PCP receptor and dopamine uptake sites are discriminated by chiral TCP and BTCP derivatives of opposite configuration

Autor:	P Cerruti, E Coderc, Jacques Vignon, Jean-Marc Kamenka, JF Rouayrenc
Rok vydání:	1995
Předmět:	Pharmacology biology Chemistry Stereochemistry Organic Chemistry General Medicine Chemical synthesis chemistry.chemical_compound Dopamine Dopamine receptor Drug Discovery medicine biology.protein Piperidine Enantiomer Selectivity Chirality (chemistry) medicine.drug Dopamine transporter
Zdroj:	European Journal of Medicinal Chemistry. 30:463-470
ISSN:	0223-5234
Popis:	Summary 3-Methylpiperidine derivatives of 1-[1-(2-thienyl)cyclohexyl]piperidine (TCP) and l-[1-(2-benzo[ b ]thiophenyl)cyclohexyl] piperidine (BTCP) were obtained in their racemic and homochiral forms. They have been tested for their affinity for the PCP receptor labeled with [ 3 H]TCP and for the dopamine transporter labeled with [ 3 H]BTCP. The homochiral TCP derivative (+)- R displayed a very high affinity (5.2 nM) and selectivity for the PCP receptor. In contrast, the homochiral BTCP derivative (−)- S therefore of opposite configuration, displayed a very high affinity (3.5 nM) and selectivity for the dopamine transporter.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::8c923b6e82406c3ff8e08e9a3e7cfdf5 https://doi.org/10.1016/0223-5234(96)88257-2 Zobrazit plný text záznamu Full Text from ScienceDirect