Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.

Article Details

Citation

Fernandez J, Alonso JM, Andres JI, Cid JM, Diaz A, Iturrino L, Gil P, Megens A, Sipido VK, Trabanco AA

Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.

J Med Chem. 2005 Mar 24;48(6):1709-12.

PubMed ID
15771415 [ View in PubMed
]
Abstract

A series of novel tetracyclic tetrahydrofuran derivatives was prepared and evaluated for its potential psychotropic properties. In vitro affinities for multiple dopaminergic, serotonergic, alpha-adrenergic, and histamine receptors and for the norepinephrine transporter as well as the ED(50) values obtained in some in vivo assays for antipsychotic, anxiolytic, and antidepressant potential are reported. Compounds (-)-1, (-)-8d, and (+)-8d have been identified as potential broad-spectrum psychotropic agents.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
OlanzapineD(1) dopamine receptor (Protein Group)Protein groupHumans
Unknown
Antagonist
Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Clozapine5-hydroxytryptamine receptor 2AKi (nM)6.3N/AN/ADetails
Clozapine5-hydroxytryptamine receptor 2CKi (nM)21N/AN/ADetails
Clozapine5-hydroxytryptamine receptor 7Ki (nM)48N/AN/ADetails
ClozapineAlpha-2A adrenergic receptorKi (nM)24N/AN/ADetails
ClozapineAlpha-2C adrenergic receptorKi (nM)2.9N/AN/ADetails
ClozapineDopamine D2 receptorKi (nM)144N/AN/ADetails
ClozapineDopamine D3 receptorKi (nM)242N/AN/ADetails
ClozapineHistamine H1 receptorKi (nM)1.1N/AN/ADetails
Haloperidol5-hydroxytryptamine receptor 2AKi (nM)435N/AN/ADetails
HaloperidolDopamine D2 receptorKi (nM)2.5N/AN/ADetails
HaloperidolDopamine D3 receptorKi (nM)4.4N/AN/ADetails
Mianserin5-hydroxytryptamine receptor 2AKi (nM)4.3N/AN/ADetails
Mianserin5-hydroxytryptamine receptor 2CKi (nM)4.4N/AN/ADetails
Mianserin5-hydroxytryptamine receptor 7Ki (nM)56N/AN/ADetails
MianserinAlpha-2A adrenergic receptorKi (nM)4.8N/AN/ADetails
MianserinAlpha-2C adrenergic receptorKi (nM)3.8N/AN/ADetails
MianserinDopamine D2 receptorKi (nM)2197N/AN/ADetails
MianserinDopamine D3 receptorKi (nM)2841N/AN/ADetails
MianserinHistamine H1 receptorKi (nM)1.7N/AN/ADetails
Mirtazapine5-hydroxytryptamine receptor 2AKi (nM)69N/AN/ADetails
Mirtazapine5-hydroxytryptamine receptor 2CKi (nM)39N/AN/ADetails
MirtazapineAlpha-2A adrenergic receptorKi (nM)20N/AN/ADetails
MirtazapineHistamine H1 receptorKi (nM)1.6N/AN/ADetails
Olanzapine5-hydroxytryptamine receptor 2AKi (nM)2.3N/AN/ADetails
Olanzapine5-hydroxytryptamine receptor 2CKi (nM)14N/AN/ADetails
OlanzapineDopamine D2 receptorKi (nM)78N/AN/ADetails
OlanzapineDopamine D3 receptorKi (nM)43N/AN/ADetails
OlanzapineHistamine H1 receptorKi (nM)1.2N/AN/ADetails