ABT 925 Fumerate - CAS 220519-07-3
Catalog number: 220519-07-3
Category: Inhibitor
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Dopamine Receptor
A 437203 is a selective dopamine (DA) D3 receptor antagonist suited to evaluate the physiological role(s) of D3 receptors. A 437203 shows an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors.
Solid powder
(E)-but-2-enedioic acid;2-[3-[4-[2-tert-butyl-6-(trifluoromethyl)pyrimidin-4-yl]piperazin-1-yl]propylsulfanyl]-1H-pyrimidin-6-one; UNII-DMH23OL273; 220519-07-3 (anhydrous); 220519-06-2 (anhydrous free base); ABT-925 anhydrous
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1.Dopamine D₃ receptor antagonism--still a therapeutic option for the treatment of schizophrenia.
Gross G;Wicke K;Drescher KU Naunyn Schmiedebergs Arch Pharmacol. 2013 Feb;386(2):155-66. doi: 10.1007/s00210-012-0806-3. Epub 2012 Nov 6.
The potential of D(3) receptor antagonism to treat positive, negative, and cognitive symptoms of schizophrenia is reviewed on the basis of preclinical results and preliminary clinical data. Dopamine D(3) receptors are expressed in mesencephalic, limbic, and cortical areas relevant to psychotic and cognitive symptoms of schizophrenia. As expected, selective dopamine D(3) receptor antagonists are not effective in antipsychotic animal models, reflecting D(2) receptor antagonism. However, selective D(3) receptor antagonists affect electrical activity of dopamine neurons in the ventral tegmental area similar to atypical antipsychotics, counteract effects produced by NMDA glutamate receptor blockade, and enhance cortical dopamine and acetylcholine in microdialysis. In contrast to dopamine D(2) receptor antagonists, D(3) antagonists positively influence a variety of social and cognitive behaviors in rodents, including tests representing cognitive flexibility and executive function, which are both impaired in schizophrenia patients. Despite considerable affinity for D(3) receptors, the second-generation antipsychotics clozapine, risperidone, and olanzapine when administered to patients with schizophrenia seem not to occupy D(3) receptors sufficiently to derive any conclusion on a D(3)-mediated therapeutic benefit.
2.Blockade of [11C](+)-PHNO binding in human subjects by the dopamine D3 receptor antagonist ABT-925.
Graff-Guerrero A;Redden L;Abi-Saab W;Katz DA;Houle S;Barsoum P;Bhathena A;Palaparthy R;Saltarelli MD;Kapur S Int J Neuropsychopharmacol. 2010 Apr;13(3):273-87. doi: 10.1017/S1461145709990642. Epub 2009 Sep 15.
Dopamine D3 receptors are preferentially localized in the limbic system and midbrain, and thus may be involved in the pathophysiology of neuropsychiatry disorders. [11C](+)-PHNO is the first preferential D3 receptor radioligand in humans, yet there are no blockade studies with a D3 receptor antagonist in humans. This study characterized the blockade of [11C](+)-PHNO binding by ABT-925, a D3 receptor antagonist, in healthy male subjects. Sixteen subjects underwent 2-3 positron emission tomography (PET) scans, at baseline and following one or two doses of ABT-925 ranging from 50 mg to 600 mg. Receptor occupancies were estimated for globus pallidus, substantia nigra, caudate, putamen, and ventral striatum. At the 600-mg dose (n=9), ABT-925 receptor occupancy (mean+/-s.d.) was higher in substantia nigra (75+/-10%) and globus pallidus (64+/-22%) than in ventral striatum (44+/-17%), caudate (40+/-18%) and putamen (38+/-17%) (ANOVA: F4,140=15.02, p<0.001). The fractions of [11C](+)-PHNO binding attributable to D3 receptors in D3 receptor-rich regions were 100% (substantia nigra) and 90% (globus pallidus), and in D2 receptor-rich regions were 55% (caudate) and 53% (putamen). The ED50 of ABT-925 was 4.
3.Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response.
Bhathena A;Wang Y;Kraft JB;Idler KB;Abel SJ;Holley-Shanks RR;Robieson WZ;Spear B;Redden L;Katz DA Transl Psychiatry. 2013 Apr 9;3:e245. doi: 10.1038/tp.2013.22.
ABT-925, a selective dopamine D3 receptor (DRD3) antagonist, was tested in schizophrenia. A DRD3 gene polymorphism results in an S9G amino-acid change that has been associated with lower risk of schizophrenia, higher affinity for dopamine and some antipsychotics, and differential response to some antipsychotics. The effect of S9G genotype on response to ABT-925 was examined. DNA samples (N=117) were collected in a proof-of-concept, double-blind, randomized, placebo-controlled study of ABT-925 (50 or 150 mg QD) in acute exacerbation of schizophrenia. A pre-specified analysis assessed impact of genotype (SS versus SG+GG) on change from baseline to final evaluation for the Positive and Negative Syndrome Scale (PANSS) total score using analysis of covariance with genotype, treatment and genotype-by-treatment interaction as factors, and baseline score as covariate. Significant genotype-by-treatment interaction (P=0.015) was observed for change from baseline to final evaluation for the PANSS total score. Within subgroup analyses showed significant improvement from placebo in the SG+GG group treated with ABT-925 150 mg. More favorable clinical outcomes were observed in patients treated with ABT-925 150 mg who carried the DRD3 G allele than in those who carried the DRD3 SS genotype.
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