156544-93-3Relevant academic research and scientific papers
3-(1-Piperazinyl)-4,5-dihydro-1H-benzo[g]indazoles: High affinity ligands for the human dopamine D4 receptor with improved selectivity over ion channels
Collins, Ian,Rowley, Michael,Davey, William B.,Emms, Frances,Marwood, Rosemarie,Patel, Shil,Patel, Smita,Fletcher, Alan,Ragan, Ian C.,Leeson, Paul D.,Scott, Ann L.,Broten, Theodore
, p. 743 - 753 (1998)
3-(4-Piperidinyl)-5-arylpyrazoles, such as 1, were selective for the cloned human dopamine D4 receptor (hD4), but also showed affinity at voltage sensitive calcium, sodium and potassium ion channels. A combination of substituent changes to reduce the basicity of the piperidine nitrogen and conformational restriction to give 4,5-dihydro-1H-benzo[g]indazoles reduced this ion channel affinity at the expense of selectivity for hD4 over other dopamine receptors. Incorporation of piperazine into the 4,5-dihydro-1H-benzo[g]indazoles in place of piperidine gave a novel series of high affinity, selective, orally bioavailable hD4 ligands, such as 16, with improved selectivity over ion channels. Copyright (C) 1998 Elsevier Science Ltd.
Dopamine receptor subtype ligands
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, (2008/06/13)
Fused tricyclic heteroaromatic compounds of formula STR1 wherein one of X and Y represents nitrogen, and the other of X and Y represents oxygen, sulphur or N--R 2 ;Q represents a substituted five- or six-membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the sole heteroatom and is linked to the five-membered heteroatomic ring containing the moieties X and Y via a carbon atom: as well as substituted 3,4-dihydro-1-hydroxy-2-oxomethyl-naphthalene precursors thereto, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia.
