Differential sensitivities of mouse strains to morphine and [Dmt1]DALDA analgesia.
[Dmt(1)]DALDA (H-Dmt-D-Arg-Phe-Lys-NH(2)), is a highly potent and selective mu-opioid agonist. Nevertheless, systemic [Dmt(1)]DALDA retained its analgesic actions in MOR-1 knockout animals and CXBK mice despite the inactivity of morphine in these mice. [Dmt(1)]DALDA was 6-fold less potent in C57BL/6J mice than in CD-1 mice, whereas morphine potency did not differ between the two strains. Thus, [Dmt(1)]DALDA is a highly selective mu-opioid analgesic with significant pharmacological differences with the prototypic mu-opioid morphine.
Laboratory of Molecular Neuropharmacology, Memorial Sloan Kettering Cancer Center, New York, NY 10021, USA.
Claire L
CL
Neilan
Michael A
MA
King
Grace
G
Rossi
Michael
M
Ansonoff
John E
JE
Pintar
Peter W
PW
Schiller
Gavril W
GW
Pasternak
D000701:Analgesics, Opioid / Q000494:pharmacology*; D000818:Animals; D004305:Dose-Response Relationship, Drug; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D018345:Mice, Knockout; D009020:Morphine / Q000494:pharmacology*; D009842:Oligopeptides / Q000494:pharmacology*; D010147:Pain Measurement / Q000187:drug effects; D017450:Receptors, Opioid, mu / Q000819:agonists* / Q000235:genetics; D013045:Species Specificity
C424424:2',6'-dimethyltyrosyl-arginyl-phenylalanyl-lysinamide; D000701:Analgesics, Opioid; D009842:Oligopeptides; D017450:Receptors, Opioid, mu; D009020:Morphine