Drug intelligence / Profile preview

lorpiprazole

Development stage
Phase 2
Modality
Small Molecules
Administration
Oral
01

Overview

Lorpiprazole is a small molecule drug of the phenylpiperazine group, marketed under the brand name Normarex. It is classified as a serotonin antagonist and reuptake inhibitor (SARI), similar to trazodone and nefazodone. Lorpiprazole acts by antagonizing serotonin 5-HT2A and 5-HT2C receptors, alpha1 and alpha2 adrenergic receptors, H1 histaminergic receptors, and at higher doses inhibits the SERT (serotonin transporter). This pharmacological profile allows it to increase synaptic levels of serotonin as well as modulate norepinephrine and dopamine transmission. Lorpiprazole is primarily indicated for major depressive disorder but has also been marketed as an anxiolytic[1][2][3][4][5][7].

Brand names
Normarex
Other names
lorpiprazole
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA1A (α1A)ADRA2A (α2A)HRH1 (Histamine H1 Receptor)SERT (Sodium-dependent serotonin transporter)

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