Author/Authors :
Kumiko Takeuchi، نويسنده , , Todd J. Kohn، نويسنده , , Nicholas A. Honigschmidt، نويسنده , , Vincent P. Rocco، نويسنده , , Patrick G. Spinazze، نويسنده , , Susan K. Hemrick-Luecke، نويسنده , , Linda K. Thompson، نويسنده , , David C. Evans، نويسنده , , Kurt Rasmussen، نويسنده , , Deanna Koger، نويسنده , , David Lodge، نويسنده , , Laura J. Martin، نويسنده , , Janice Shaw، نويسنده , , Penny G. Threlkeld، نويسنده , , David T. Wong، نويسنده ,
Abstract :
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinities at the 5-HT1A receptor and serotonin reuptake site in vitro. In vivo evaluation of this series of compounds demonstrated elevated extracellular serotonin levels from the basal and quick recovery of neuron firing that was presumably suppressed by the initial acute activation of 5-HT1A somatodendritic autoreceptors.
Keywords :
Serotonin , 5- HT1A receptor antagonist , Selective serotonin reuptake inhibitor , 5-HT1A/SSRI , Antidepressants , 1-Aryloxy-3-piperidinylpropan-2-ols
