Drug intelligence / Profile preview

naltrexone + trazodone

Development stage
Unknown
Lead developer
Biovista
Modality
Small Molecules
Administration
Oral
01

Overview

Naltrexone + trazodone is a combination of two small molecule drugs, each with distinct mechanisms of action. Naltrexone is an opioid receptor antagonist primarily used for the management of opioid and alcohol dependence. It blocks the effects of opioids by competitively binding to opioid receptors, and at low doses may also inhibit microglial activation via TLR4 antagonism, potentially reducing neuroinflammation. Trazodone is an antidepressant with complex pharmacology; it inhibits serotonin reuptake and acts as an antagonist at several serotonin (notably 5-HT2A) and alpha-1 adrenergic receptors, as well as histamine H1 receptors. This combination has been explored in research settings for rapid opiate detoxification protocols and proposed for use in conditions such as chronic fatigue syndrome due to their complementary actions on neuroinflammation, sleep regulation, mood stabilization, and withdrawal symptom control[1][4][5][6].

02

Targets

SERT (Sodium-dependent serotonin transporter)TLR4 (Toll-like receptor 4)HRH1 (Histamine H1 Receptor)MOR (Mu opioid receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)

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