Endomorphinsarerecentlydiscoveredendogenousopioidpeptidescomposedoffouraminoacids:Endomorphin-1(EM-1)isTyr-Pro-Trp-Phe-NH2,and Endomorphin-2(EM-2)isTyr-Pro-Phe-Phe-NH2.Thesepeptideshaveaveryhighaffinityandspecificityformu-opioidreceptorsasithasbeenreportedinmanypharmacologicalstudies.EM-1isdistributedinmanybrainregions,whereasEM-2isprevalentinbrainstemandspinalcord. EM-1andEM-2exerttheirantinociceptiveactivitybyinteractingwithmu-opioidreceptors.EM-1anfEM-2bindwithmu-opioidreceptorwithhighaffinityandselectivityincomparisonwithbindingtoopioiddeltaandkappareceptors.EM-1andEM-2tetrapeptidesactivateG-proteinsandinhibitadenylylcyclaseactivitywhenbindtomu-opioidreceptors.
Image:Endomorphin-2Staininginratdorsalhorn.
Note:Ouraffinity-purifiedantiEND-1antibody labelneuronalfibersinvariousbrainregionsincluding(butnotlimitedto)thalamicnuclei,periaqueductalgraymatter,amygdala,locuscoeruleus,nucleusaccumbens,parabrachialnucleus,nucleustractussolitariusandseptum.Ouraffinity-purifiedanti EM-2antibodieslabelneuronalprocessesinspinalcorddorsalhornandtrigeminaltract,andlabelneuronalcellbodiesinthalamus. END-1and2 distributioninbrainoverlapswithmu-opioidreceptors.
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