HEROIN

Use

Heroin, was first commercially synthesized in 1898 byBayer company in Germany as an alternate analgesic tomorphine. Heroin is the 3,6 diacetylated form of morphine. The laboratory researchers, which also used theacetylation process to convert salicylic acid into acetylsalicylic acid (aspirin), believed that heroin would be an effectiveanalgesic with no addictive properties. This was unfortunatelynot the case. They named the product “heroin”because it made the test subjects, including some of thechemists, feel “heroic.” With both OH groups protected asan ester, heroin can pass through the blood-brain barrierquicker than morphine and lead to the euphoric “rush” thatbecomes so addictive to addicts, especially after IV injection.Once heroin is in the brain, it is quickly metabolizedto 3-acetylmorphine, which has low to zero activity at theμ-receptor and 6-acetylmorphine, which is 2 to 3 timesmore potent at the μ-receptor than morphine.Heroin is not available as a prescription product in theUnited States, although it is available in some countries totreat pain associated with cancer and myocardial infarctions.It remains one of the most widely used narcotics for illicitpurposes and places major economic burdens on society.