We have prepared and studied some new 2-methoxyphenylpiperazine derivatives as combined ligands for 5-HT1A and D3 receptor subtypes. The introduction of a phenyloxy moiety between the phthalimido group and the polymethylene chain of nanserone does not impair the typical high affinity for 5-HT1A receptors, but reduces in different measures the affinity for 5-HT2, D2 and α1-receptors. Good affinity for the D3-receptor subtype has also been observed. The polymethylene chain length remains a critical factor in determining optimal affinity and selectivity.

2-{4-[ω-[4-(2-methoxyphenyl)-1-piperazinyl] alkoxy] phenyl}phthalimides as ligands for some 5-HT, dopamine and adrenergic receptor subtypes / A. Sparatore, F. Sparatore. - In: PHARMACY AND PHARMACOLOGY COMMUNICATIONS. - ISSN 1460-8081. - 6:12(2000), pp. 559-562.

2-{4-[ω-[4-(2-methoxyphenyl)-1-piperazinyl] alkoxy] phenyl}phthalimides as ligands for some 5-HT, dopamine and adrenergic receptor subtypes

A. Sparatore
Primo
;
2000

Abstract

We have prepared and studied some new 2-methoxyphenylpiperazine derivatives as combined ligands for 5-HT1A and D3 receptor subtypes. The introduction of a phenyloxy moiety between the phthalimido group and the polymethylene chain of nanserone does not impair the typical high affinity for 5-HT1A receptors, but reduces in different measures the affinity for 5-HT2, D2 and α1-receptors. Good affinity for the D3-receptor subtype has also been observed. The polymethylene chain length remains a critical factor in determining optimal affinity and selectivity.
2 { 4 [omega [4 (2 methoxyphenyl) 1 piperazinyl]alkpxy]phenyl} phthalimide; adrenalin; adrenergic receptor; dopamine; dopamine receptor; phthalimide derivative; receptor subtype; serotonin; serotonin 1A receptor;
Settore CHIM/08 - Chimica Farmaceutica
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/187543
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