Potential atypical antipsychotics: synthesis, binding affinity and SAR of new heterocyclic bioisosteric butyrophenone analogues as multitarget ligands
- 11 October 2011
- journal article
- research article
- Published by Royal Society of Chemistry (RSC) in MedChemComm
- Vol. 2 (12) , 1194-1200
Abstract
A series of 15 heterocyclic butyrophenone analogues was synthesized as potential multi-target ligands. The compounds were assayed for their in vitro human D2 and 5-HT2A receptor affinity, and those compounds exhibiting the highest affinities were evaluated for binding affinity on D1, D3, 5-HT1A, 5-HT2C and 5-HT6 receptors.Keywords
This publication has 40 references indexed in Scilit:
- Discovery of Bishomo(hetero)arylpiperazines as Novel Multifunctional Ligands Targeting Dopamine D3 and Serotonin 5-HT1A and 5-HT2A ReceptorsJournal of Medicinal Chemistry, 2010
- S33138 (N-[4-[2-[(3 aS,9 bR)-8-cyano-1,3 a,4,9 b-tetrahydro[1] benzopyrano[3,4-c]pyrrol-2(3 H)-yl)-ethyl]phenyl-acetamide), a Preferential Dopamine D3 versus D2 Receptor Antagonist and Potential Antipsychotic Agent: III. Actions in Models of Therapeutic Activity and Induction of Side EffectsThe Journal of Pharmacology and Experimental Therapeutics, 2008
- Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychoticsBioorganic & Medicinal Chemistry Letters, 2004
- Selective Antagonism at Dopamine D3 Receptors Enhances Monoaminergic and Cholinergic Neurotransmission in the Rat Anterior Cingulate CortexNeuropsychopharmacology, 2002
- Binding of antipsychotic drugs to human brain receptorsLife Sciences, 2000
- The Role of Serotonin in Antipsychotic Drug ActionNeuropsychopharmacology, 1999
- Rhodium(II)-catalyzed Cycloaddition of Cyclic Diazodicarbonyl Compounds with Nitriles. Synthesis of Tetrahydrobenzoxazoles, Tetrahydrobenzofurans, and TetrahydrobenzodioxolesHETEROCYCLES, 1998
- A Clinical Guide to Antipsychotic DrugsDrugs, 1992
- ClozapineDrugs, 1990
- Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionBiochemical Pharmacology, 1973