Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug.

Article Details

Citation

Taylor DP, Carter RB, Eison AS, Mullins UL, Smith HL, Torrente JR, Wright RN, Yocca FD

Pharmacology and neurochemistry of nefazodone, a novel antidepressant drug.

J Clin Psychiatry. 1995;56 Suppl 6:3-11.

PubMed ID
7649970 [ View in PubMed
]
Abstract

Nefazodone is a new antidepressant drug with a pharmacologic profile distinct from that of the tricyclic, monoamine oxidase inhibitor, and serotonin selective reuptake inhibitor antidepressants. Nefazodone was initially discovered for its ability to block 5-HT2A receptors and its reduced potency as an alpha 1-adrenergic blocker. It was later shown to inhibit both serotonin and norepinephrine uptake in vitro, attributes which most likely impart its clinical efficacy and which differentiate nefazodone from its chemical predecessor trazodone. The combination of these two mechanisms may ultimately result in a facilitation of 5-HT1A-mediated neurotransmission, which may be beneficial for treating symptoms of depression as evidenced by recent clinical findings. In addition, the preclinical profile of nefazodone demonstrates that it has decreased anticholinergic and antihistaminic activity relative to traditional agents. Clinical findings to date are consistent with these observations.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Nefazodone5-hydroxytryptamine receptor 2AProteinHumans
Yes
Antagonist
Details
NefazodoneAlpha-1A adrenergic receptorProteinHumans
No
Antagonist
Details
NefazodoneSodium-dependent noradrenaline transporterProteinHumans
Yes
Inhibitor
Details
NefazodoneSodium-dependent serotonin transporterProteinHumans
Yes
Inhibitor
Details