Guanine nucleotide regulation of agonist interactions at [3H]SCH23390-labeled D1 dopamine receptors in rat striatum.
Guanine nucleotide regulation of agonist interactions at [3H]SCH23390-labeled D1 dopamine receptors in rat striatum.
复制标题
鸟嘌呤核苷酸对大鼠纹状体中 [3H]SCH23390 标记的 D1 多巴胺受体激动剂相互作用的调节。
DOI：
10.1016/0014-2999(86)90389-4
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发表时间：
1986
影响因子：
5
通讯作者：
Creese,I
中科院分区：
文献类型：
--
作者：
Hess,EJ;Battaglia,G;Norman,AB;Iorio,LC;Creese,I
We report here the regulation of agonist interactions with [3H]SCH23390-labeled D1dopamine receptors in rat striatum. Scatchard analyses of [3H]SCH23390 saturation data revealed a single high affinity binding site (KD= 0.49 nM) with a Bmaxof 64 pmol/g tissue. The specific binding of 0.25 nM [3H]SCH23390 represented 90% of total binding. Antagonist competition for [3H]SCH23390 binding was monophasic (i.e. pseudo-Hill slope ∼ 1) and the rank order of antagonists' affinities was consistent with the pharmacology of D1dopamine receptors (e.g. cis-flupentixol > haloperidol > spiperone). In contrast, agonist competition curves were shallow (pseudo-Hill slope < 1) and computer-assisted analysis indicated that, for all agonist, the data best fit a two-site model composed of a high (KH) and a low (KL) affinity component. In the presence of 0.3 mM GTP, the high affinity binding component (%RH) of various agonists was reduced by approximately 50%. No significant effect of 0.3 mM GTP on [3H]SCH23390 binding was observed. Additionally, it was noted that [3H]SCH23390 labels S2serotonin receptors in extrastriatal brain regions. However, [3H]SCH23390 apparently does not have an affinity high enough to label S2receptors at the concentration of [3H]SCH23390 employed in labeling striatal D1dopamine receptors. These data indicate that [3H]SCH23390 represents a superior radioligand for labeling the two-state striatal D1dopamine receptor in that its high percent specific binding makes it especially suitable for detailed mechanistic studies of this receptor.
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DOI：
--
发表时间：
1983-08
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
L. Iorio;A. Barnett;F. Leitz;V. Houser;C. Korduba
通讯作者：
L. Iorio;A. Barnett;F. Leitz;V. Houser;C. Korduba
影响因子：
4.7
作者：
BATTAGLIA, G;SHANNON, M;TITELER, M
通讯作者：
TITELER, M
影响因子：
4.1
作者：
L. Limbird
通讯作者：
L. Limbird
SCH 23390 对多巴胺 D-1 受体的选择性阻断公开了介导大鼠体内腺苷酸环化酶抑制的纹状体多巴胺 D-2 受体。
影响因子：
5
作者：
P. Onali;M. Olianas;G. Gessa
通讯作者：
G. Gessa
移动受体假说和激素结合的“协同性”。
DOI：
10.1016/0005-2736(76)90275-3
发表时间：
1976
期刊：
Biochimica et biophysica acta
影响因子：
--
作者：
S. Jacobs;P. Cuatrecasas
通讯作者：
P. Cuatrecasas