We have prepared and studied some new 2-methoxyphenylpiperazine derivatives as combined ligands for 5-hydroxytryptamine 5-HT(1A) and dopamine D3 receptor subtypes. The compounds displayed affinity for 5-HT(1A) and D3 receptors, which improved with the lengthening of the intermediate aliphatic chain. Conversely, binding to 5-HT(2A), D2 and α1-receptor subtypes was affected in an irregular, and mainly negative, manner by the chain length. Benzotriazole derivatives with 4-5 methylenes exhibited good or excellent selectivity for 5-HT(1A) and D3 vs 5-HT(2A), D2 and α1-receptors.

2-{4-[ω-[4-(2-methoxyphenyl)-1-piperazinyl]alkoxy]phenyl}-2H-benzotriazole s and their N-oxides as ligands for some 5-hydroxytryptamine, dopamine and adrenergic receptor subtypes / A. Sparatore, F. Sparatore. - In: PHARMACY AND PHARMACOLOGY COMMUNICATIONS. - ISSN 1460-8081. - 6:9(2000), pp. 421-425.

2-{4-[ω-[4-(2-methoxyphenyl)-1-piperazinyl]alkoxy]phenyl}-2H-benzotriazole s and their N-oxides as ligands for some 5-hydroxytryptamine, 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-hydroxytryptamine 5-HT(1A) and dopamine D3 receptor subtypes. The compounds displayed affinity for 5-HT(1A) and D3 receptors, which improved with the lengthening of the intermediate aliphatic chain. Conversely, binding to 5-HT(2A), D2 and α1-receptor subtypes was affected in an irregular, and mainly negative, manner by the chain length. Benzotriazole derivatives with 4-5 methylenes exhibited good or excellent selectivity for 5-HT(1A) and D3 vs 5-HT(2A), D2 and α1-receptors.
2 [4 [omega [4 (2 methoxyphenyl) 1 piperazinyl]alkoxy]phenyl] 2h benzotriazole; 2 methoxypiperazine derivative; benzotriazole derivative; dopamine 2 receptor; dopamine 3 receptor; haloperidol; ketanserin; ligand; metergoline; piperazine derivative; prazosin; receptor subtype; serotonin 1A receptor; serotonin 2A receptor; spiperone;
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/2434/187562
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