期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 15, 页码 7291-U3出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.06.030
关键词
haloperidol; antipsychotics; butyrophenone; dopamine receptor ligands; serotonin receptor ligands; D2-like receptor ligands; diazepane; atypical antipsychotics
资金
- National Institute of General Medical Studies (NIGMS) [GM 08111]
- NIMH Psychoactive Drug Screening Program
- NCRR [G12 RR 03020]
- Title III Grant to Florida AM University
- Pharmaceutical Research Center [NIH/NCRR 1 C06-RR12512-01]
The synthesis and exploration of novel butyrophenones have led to the identification of a diazepane analogue of haloperidol, 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl) butan-1-one (compound 13) with an interesting multireceptor binding profile. Compound 13 was evaluated for its binding affinities at DA subtype receptors, 5HT subtype receptors, H-1, M-1 receptors and at NET, DAT, and SERT transporters. At each of these receptors, compound 13 was equipotent or better than several of the standards currently in use. In in vivo mouse and rat models to evaluate its efficacy and propensity to elicit catalepsy and hence EPS in humans, compound 13 showed similar efficacy as clozapine and did not produce catalepsy at five times its ED(50) value. Published by Elsevier Ltd.
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