Analgesics and narcotics

Analgesic and Narcotic Antagonist Activity of Some Hasubanan Alkaloids in Mice"... 

By the early part of the nineteenth century the main constituent, morphine, had been isolated by Wilhelm Serturner in Germany and shown to be a powerful analgesic and narcotic, able to induce sleep. He called it morphine after Morpheus, the Greek god of dreams. The invention of the hypodermic syringe allowed morphine to be injected which made it more rapidly effective but also increased its addictive properties. 

Opium has been widely used as a recreational drug and pain-killing remedy for centuries. The analgesic and narcotic effects of opium are largely due to morphine. Poppy seed tea, which contains morphine, was used as a folk remedy in parts of England until World War II. 

Morphine binds with very high affinity to several receptors in the CNS and is a potent analgesic and central depressant. It is also the prototype for many semisynthetic derivatives (e.g., naloxone, oxycodone, ethorphine, nalbuphine, and buprenophine) with various degrees of analgesic and narcotic properties. Heroin is diacetyl morphine. 

Redhill, Surrey, United Kingdom Opioid analgesics and narcotic antagonists... 

Olofson and Martz have developed numerous applications of ACE-CI to the N-dealkylation of significant tertiary amines, especially in the field of analgesics and narcotic antagonists alkaloids, for example in a brilliant synthesis of Nalbuphine from Oxycodone in 69 % overall yield (Ref. 191). The scope and limitations of ACE-CI as a new reagent for the selective, high-yield N-dealkylation of tertiary amines will be examined in section 4-5 of voi. 2. 

The 93-propyl levo Isomer (3c) was considerably more potent subcutaneously than morphine, while the 9oi-propyl levo Isomer (3d) was equipotent with morphine as an analgesic. None of the optical isomers suppressed withdrawal signs in monkeys the 9f5-propyl levo isomer exacerbated the withdrawal syndrome, indicating that it possesses some narcotic antagonist activity.The most active compound (4) of six homobenzomorphans was as potent subcutaneously as morphine (measured by pressure stimuli on mouse tail).115,116 Simplified procedures for the synthesis of the 6,7-benzomor-phan series have been described.117,118 Several 11-hydroxy and 11-alkoxy-2,6-methano-3-benzazocines display as potent analgesic and narcotic antagonist activity as cyclazocine.H ... 

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