19905-07-8Relevant articles and documents
DOPAMINE RECEPTOR LIGANDS
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, (2008/06/13)
Described herein are D4 receptor-selective compounds of the general formula: STR1 wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from CH 2, O, NH, S, C=O, CH--OH, CH--N(C 1-4 alkyl) 2, C=CHCl, C= CHCN, N-C 1-4 alkyl, N-acetyl, SO 2 and SO;X. sub.2--is selected from N=, CH 2--, CH=, C(O)--, O--, and S--;R 1 represents C 1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R 2 is C 1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; andE is a saturated or unsaturated 5-or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C 1-4 alkyl and halogen-substituted C 1-4 alkyl;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
NONCATALEPTIC NEUROLEPTIC AGENTS: 2-(4-(2-(2-CHLORO-10,11-DIHYDRODIBENZOTHIEPIN-10-YLOXY)ETHYL)PIPERAZINE-1-YL)ETHANOL AND SOME RELATED COMPOUNDS
Jilek, Jiri,Valchar, Martin,Holubek, Jiri,Dlohozkova, Natasa,Pomykacek, Josef,et al.
, p. 2731 - 2741 (2007/10/02)
10-(2-Bromoethoxy)-2-chloro-10,11,dihydrodibenzothiepin (X), prepared by two methods, was subjected to substitution reactions with 2-(1-piperazinyl)ethanol, 3-(1-piperazinyl)propanol, 1-methylpiperazine, 3-(1-piperazinyl)propionamide, piperazine, and 1-(ethoxycarbonyl)piperazine and gave the title compounds II-VII.The alcohol II was esterified by treatment with acid chlorides to compounds VIII and IX.Compounds II, V, and VIII proved to be noncataleptic neuroleptic agents and II (clopithepin, VUFB-17 076) was selected for preclinical studies.
