MarketPravadoline
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Pravadoline

Pravadoline (WIN 48,098) is an anti-inflammatory and analgesic drug with an IC50 of 4.9 μM 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).

Animal studies
Administration of pravadoline on rats showed: • Prolonged the response latency induced by tail immersion in hot water at a temperature of 55 °C (minimum effective dose 100 mg/kg s.c.) • Prevented hyperalgesia in rats with brewer's yeast injections during (Randall-Selitto test) (minimum effective dose 1 mg/kg, p.o.) • Prevented the nociceptive response induced by paw flexion in the adjuvant-arthritic rat (ED50 41 mg/kg, p.o.) • Prevented the nociceptive response of bradykinin-induced head and forepaw flexion (ED50 78 mg/kg, p.o.) The antinociceptive activity of pravadoline cannot be explained by an opioid mechanism, because pravadoline-induced antinociception was not antagonized by naloxone (1 mg/kg, s.c.) and pravadoline did not bind to the opioid receptors at concentrations up to 10 μM. ==See also==
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