FURTHER CHARACTERIZATION OF [H-3] IFENPRODIL BINDING IN RAT-BRAIN
FURTHER CHARACTERIZATION OF [H-3] IFENPRODIL BINDING IN RAT-BRAIN
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DOI：
10.1016/0922-4106(94)90211-9
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发表时间：
1994-01-01
期刊：
影响因子：
--
通讯作者：
LONDON, ED
中科院分区：
文献类型：
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作者：
HASHIMOTO, K;MANTIONE, CR;LONDON, ED
本研究进行了表征[H-3]艾芬地尔结合在大鼠脑。[H-3]艾芬地尔在4 ℃下显示出可饱和的高亲和力结合。以10 μ M艾芬地尔作为竞争剂确定的特异性结合被S受体配体GBR 12909、1，3-二邻甲苯基胍（DTG）和（+）-3-（3-羟基苯基）-N-丙基哌啶（（+）3-PPP）双相抑制。在4 ℃下，3 μ M GBR 12909可抑制约50%的[H-3]艾芬地尔特异性结合，用于掩蔽α受体。在这些条件下，[H-3]艾芬地尔的特异性结合被艾芬地尔、SL 82.0715、聚（L-精氨酸）、聚（L-赖氨酸）、新霉素、钌红、精胺、青蒿素和亚精胺强力抑制。在3 μ M GBR 12909存在下，Zn ~（2+）和Mg ~（2+）在4 ℃下部分抑制[H-3]艾芬地尔的特异性结合。相反，在不存在GBR 12909的情况下，在37 ℃下，[H-3]艾芬地尔的特异性结合被Zn 2+部分抑制，但不被Mg 2+抑制。4 ℃时[~ 3 H]艾芬地尔（包括GBR 12909）结合在大鼠脑内的解剖分布与[~ 3 H]MK-801（地佐环平）结合在大鼠脑内的解剖分布接近（r=0.971，P
The present study was undertaken to characterize [H-3]ifenprodil binding in rat brain. [H-3]ifenprodil showed saturable, high-affinity binding at 4 degrees C. Specific binding, defined with 10 mu M ifenprodil as a competitor, was inhibited biphasically by the s receptor ligands, GBR 12909, 1,3-di-o-tolylguanidine (DTG), and (+)-3-(3-hydroxyphenyl)-N-propylpiperidine ((+)3-PPP). At 4 degrees C, 3 mu M GBR 12909, which inhibited about 50% of specific binding of [H-3]ifenprodil, was used to mask a receptors. Under these conditions, specific binding of [H-3]ifenprodil was inhibited potently by ifenprodil, SL 82.0715, poly(L-arginine), poly(L-lysine), neomycin, ruthenium red, spermine, arcaine and spermidine. In the presence of 3 mu M GBR 12909, Zn2+ and Mg2+ partially inhibited specific binding of [H-3]ifenprodil at 4 degrees C. In contrast, in the absence of GBR 12909, at 37 degrees C specific binding of [H-3]ifenprodil was partially inhibited by Zn2+, but not by Mg2+. The anatomical distribution of [3H]ifenprodil binding at 4 degrees C (GBR 12909 included) in rat brain closely paralleled that of [3H]MK-801 (dizocilpine) binding (r=0.971, P