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1
S-(+)-aporphines are not selective for human D3 dopamine receptors.S-(+)-阿朴啡对人D3多巴胺受体没有选择性。
Cell Mol Neurobiol. 1994 Apr;14(2):185-91. doi: 10.1007/BF02090784.
2
Isomeric selectivity at dopamine D3 receptors.多巴胺D3受体的异构体选择性。
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3
Identification of D3 and sigma receptors in the rat striatum and nucleus accumbens using (+/-)-7-hydroxy-N,N-di-n-[3H]propyl-2-aminotetralin and carbetapentane.使用（±）-7-羟基-N，N-二-n-[³H]丙基-2-氨基四氢萘和卡比戊烷鉴定大鼠纹状体和伏隔核中的D3和σ受体。
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4
Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: II. Both D2 and "silent" D3 autoreceptors control synthesis and release in mesolimbic, mesocortical and nigrostriatal pathways.大鼠体内多巴胺D3受体激活的功能相关性及其被选择性拮抗剂（+）-S 14297的调节：II. D2和“沉默”D3自身受体均控制中脑边缘、中脑皮质和黑质纹状体通路中的合成与释放。
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5
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6
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9
Presynaptic inhibition of dopamine synthesis in rat striatal tissue by enantiomeric mono- and dihydroxyaporphines.对映体单羟基和二羟基阿朴啡对大鼠纹状体组织中多巴胺合成的突触前抑制作用。
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Differential pharmacological profile of striatal and cerebellar dopamine receptors labeled by [3H]quinpirole: identification of a discrete population of putative D3 receptors.用[3H]喹吡罗标记的纹状体和小脑多巴胺受体的差异药理学特征：鉴定假定的D3受体的离散群体。
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本文引用的文献

1
Molecular neurobiology of dopaminergic receptors.多巴胺能受体的分子神经生物学
Int Rev Neurobiol. 1993;35:391-415. doi: 10.1016/s0074-7742(08)60573-5.
2
Expression and characterization of the rat D3 dopamine receptor: pharmacologic properties and development of antibodies.大鼠D3多巴胺受体的表达与特性：药理学性质及抗体的研制
J Pharmacol Exp Ther. 1993 Feb;264(2):1002-11.
3
Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines.
J Pharmacol Exp Ther. 1994 Jan;268(1):495-502.
4
Differential visualization of dopamine D2 and D3 receptor sites in rat brain. A comparative study using in situ hybridization histochemistry and ligand binding autoradiography.大鼠脑中多巴胺D2和D3受体位点的差异可视化。一项使用原位杂交组织化学和配体结合放射自显影术的比较研究。
Eur J Neurosci. 1993 Feb 1;5(2):145-53. doi: 10.1111/j.1460-9568.1993.tb00480.x.
5
Hexahydrobenzo[a]phenanthridines: novel dopamine D3 receptor ligands.
Eur J Pharmacol. 1993 Aug 3;239(1-3):271-3. doi: 10.1016/0014-2999(93)91012-c.
6
Isomeric selectivity at dopamine D3 receptors.多巴胺D3受体的异构体选择性。
Eur J Pharmacol. 1993 Aug 3;239(1-3):269-70. doi: 10.1016/0014-2999(93)91011-b.
7
Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors.抗精神病药物与人多巴胺D2A、D2B和D3受体相互作用的独特结合特性。
Mol Pharmacol. 1993 May;43(5):749-54.
8
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.（R,S）-2'-反式-7-羟基-2-[N-正丙基-N-（3'-碘-2'-丙烯基）-氨基]四氢萘（反式-7-OH-PIPAT）的合成：一种新型D3多巴胺受体配体。
J Med Chem. 1993 May 14;36(10):1499-500. doi: 10.1021/jm00062a025.
9
Dopamine D4 receptors bind inactive (+)-aporphines, suggesting neuroleptic role. Sulpiride not stereoselective.多巴胺D4受体与无活性的（+）-阿朴啡结合，提示其具有抗精神病作用。舒必利无立体选择性。
Eur J Pharmacol. 1993 Mar 16;233(1):173-4. doi: 10.1016/0014-2999(93)90365-o.
10
Altered spontaneous behavior and sensitivity to apomorphine in rats following pretreatment with S(+)-aporphines or fluphenazine.用S(+)-阿朴啡或氟奋乃静预处理后大鼠的自发行为改变及对阿扑吗啡的敏感性
Psychopharmacology (Berl). 1993;111(3):351-8. doi: 10.1007/BF02244952.

S-(+)-阿朴啡对人D3多巴胺受体没有选择性。

S-(+)-aporphines are not selective for human D3 dopamine receptors.

作者信息

Kula N S, Baldessarini R J, Kebabian J W, Neumeyer J L

机构信息

Mailman Research Center, McLean Division-Massachusetts General Hospital, Belmont 02178.

出版信息

Cell Mol Neurobiol. 1994 Apr;14(2):185-91. doi: 10.1007/BF02090784.

DOI:10.1007/BF02090784
PMID:7842476
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11566802/
Abstract
  1. Our aim was to test the hypothesis that selectivity for D3 dopamine (DA) receptors may contribute to limbic anti-DA selectivity of S-(+)-aporphine DA partial agonists. 2. Affinity was tested with 3H-emonapride, using human D3 receptors in mouse fibroblasts and D2 receptors in rat striatal tissue. 3. D3 receptors showed a picomolar affinity for 3H-emonapride, Na+ dependence, and reversible saturability, as well as stereoselectivity. Confirmatory or novel D3/D2 pharmacologic selectivity was found with several benzamides, thioxanthenes, buspirone, GBR-12909, and DA agonists including hydroxyaminotetralins [ADTN, (+)-7-OH-DPAT, (-)-PPHT and its fluorescein derivative], (-)-N-propylnorapomorphine, (-)-3-PPP, (-)-quinpirole, and SDZ-205-502, but neither aminoergoline nor (+)-aporphine partial agonists. 4. The results extend pharmacologic characterization of D3-transfected cell membranes but fail to account for the high limbic anti-DA selectivity of S-(+)-aporphines.
摘要
  1. 我们的目的是检验以下假设：对D3多巴胺（DA）受体的选择性可能有助于S-(+)-阿朴啡DA部分激动剂的边缘抗DA选择性。2. 使用小鼠成纤维细胞中的人D3受体和大鼠纹状体组织中的D2受体，用3H-依莫必利测试亲和力。3. D3受体对3H-依莫必利表现出皮摩尔亲和力、钠依赖性、可逆饱和性以及立体选择性。在几种苯甲酰胺、硫杂蒽类、丁螺环酮、GBR-12909和DA激动剂（包括羟基氨基四氢萘[ADTN、(+)-7-OH-DPAT、(-)-PPHT及其荧光素衍生物]、(-)-N-丙基去甲阿朴吗啡、(-)-3-PPP、(-)-喹吡罗和SDZ-205-502）中发现了确证性或新型的D3/D2药理选择性，但在氨基麦角林或(+)-阿朴啡部分激动剂中未发现。4. 这些结果扩展了D3转染细胞膜的药理学特征，但未能解释S-(+)-阿朴啡的高边缘抗DA选择性。