Opioids morphine derivatives

The chemical structures and biological activities of hundreds of opioid analgesics derived from the prototype opioid drug morphine are most comprehensively described in two books published in 1986, one entitled Opioid Analgesics, Chemistry and Receptors by Casy and Parfitt [1] and the other entitled Opiates by Lenz et al. [2]. Follow-up articles include those by Casy in 1989, entitled Opioid Receptors and their Ligands Recent Developments [3] which also includes sections on opioid peptides, affinity labelling and opioid receptor subtypes Rees and Hunter in 1990 [4] covering the... 

It is worth mentioning that iV-allylic substitution in a number of morphine derivatives, as a rule, leads to antagonistic properties. Naloxone is a few times stronger than nalorphine as an antagonist. It blocks opiate receptors. It eliminates central and peripheral action of opioids, including respiratory depression. Naloxone is used upon overdose of narcotic analgesics.Synonyms for this drug are narkan, talwin, and others. 

Pharmacology Buprenorphine is a semisynthetic centrally acting opioid analgesic derived from thebaine a 0.3 mg dose is approximately equivalent to 10 mg morphine in analgesic effects. Buprenorphine exerts its analgesic effect via high affinity binding of CNS opiate receptors. 

For centuries opium was used for both medicinal and recreational purposes. Derived from the poppy Papaver somniferum, it contains numerous opiates, the primary one of which is morphine. The term opiate has largely been replaced by opioid, which represents all compounds with morphinelike activity and includes morphine, morphine derivatives, and peptides. Opiate is used to refer to morphinelike drugs derived from the plant and structurally similar analogues. These drugs are frequently referred to as narcotics, a Greek term for stupor, which is scientifically obsolete. Even in its early history, opium presented a problem when it was smoked or taken orally. The introduction of the hypodermic needle and syringe, however, drastically enhanced the euphoric properties of opioids and thereby altered their abuse liability. In addition, the synthesis of heroin resulted in an opioid that was more potent than morphine and ideally suited for intravenous administration. 

The pure opioid antagonist drugs naloxone,naltrexone, and nalmefene are morphine derivatives with bulkier substituents at the l l17 position. These agents have a relatively high affinity for - opioid binding sites. They have lower... 

An examination of the structure-activity relationship (SAR) of a series of enkephalin analogues and morphine derivatives in competing with the binding of radioisotope labeled DADLE and FK 33-824 or opiates revealed that DADLE binds to an opioid receptor selective to Leu-enkephalin and its analogues. In contrast, FK 33-824, morphine, or naloxone binds to opioid receptors with selectivity in favor of morphine and derivatives simi-... 

To date more than 50 pharmaceuticals or drugs of abuse have been reported to be detectable in hair after oral or parenteral administration, in addition to the "classical" drugs mentioned above. The present chapter aims to review the papers devoted to these "unusual" compounds, that have been categorized in 11 classes opioids (i.e., semisynthetic or synthetic morphine derivatives), hallucinogens, psychostimulants (including nicotine), barbiturates, benzodiazepines, other sedatives/hypnotics. 

Lopez D, Quinoa E, Riguera R (2000) The [4+2] addition of singlet oxygen to thebaine new access to highly functionalized morphine derivatives via opioid endoperoxides. J Org Chem 65 4671 678... 

FIGURE 17.5 Opioids. Morphine and codeine are natural alkaloids in the opium poppy. Heroin is a synthetic derivative with similar activity as a drug, but it is dangerously addictive. 

Oripavine is an opiate and the major metabolite of thebaine. It is the parent compound from which a series of semisynthetic opioids are derived, which includes the compounds etorphine and buprenorphine. Although its analgesic potency is comparable to morphine, it is not used clinically due to its severe toxicity and low therapeutic index. Oripavine possesses an analgesic potency comparable to morphine however, it is not clinically useful due to severe toxicity and low therapeutic index. In both mice and rats, toxic doses caused tonic-clonic seizures followed by death, similar to thebaine. Oripavine has a potential for dependence which is significantly greater than that of thebaine but slightly less than that of morphine. 

Opioids and morphine derivatives Fentanyl, Codeine, Heroin, Morphine, Opium, Methadone, Oxycodone, HCL... 

In the strict sense, opiates are drugs which are derived from opium and include the natural products morphine, codeine, thebaine and many semi-synthetic congeners derived from them. In the wider sense, opiates are morphine-like drugs with non-peptidic structures. The old term opiates is now more and more replaced by the term opioids which applies to any substance, whether endogenous or synthetic, pqrtidic or non-peptidic, that produces morphine-like effects through an action on opioid receptors. 

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