Drug intelligence / Profile preview

thebaine

Development stage
Discontinued
Lead developer
Antheia
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Not Used Therapeutically; No Clinical Route Of Administration.
01

Overview

Thebaine is a naturally occurring opiate alkaloid found in the opium poppy (Papaver somniferum) and related species. Chemically similar to morphine and codeine, it differs by having stimulatory rather than depressant effects. At high doses, it can cause convulsions similar to strychnine poisoning. Thebaine itself is not used therapeutically but serves as a key precursor for the industrial synthesis of several important opioid medications including hydrocodone, oxycodone, oxymorphone, naloxone, naltrexone, buprenorphine and others. Its mechanism of action includes antagonism at glycine and GABA receptors in addition to weak activity at opioid receptors; however its primary pharmacological significance lies in its role as a chemical intermediate rather than as an active pharmaceutical ingredient[3][4][7][10].

Other names
paramorphinecodeine methyl enol ether
02

Targets

DOR (Opioid Receptor Delta 1)GABRR (GABA-A receptor subunit rho)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)Glycine receptor

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