Analgesic mechanism

A COX-2 inhibitor s analgesic mechanism may not be as simple as sometimes thought, because COX-2 inhibitors reduce pain, even in noninflammatory conditions. 

Papaver somniferum Papaveraceae (opium poppy) has been used as an analgesic since 3000 BC [26]. The opium latex contains many alkaloids, including codeine, thebaine, papaverine and morphine - its main analgesic constituent [27]. Although morphine has found large clinical use, its analgesic mechanism was first elucidated only with the discovery of both endogenous peptide opioids (such as enkephalins, dynorphins, endorphins and nociceptin) and the opioid receptors, p, 8, k... 

Morphine and its salts are very valuable analgesic drugs but are highly addictive. In addition to suppression of pain, morphine causes constipation, decreases pupillary size and depresses respiration. Only the (-l-)-stereoisoraer is biologically active. They appear to produce their effects on the brain by activating neuronal mechanisms normally activated by... 

Oxolamine [959-14-8] (57) is sold in Europe. It is an oxadiazole, and its general pharmacological profile is described (81). The compound possesses analgesic, antiinflammatory, local anesthetic, and antispasmodic properties, in addition to its antitussive activity. Although a central mechanism may account for some of the activity, peripheral inhibition of the cough reflex may be the dominant effect. The compound has been shown to be clinically effective, although it is less active than codeine (82,83). The synthesis of oxolamine is described (84). 

It is generally accepted that the narcotic analgesics do not in fact interfere with the pain as such rather, these compounds change the perception of the pain. In other words, the patient may come to regard pain with detachment. This very mechanism may be responsible for one of the major drawbacks of the narcotic 286... 

The intramolecnlar Michael addition is used as a key step for synthesis of epibaddine fScheme4 36 Epibaddine is an analgesic, operating by a nonopioid mechanism, it is severiil hundred dmes more potent than morphine... 

Acetaminophen is a nonsalicylate nonnarcotic analgesic whose mechanism of action is unknown. Lake the salicylates, acetaminophen has analgesic and antipyretic activity. However, acetaminophen does not possess antiinflammatory action and is of no value in the treatment of inflammation or inflammatory disorders. 

The dimethylheptyl side-chain analogue of 9-carboxy-A -THC, ajulemic acid, CT-3, (166) is currently in clinical development for treatment of pain and inflammation [121, 122]. Compound (166) does show some affinity for CBi and CB2 receptors, but may also exert anti-inflammatory and analgesic effects through other mechanisms. It does not appear to be psychoactive in humans [123]. 

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