[Dmt1, d-1-Nal3]morphiceptin, a novel opioid peptide analog with high analgesic activity.
The morphiceptin-derived peptide [Dmt1, d-1-Nal3]morphiceptin, labeled mu-opioid receptor (MOP) with very high affinity and selectivity in the receptor binding assays. In the mouse hot plate test, [Dmt1, d-1-Nal3]morphiceptin given intracerebroventricularly (i.c.v.) produced profound supraspinal analgesia, being approximately 100-fold more potent than the endogenous MOP receptor ligand, endomorphin-2. The antinociceptive effect of this new analog lasted up to 120min. Thus, [Dmt1, d-1-Nal3]morphiceptin is an interesting and extraordinarily potent analgesic, raising the possibility of novel approaches in the design of clinically useful drugs for pain treatment.
Fichna
Jakub
J
Laboratory of Biomolecular Chemistry, Institute of Biomedicinal Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
do-Rego
Jean-Claude
JC
Chung
Nga N
NN
Costentin
Jean
J
Schiller
Peter W
PW
Janecka
Anna
A
D000701:Analgesics, Opioid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004723:Endorphins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D018847:Opioid Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000701:Analgesics, Opioid; D004723:Endorphins; D018847:Opioid Peptides; C530458:morphiceptin, Dmt(1)-Nal(3)-; C028889:morphiceptin