A partially rigid butyrophenone analog with extended conformation

The synthesis and in vitro dopamine D2 receptor binding of a conformationally restricted analog of 4-piperidinobutyrophenone is described. 2-(2-Piperidinoethyl)-1-tetralone displaces [3H]spiperone from the rat striatal dopamine receptor with an IC50 of 1.2 X 10(-4)mol/l.

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Bibliographische Detailangaben
Veröffentlicht in:	Pharmazie 1986-12, Vol.41 (12), p.835-836
Hauptverfasser:	CHAN, C. C, FARMER, P. S
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antipsychotic Agents - chemical synthesis Antipsychotic Agents - pharmacology Binding, Competitive - drug effects Biological and medical sciences Butyrophenones - chemical synthesis Butyrophenones - pharmacology Catecholaminergic system Chemical Phenomena Chemistry, Physical Corpus Striatum - metabolism In Vitro Techniques Magnetic Resonance Spectroscopy Medical sciences Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Receptors, Dopamine - metabolism Spiperone - metabolism Tetralones
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Beschreibung
Zusammenfassung:	The synthesis and in vitro dopamine D2 receptor binding of a conformationally restricted analog of 4-piperidinobutyrophenone is described. 2-(2-Piperidinoethyl)-1-tetralone displaces [3H]spiperone from the rat striatal dopamine receptor with an IC50 of 1.2 X 10(-4)mol/l.
ISSN:	0031-7144