Drug intelligence / Profile preview

Aceprometazine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Aceprometazine is a phenothiazine derivative with neuroleptic, sedative, antihistamine, and antiemetic properties. It primarily functions by blocking dopamine D2 receptors in the brain, which contributes to its antipsychotic and sedative effects. Additionally, it acts as an antihistamine by blocking histamine H1 receptors, providing sedative and anti-allergy benefits. The drug also exhibits anticholinergic effects, which can reduce secretions and muscular spasms, and its comprehensive receptor blockade aids in mitigating nausea and vomiting. While it has been used in human medicine for conditions such as anxiety, depression, and sleep disorders (often in combination with meprobamate), its use in humans has become less frequent due to the availability of newer drugs with more favorable side effect profiles. It is also used in veterinary medicine. Aceprometazine can be administered orally, intramuscularly, and intravenously.

02

Targets

DRD4 (Dopamine D4 Receptor)HRH1 (Histamine H1 Receptor)ADRA2A (α2A)HTR2A (Serotonin receptor 5-HT2A)KCNH2 (Voltage-gated potassium channel subfamily H member 2)DRD1 (Dopamine D1 Receptor)ADRA1A (α1A)5-HT1R (5-HT1 receptor family)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)

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