Dopamine D3 receptor antagonists

Laszy J, Laszlovszky I, Gyertyan I. Dopamine D3 receptor antagonists improve the learning performance in memory-impaired rats. Psychopharmacology (Berl) 2005 179 567-575. 

Generation of the first tellurium-containing diheteropentalene has been reported <02OL1193>. Treatment of dibromide 131 with tellurium followed by silver trifluoroacetate gave intermediate 132 which upon treatment with base gave telluro[3,4-c]thiophene 133. Finally, benzo[b]tellurophene derivatives were synthesized and evaluated as selective dopamine D3 receptor antagonists <02JMC4594>. 

A series of dopamine D3-receptor antagonists was pre-pared. Changing from the l//-pyrimidin-2-one (X = N) compound (53) to the l//-pyridin-2-one (X = CH) analog (54) increased the logP value 1.1 units and decreased PSA by 13 angstroms, which resulted in greater brain penetration and a B/P ratio of 3.7. 

Geneste, H., Amberg, W., Backfisch, G. et al. Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists variations on the 177-pyrimidin-2-one theme. Bioorg. Med. Chem. Lett. 2006,16, 1934-1937. 

Redden L, Rendenbach-MueUer B, Abi-Saab WM, Katz DA, Goenjian A, Robieson WZ, Wang Y, Goss SL, Greco N 4th, SaltareUi MD (2011) A double-blind, randomized, placebo-controUed study of the dopamine D3 receptor antagonist ABT-925 in patients with acute schizophrenia. 1 CUn Psychopharmacol 31 221-225... 

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