Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid |
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| Authors: | Thomas C Hübner H Gmeiner P |
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| Affiliation: | 1. Addictions Division, Centre for Addiction and Mental Health, Toronto, Canada;2. Laboratory of Clinical Psychopharmacology, Beijing Key Lab of Mental Disorders, Beijing Anding Hospital, Capital Medical University, Beijing, China;3. Eastern State Hospital, Lexington, Kentucky, USA;4. Apalachee, Inc., Eastside Psychiatric Hospital, Tallahassee, Florida, USA;5. University of Kentucky Mental Health Research Center, Eastern State Hospital, Lexington, Kentucky, USA;6. Psychiatry and Neurosciences Research Group (CTS-549), Institute of Neurosciences, University of Granada, Granada, Spain;7. Biomedical Research Centre in Mental Health Net (CIBERSAM), Santiago Apostol Hospital, University of the Basque Country, Vitoria, Álava, Spain;1. Università degli Studi di Milano, Dipartimento di Chimica, via C. Golgi, 19, 20133 Milano, Italy;2. Sapienza Università di Roma, Dipartimento di Chimica e Tecnologie del Farmaco, piazzale A. Moro, 5, 00185 Roma, Italy;3. Università degli Studi dell’Insubria, Dipartimento di Scienza e Alta Tecnologia, via Valleggio, 11, 22100 Como, Italy |
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| Abstract: | Subreceptor selectivity tuning of N-(3-pyrrolidinyl)benzamides leading to the selective dopamine D3 ligand ent1h and the derivatives 1g and 1e/ent1e which preferably recognize human D2 or D4 receptors, respectively, is described. Binding profiles were controlled by both, absolute and relative configuration. The enantiopure target compounds were synthesized from aspartic acid. |
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