TABLE 1

Opioid receptors and ligands

Receptor and Site of ActionEffectsAgonistAntagonist
μ
    SystemicAnalgesiaDAMGOCTOP
EuphoriaMorphineNaloxone
ConstipationFentanyl
Respiratory depressionEndomorphins
β-Endorphin
    PeripheralAnalgesiaDiPOAAlvimopan
ConstipationHS731/AS006Naloxone methiodide
Reduced inflammationLoperamideMethylnaltrexone
Frakefamide
DALDA
δ
    SystemicAnalgesiaDPDPENaltrindole
ConstipationSNC 80ICI 174,864
Respiratory depressionEnkephalinsNaloxone
Deltorphin
β-Endorphin
    PeripheralAnalgesiaUK-321,130Naloxone methiodide
Constipation
κ
    SystemicAnalgesiaU-69593, U50,488Norbinaltorphimine
DiuresisBremazocineNaloxone
DysphoriaDynorphin A-B
    PeripheralAnalgesiaAsimadolineNaloxone methiodide
Reduced inflammationFE200665/CR845
  • DAMGO, [d-Ala2,N-Me-Phe4,Gly5-ol]-enkephalin; CTOP, d-Phe-Cys-Tyr-d-Trp-Orn-Thr-Pen-Thr-NH2; HS731, 14-O-methyloxymorphone; DALDA, Tyr-Arg-Phe-Lys-NH2; DPDPE, [d-Pen2,d-Pen5]-enkephalin; SNC 80, 4-(α-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide; ICI 174,864, N,N-diallyl-Tyr-Aib-Aib-Phe-Leu; U-69593, N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]dec-8-yl]acetamide; U50,488, trans-3,4-dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide.