Pravadoline is a nonacidic, aminoalkylindole analgesic agent that inhibits cyclooxygenase.pravadoline sales,WIN 48098,am964,rcs 4 cannabinoid,win55 512 2,pravadoline for sale
Like NSAIDs, pravadoline inhibits prostaglandin synthesis (IC50 = 5 ?M in mouse brain microsomes) and displays antinociceptive activity (ED50 = 26 mg/kg in an acetylcholine-induced writhing assay in mice).
In contrast to NSAIDs, pravadoline inhibits neuronally stimulated contractions in mouse vas deferens preparations (IC50 = 0.45 ?M), an effect similar to that which is produced by opioid analgesics, yet is not attenuated by the opioid receptor antagonist, naloxone.
Pravadoline does not produce gastrointestinal irritation following acute or chronic administration to rodents.
Pravadoline� is an antiinflammatory and analgesic drug with an IC50�of 4.9�?M and a�Ki�of 2511�nM at�CB1, related in structure to�nonsteroidal anti-inflammatory drugs�(NSAIDs) such as�indometacin.
It was developed in the 1980s as a new antiinflammatory and�prostaglandin�synthesis inhibitor, acting through inhibition of the enzyme�cyclooxygenase�(COX).pravadoline sales,WIN 48098,am964,rcs 4 cannabinoid,win55 512 2
However, pravadoline was found to exhibit unexpectedly strong analgesic effects, which appeared at doses ten times smaller than the effective anti-inflammatory dose and so could not be explained by its action as a�COX inhibitor.HU-331
These effects were not blocked by opioid�antagonists�such as�naloxone,�and it was eventually discovered that pravadoline represented the first compound from a novel class of�cannabinoid�agonists, the aminoalkylindoles.pravadoline for sale
Pravadoline was never developed for use as an analgesic, partly due to toxicity concerns (although these were later shown to be a result of the salt form that the drug had been prepared in rather than from the pravadoline itself),
however the discovery of cannabinoid activity in this structurally novel family of drugs led to the discovery of several new cannabinoid agonists, including the drug�WIN 55,212-2, which is now widely used in scientific research.
Chemical and physical data
Molar mass 378.46 g/mol