选择性多巴胺D3受体配体(+)-UH232是一种部分激动剂。
The preferential dopamine D3 receptor ligand, (+)-UH232, is a partial agonist.
作者信息
Griffon N, Pilon C, Schwartz J C, Sokoloff P
机构信息
Unité de Neurobiologie et Pharmacologie de l'INSERM, Centre Paul Broca, Paris, France.
出版信息
Eur J Pharmacol. 1995 Aug 25;282(1-3):R3-4. doi: 10.1016/0014-2999(95)00460-3.
In a NG 108 15 hybrid cell line stably expressing a recombinant dopamine D3 receptor, (+)-UH 232 (cis-(+)-1S,2R)-5-methoxy-1-methyl-2-(di-n- propylamino)tetralin), a partially selective D3 receptor ligand, stimulates mitogenesis, as measured by incorporation of [3H]thymidine, with an EC50 of 7.6 nM and a maximal increase corresponding to 23% of the response elicited by quinpirole, a full agonist. This effect was antagonised by nafadotride, a D3 receptor-selective antagonist. (+)-UH 232 also antagonised quinpirole-induced mitogenesis with a Ki value of 9.4 nM. (+)-UH 232 (1 microM) inhibited by 22% the forskolin-induced accumulation of cAMP, whilst the inhibition by quinpirole (100 nM) was 53%. These results indicate that (+)-UH 232 is a partial agonist at the D3 receptor with an intrinsic activity of 0.2-0.4.
在稳定表达重组多巴胺D3受体的NG 108 15杂交细胞系中，部分选择性D3受体配体(+)-UH 232（顺式-(+)-1S,2R)-5-甲氧基-1-甲基-2-(二正丙基氨基)四氢萘）可刺激有丝分裂，通过[3H]胸腺嘧啶核苷掺入量来测定，其EC50为7.6 nM，最大增加量相当于完全激动剂喹吡罗所引发反应的23%。这种效应可被D3受体选择性拮抗剂萘法唑酮拮抗。(+)-UH 232也能拮抗喹吡罗诱导的有丝分裂，其Ki值为9.4 nM。(+)-UH 232（1 μM）使福斯高林诱导的cAMP积累量抑制了22%，而喹吡罗（100 nM）的抑制率为53%。这些结果表明，(+)-UH 232是D3受体的部分激动剂，内在活性为0.2 - 0.4。
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