Aplindore Fumarate - CAS 189681-71-8
Catalog number: 189681-71-8
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Dopamine Receptor
Aplindore Fumarate is a partial agonist selective for the dopamine receptor D2 used in the therapeutic treatment of Parkinson Disease and restless legs syndrome.
Related CAS:
189681-70-7(Aplindore free base); 189681-71-8 (Aplindore Fumarate)
Solid powder
(2S)-2-[(benzylamino)methyl]-2,3,7,9-tetrahydro-[1,4]dioxino[2,3-e]indol-8-one;(E)-but-2-enedioic acid; (S)-2-(benzylamino-methyl)-2,3,8,9-tetrahydro-7H-1,4-dioxino(2,3-e)indol-8-one fumarate; aplindore fumarate; 189681-70-7(Aplindore free base); DAB-452; DAB 452; DAB452
Canonical SMILES:
1.Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist.
Heinrich JN;Brennan J;Lai MH;Sullivan K;Hornby G;Popiolek M;Jiang LX;Pausch MH;Stack G;Marquis KL;Andree TH Eur J Pharmacol. 2006 Dec 15;552(1-3):36-45. Epub 2006 Sep 14.
The pharmacology of aplindore (DAB-452) was characterized in CHO-K1 cells stably transfected with the human dopamine D(2) receptor short isoform (CHO-D(2s)) and in a behavioral model for post-synaptic agonism in rats. In [(3)H]-spiperone competition binding studies, aplindore showed high affinity for dopamine D(2) and D(3) receptors and low affinity for the dopamine D(4), serotonin (5-HT)(1A), 5-HT(2) receptors and the alpha1-adrenoceptor. The high potency partial agonist activity of aplindore was demonstrated in [(35)S]guanosine 5'-O-(3-thiotriphosphate) ([(35)S]GTPgammaS) binding, extracellular signal-regulated kinase (ERK)-phosphorylation and intracellular calcium flux assay using fluorometric plate reader ([Ca(2+)](i)-FLIPR) format. The [Ca(2+)](i)-FLIPR assay was conducted with CHO-D(2S) receptor cells also stably expressing chimeric G(alphaq/o)-proteins. In all assay modalities, the potencies and intrinsic activities of aplindore were lower than dopamine and higher than aripiprazole. In contrast to the [(35)S]GTPgammaS binding and ERK-phosphorylation assays, the [Ca(2+)](i)-FLIPR assay was able to detect the low partial agonist activity of SDZ 208-912. In unilaterally 6-hydroxydopamine (6-OHDA) lesioned rats, aplindore induced contralateral turning, which was blocked by the dopamine D(2) receptor antagonist raclopride.
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