Pharmacological characterization of the vesamicol analogue (+)-[(125)I]MIBT in primate brain.
Pharmacological characterization of the vesamicol analogue (+)-[(125)I]MIBT in primate brain.
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维萨米考类似物 ( )-[(125)I]MIBT 在灵长类动物脑中的药理学特征。
DOI：
10.1016/s0014-2999(97)81944-9
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发表时间：
1997
影响因子：
5
通讯作者：
Efange,SM
中科院分区：
文献类型：
--
作者：
Staley,JK;Mash,DC;Parsons,SM;Khare,AB;Efange,SM
评价了vesamicol类似物，Meta-[125 I]碘苄基曲唑霉素[（+）-[125 I]MIBT]作为灵长类动物脑中囊泡乙酰胆碱转运蛋白体外标记的探针。在纹状体中，（+）-[125 I]MIBT结合单个高亲和力位点，Kd值为4.4±0.7 nM。一组vesamicol类似物竞争（+）-[125 I]MIBT与纹状体的结合，其药理学特征与先前在电鳐突触囊泡上观察到的囊泡乙酰胆碱转运蛋白效力的等级顺序相似。枕叶皮质中（+）-[125 I]MIBT的高亲和力结合特征为Kd值为4.6±1.1 nM。然而，相同供试化合物抑制（+）-[125 I]MIBT与枕叶皮质结合的效价排序与在纹状体中观察到的不同。结果表明，（+）-[125 I]MIBT是灵长类纹状体囊泡乙酰胆碱转运体的可靠探针，但其在灵长类枕叶皮层的结合更为复杂。
The vesamicol analogue, meta-[125I ]iodobenzyltrozamicol [(+)-[125I ]MIBT] was evaluated as a probe for the in vitro labeling of the vesicular acetylcholine transporter in primate brain. In the striatum, (+)-[125I ]MIBT bound a single high-affinity site with a Kdvalue of 4.4±0.7 nM. Competition for (+)-[125I ]MIBT binding to the striatum by a group of vesamicol analogues displayed a pharmacological profile similar to the rank order of potency previously observed for the vesicular acetylcholine transporter on Torpedo synaptic vesicles. High-affinity binding of (+)-[125I ]MIBT in the occipital cortex was characterized by a Kdvalue of 4.6±1.1 nM. However, the rank order of potency for inhibition of (+)-[125I ]MIBT binding to the occipital cortex by the same test compounds differed from that observed in the striatum. The results suggest that (+)-[125I ]MIBT is a reliable probe of the vesicular acetylcholine transporter in primate striatum, but its binding in primate occipital cortex is more complex.