PMID- 2869809
OWN - NLM
STAT- MEDLINE
DCOM- 19860514
LR  - 20190510
IS  - 0007-1188 (Print)
IS  - 0007-1188 (Linking)
VI  - 87
IP  - 1
DP  - 1986 Jan
TI  - Dermorphin analogues containing D-kyotorphin: structure-antinociceptive 
      relationships in mice.
PG  - 183-9
AB  - The antinociceptive effects of synthetic dermorphin and its analogues containing 
      D-Arg in position 2 injected into the lateral cerebroventricle were examined in 
      conscious mice. Intracerebroventricular (i.c.v.) administration of dermorphin and 
      [D-Arg2] dermorphin produced potent and long-lasting antinociceptive activity as 
      assayed by the tail-pressure test. Dermorphin and [D-Arg2] dermorphin were 210 
      and 52 times more potent than morphine, respectively. The antinociceptive effects 
      produced by these heptapeptides were antagonized by a low dose (0.5 mg kg-1, 
      i.p.) of the opioid antagonist naloxone. The ED50 values for [D-Arg2] dermorphin 
      (1-6), (1-5) and (1-4) were not significantly different from that for [D-Arg2] 
      dermorphin. The potency of the shortest fragment, [D-Arg2] dermorphin (1-2) was 
      found to possess a severely reduced activity, whilst [D-Arg2] dermorphin (1-3) 
      maintained activity and was 10 times more potent than morphine. [D-Arg2] 
      dermorphin analogues showed almost identical effects when tested on the 
      electrically-induced contractions of the guinea-pig isolated ileum. These results 
      led us to conclude that the presence of the N-terminal tripeptide in the 
      structure of [D-Arg2] dermorphin is of crucial importance for the manifestation 
      of the full intrinsic opioid-like antinociceptive activity of [D-Arg2] 
      dermorphin, which is presumably mediated through opioid receptors in the brain.
FAU - Kisara, K
AU  - Kisara K
FAU - Sakurada, S
AU  - Sakurada S
FAU - Sakurada, T
AU  - Sakurada T
FAU - Sasaki, Y
AU  - Sasaki Y
FAU - Sato, T
AU  - Sato T
FAU - Suzuki, K
AU  - Suzuki K
FAU - Watanabe, H
AU  - Watanabe H
LA  - eng
PT  - Journal Article
PL  - England
TA  - Br J Pharmacol
JT  - British journal of pharmacology
JID - 7502536
RN  - 0 (Analgesics, Opioid)
RN  - 0 (Oligopeptides)
RN  - 0 (Opioid Peptides)
RN  - 0 (Peptide Fragments)
RN  - 2SEC01B703 (dermorphin)
RN  - 96425-96-6 (dermorphin, Arg(2)-)
SB  - IM
MH  - Analgesics, Opioid/*pharmacology
MH  - Animals
MH  - Dose-Response Relationship, Drug
MH  - Electric Stimulation
MH  - Guinea Pigs
MH  - Ileum/drug effects
MH  - In Vitro Techniques
MH  - Male
MH  - Mice
MH  - Muscle Contraction/drug effects
MH  - Oligopeptides/*pharmacology
MH  - Opioid Peptides
MH  - Peptide Fragments/pharmacology
MH  - Structure-Activity Relationship
PMC - PMC1916917
EDAT- 1986/01/01 00:00
MHDA- 1986/01/01 00:01
PMCR- 1987/01/01
CRDT- 1986/01/01 00:00
PHST- 1986/01/01 00:00 [pubmed]
PHST- 1986/01/01 00:01 [medline]
PHST- 1986/01/01 00:00 [entrez]
PHST- 1987/01/01 00:00 [pmc-release]
AID - 10.1111/j.1476-5381.1986.tb10170.x [doi]
PST - ppublish
SO  - Br J Pharmacol. 1986 Jan;87(1):183-9. doi: 10.1111/j.1476-5381.1986.tb10170.x.