. This is consistent with the known induction of acetylcholine turnover in the striatum in response to D2-receptor blockade and demonstrates that the amount of [F-18]-(-)-NEFA incorporated was influenced by the cholinergic activity in the target neurones.