Antinociceptive, prolactin releasing and intestinal motility inhibiting activities of dermorphin and analogues after subcutaneous administration in the rat.
A series of analogues and shorter homologues of dermorphin (DM), a frog skin heptapeptide with potent morphine-like activity, have been assayed in the rat after subcutaneous (SC) administration at the screening dose of 4 mg/kg. The effects taken into account are: analgesia (tail-pinch test), stimulation of prolactin (PRL) secretion, and inhibition of gastro-intestinal (GI) motility (charcoal meal transit). Effective doses were calculated for the most active compounds. The potency of DM (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) in the different tests was: tail-pinch: ED50 = 0.83 mg/kg; PRL release: ED100 = 0.3 mg/kg; inhibition of GI motility: ED30 = 1.8 mg/kg.
D000818:Animals; D005769:Gastrointestinal Motility / Q000187:drug effects*; D007279:Injections, Subcutaneous; D008297:Male; D009294:Narcotics / Q000494:pharmacology*; D009619:Nociceptors / Q000187:drug effects*; D009842:Oligopeptides / Q000008:administration & dosage / Q000494:pharmacology*; D018847:Opioid Peptides; D010146:Pain / Q000503:physiopathology; D011388:Prolactin / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D009294:Narcotics; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin; D011388:Prolactin