DPI-3290 was discovered by scientists at Burroughs Wellcome and licensed to Delta Pharmaceutical [1] and is a drug that is used in scientific research. It is a potent analgesic drug,[2] which produces little respiratory depression.[3]
DPI-3290 acts as an agonist at both μ- and δ-opioid receptor, with an IC50 of 6.2nM at μ and 1.0nM at δ.[4]
See also
References
- ^ US Patent 5552404 - Opioid compounds and methods for using same
- ^ Gengo PJ, Pettit HO, O'Neill SJ, Wei K, McNutt R, Bishop MJ, Chang KJ (December 2003). "DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. I. A mixed opioid agonist with potent antinociceptive activity". The Journal of Pharmacology and Experimental Therapeutics. 307 (3): 1221–6. doi:10.1124/jpet.103.054361. PMID 14534368. S2CID 93569860.
- ^ Gengo PJ, Pettit HO, O'Neill SJ, Su YF, McNutt R, Chang KJ (December 2003). "DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. II. A mixed opioid agonist with potent antinociceptive activity and limited effects on respiratory function". The Journal of Pharmacology and Experimental Therapeutics. 307 (3): 1227–33. doi:10.1124/jpet.103.054429. PMID 14534367. S2CID 45159720.
- ^ Ananthan S (March 2006). "Opioid ligands with mixed mu/delta opioid receptor interactions: an emerging approach to novel analgesics". The AAPS Journal. 8 (1): E118-25. doi:10.1208/aapsj080114. PMC 2751430. PMID 16584118.