3-(1-Piperazinyl)-4, 5-dihydro-1H-benzo [g] indazoles: high affinity ligands for the human dopamine D 4 receptor with improved selectivity over ion channels

…, M Rowley, WB Davey, F Emms, R Marwood…

文献索引：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 Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 6 p. 743 - 753

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被引用次数: 22

摘要

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 ...