Molecules 2004-01-01

New imide 5-HT1A receptor ligands - modification of terminal fragment geometry.

Andrzej J Bojarski, Maria J Mokrosz, Beata Duszyńska, Aneta Kozioł, Ryszard Bugno

Index: Molecules 9(3) , 170-7, (2004)

Full Text: HTML

Abstract

Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the serotonin 5-HT(1A) and 5-HT(2A) receptors. All new derivatives from series a demonstrated high 5-HT(1A) affinities, whereas THIQ analogues were much less active. With respect to 5-HT(2A) receptors, three MPP derivatives presented moderate activity but the rest of the investigated compounds were practically inactive. The influence of changes in terminus geometry on 5-HT(1A) receptor affinity was analyzed in regard to model compounds NAN190and MM199.

Related Compounds

  • 1-(2-Methoxyphenyl...

Related Articles:

Development of a novel derivatization reagent for the sampling and analysis of total isocyanate group in air and comparison of its performance with that of several established reagents.

1996-10-01

[Am. Ind. Hyg. Assoc. J. 57(10) , 905-13, (1996)]

Comparison of hollow fiber liquid-phase microextraction and ultrasound-assisted low-density solvent dispersive liquid-liquid microextraction for the determination of drugs of abuse in biological samples by gas chromatography-mass spectrometry.

2015-05-01

[J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 989 , 46-53, (2015)]

Preparation and biodistribution of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99m as a potential brain receptor imaging agent.

2015-06-05

[Eur. J. Med. Chem. 97 , 280-8, (2015)]

Role of dermal exposure in systemic intake of methylenediphenyl diisocyanate (MDI) among construction and boat building workers.

2015-02-03

[Toxicol. Lett. 232(3) , 595-600, (2015)]

Validation of a diffusive sampling method for airborne low-molecular isocyanates using 4-nitro-7-piperazinobenzo-2-oxa-1,3-diazole-impregnated filters and liquid chromatography-tandem mass spectrometry.

2006-11-17

[J. Chromatogr. A. 1134(1-2) , 112-21, (2006)]

More Articles...