01 · How it works
Classification and primary mechanism
Heroin is rapidly deacetylated in the body into 6-monoacetylmorphine (6-MAM) and morphine, which bind with high affinity to mu-opioid receptors. This binding inhibits the release of GABA, disinhibiting dopaminergic neurons in the mesolimbic system and causing an intense analgesic and euphoric surge. Its two added acetyl groups make diacetylmorphine significantly more lipophilic than natural morphine, allowing it to cross the blood-brain barrier within seconds to produce the characteristic rapid opioid "rush."
