Diamorphine

Diamorphine (heroin) is a semi-synthetic opioid, chemically known as diacetylmorphine, first synthesized in 1874 by acetylating morphine derived from opium poppy latex. Heroin is a prodrug; after administration (by injection, inhalation, or insufflation), it rapidly crosses the blood–brain barrier and is deacetylated to 6-monoacetylmorphine and then to morphine, which binds to μ-opioid receptors to produce analgesic and euphoric effects. Heroin itself is not pharmacologically very active at opioid receptors, but its metabolites, primarily morphine, are. It is highly addictive, with significant risks including respiratory depression, coma, and death. While heroin (diamorphine) may be used in some countries as a prescription analgesic for severe pain, it is most widely known and regulated as a substance of abuse[1][2][3][4][7][9]. The pharmacological target for heroin's effects is the μ-opioid receptor (also called mu-opioid receptor or MOP receptor), which is a G protein-coupled receptor. However, heroin is not the receptor/target; rather, it acts as a ligand (drug) for that target once metabolized to morphine[2][7]. Interacting drugs for heroin (as a substance) include naloxone and naltrexone (opioid receptor antagonists used to counteract overdose), but these interact with opioid receptors, not with heroin as a molecular target[4][7].

Other names

Heroindiacetylmorphinediamorphine3,6-diacetylmorphine