A 437203 - CAS 220519-06-2
Catalog number: 220519-06-2
Category: Inhibitor
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Molecular Formula:
C20H27F3N6OS
Molecular Weight:
456.53
COA:
Inquire
Targets:
Dopamine Receptor
Description:
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.
Purity:
>98%
Appearance:
White Solid
Synonyms:
2-[3-[4-[2-tert-butyl-6-(trifluoromethyl)pyrimidin-4-yl]piperazin-1-yl]propylsulfanyl]-1H-pyrimidin-6-one; 2-(3-(4-(2-tert-butyl-6-trifluoromethylpyrimidin-4-yl)piperazin-1-yl)propylsulfanyl)-3H-pyrimidin-4-one fumarate; A 437203; A-437203; 1160247-85-7; 220519-07-3 (anhydrous); 220519-06-2 (anhydrous free base)
MSDS:
Inquire
Melting Point:
202-204°C
InChIKey:
KXVAICSRMHXLJN-UHFFFAOYSA-N
InChI:
1S/C20H27F3N6OS/c1-19(2,3)17-25-14(20(21,22)23)13-15(26-17)29-10-8-28(9-11-29)7-4-12-31-18-24-6-5-16(30)27-18/h5-6,13H,4,7-12H2,1-3H3,(H,24,27,30)
Canonical SMILES:
CC(C)(C)C1=NC(=CC(=N1)N2CCN(CC2)CCCSC3=NC=CC(=O)N3)C(F)(F)F
1.Renoprotective effect of a dopamine D3 receptor antagonist in experimental type II diabetes.
Gross ML;Koch A;Mühlbauer B;Adamczak M;Ziebart H;Drescher K;Gross G;Berger I;Amann KU;Ritz E Lab Invest. 2006 Mar;86(3):262-74.
Diabetic nephropathy is the leading cause of end-stage renal disease. Dopamine receptors are involved in the regulation of renal hemodynamics and may play a role in diabetes-induced hyperfiltration. To test this hypothesis, we investigated the renal effect of a dopamine D3 receptor antagonist (D3-RA) in hypertensive type II diabetic SHR/N-cp rats. Lean and obese SHR/N-cp rats were randomly assigned to D3-RA, angiotensin-converting enzyme inhibitor (ACE-i), or D3-RA+ACE-i treatment or control conditions. Treated animals were given the D3-RA A-437203 (10 mg/kg/body weight (BW)/day) or the ACE-i trandolapril (0.3 mg/kg BW/day) or a combination of both. At 6 months following perfusion, fixed kidneys were analyzed by morphological and stereological methods. Indices of renal damage (glomerulosclerosis, glomerulosclerosis damage index (GSI), tubulointerstitial and vascular damage), glomerular geometry and functional variables such as urinary albumin excretion, glomerular filtration rate, blood pressure, blood chemistry and BW were determined. The GSI (score 0-4) was significantly higher (P<0.05) in untreated diabetic animals (1.62+/-0.3) compared to nondiabetic controls (0.4+/-0.2) and the treatment groups (D3-RA: 0.
2.Pramipexole inhibits MPTP toxicity in mice by dopamine D3 receptor dependent and independent mechanisms.
Ramirez AD;Wong SK;Menniti FS Eur J Pharmacol. 2003 Aug 15;475(1-3):29-35.
The role of dopamine D3 receptors was investigated in mediating the neuroprotective effect of the dopamine D2/D3 receptor agonist (S)-2-amino-4,5,6,7-tetrahydro-6-propylamine-benzothiazole (pramipexole) in vivo. Pramipexole retained the ability to inhibit 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced dopamine depletion in mice in which the dopamine D3 receptor had been deleted. However, the neuroprotective efficacy was reduced in the dopamine D3 receptor-deleted mice compared to that in littermates expressing the wildtype receptor. Furthermore, the dopamine D3 receptor selective antagonist 2-(3-[4-(2-tert-butyl-6-trifluoromethyl-4-pyrimidinyl)-1-piperazinyl]propylthio)-4-pyrimidinol (A-437203) partially inhibited the neuroprotective effect of pramipexole in dopamine D3 receptor expressing mice but not in receptor-deleted mice. These results indicate that pramipexole protects dopamine neurons from MPTP-induced toxicity by mechanisms that are both dependent and independent of an interaction with dopamine D3 receptors.
3.Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test.
Basso AM;Gallagher KB;Bratcher NA;Brioni JD;Moreland RB;Hsieh GC;Drescher K;Fox GB;Decker MW;Rueter LE Neuropsychopharmacology. 2005 Jul;30(7):1257-68.
Dopamine plays a role in the pathophysiology of depression and therapeutic effects of antidepressants but the contribution of individual D(2)-like receptor subtypes (D(2), D(3), D(4)) to depression is not known. We present evidence that activation of D(2)/D(3), but not D(4) receptors, can affect the outcome in the rat forced swim test (FST). Nomifensine, a dopamine uptake inhibitor (7, 14, and 28 micromol/kg); quinpirole, a D(2)-like receptor and agonist (0.4, 1.0, and 2.0 micromol/kg); PD 12,8907, a preferential D(3) receptor agonist (0.17, 0.35, and 0.7 micromol/kg); PD 168077 (0.1, 0.3, and 1.0 micromol/kg) and CP 226269 (0.3, 1.0, and 3.0 micromol/kg), both selective D(4) receptor agonists, were administered s.c. 24, 5, and 0.5/1 h before testing. Nomifensine, quinpirole at all doses and PD 128907 at the highest dose decreased immobility time in FST. PD 168077 and CP 226269 had no effect on the model. To further clarify what type of dopamine receptors were involved in the anti-immobility effect of quinpirole, we tested different antagonists. Haloperidol, a D(2)-like receptor antagonist (0.27 micromol/kg), completely blocked the effect of quinpirole; A-437203 (LU-201640), a selective D(3) receptor antagonist (17.
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