PMID- 6717754 OWN - NLM STAT- MEDLINE DCOM- 19840607 LR - 20190726 IS - 0028-3908 (Print) IS - 0028-3908 (Linking) VI - 23 IP - 1 DP - 1984 Jan TI - Comparison of the antinociceptive effects of intracerebroventricular injection of kyotorphin, cyclo (N-methyl-Tyr-Arg) and Met-enkephalin in mice. PG - 7-12 AB - Intracerebroventricular (i.c.v.) administration of kyotorphin (L-Tyrosine-L-Arginine) or Metenkephalin (Met-ENK) to conscious mice resulted in a dose-dependent antinociceptive effect as measured by three pain tests. Cyclo(N-methyl-L-Tyrosine-L-Arginine) (cyclo NMTA), an analogue of kyotorphin, increased the reaction time in the tail-pressure and tail-flick tests. Both dipeptides also decreased writhing induced by acetic acid. However, the antinociceptive activity of cyclo NMTA was substantially greater than that of kyotorphin or Met-enkephalin. At the maximum effective dose of 62.7 nmol/mouse, this cyclic dipeptide produced a more long-lasting antinociceptive effect than did kyotorphin or Met-enkephalin. Antinociception induced by cyclo NMTA or kyotorphin was significantly reversed by pretreatment with naloxone (2 or 8 mg/kg, i.p.), though naloxone was not as effective an antagonist of the antinociceptive action of these peptides as it was against Met-enkephalin. The results indicate that the antinociceptive effect induced by cyclo NMTA may in part involve the endogenous opioid system in mice. FAU - Sakurada, T AU - Sakurada T FAU - Sakurada, S AU - Sakurada S FAU - Watanabe, S AU - Watanabe S FAU - Kawamura, S AU - Kawamura S FAU - Sato, T AU - Sato T FAU - Kisara, K AU - Kisara K FAU - Akutsu, Y AU - Akutsu Y FAU - Sasaki, Y AU - Sasaki Y FAU - Suzuki, K AU - Suzuki K LA - eng PT - Comparative Study PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - Neuropharmacology JT - Neuropharmacology JID - 0236217 RN - 0 (Analgesics) RN - 0 (Endorphins) RN - 0 (Peptides, Cyclic) RN - 02N30CW3X0 (kyotorphin) RN - 36B82AMQ7N (Naloxone) RN - 58569-55-4 (Enkephalin, Methionine) RN - 83481-39-4 (cyclo(N-methyltyrosylarginyl)) SB - IM MH - *Analgesia MH - *Analgesics MH - Animals MH - Endorphins/administration & dosage/*pharmacology MH - Enkephalin, Methionine/administration & dosage/*pharmacology MH - Injections, Intraventricular MH - Male MH - Mice MH - Naloxone/pharmacology MH - Nociceptors/drug effects MH - Peptides, Cyclic/administration & dosage/*pharmacology EDAT- 1984/01/01 00:00 MHDA- 1984/01/01 00:01 CRDT- 1984/01/01 00:00 PHST- 1984/01/01 00:00 [pubmed] PHST- 1984/01/01 00:01 [medline] PHST- 1984/01/01 00:00 [entrez] AID - 10.1016/0028-3908(84)90209-0 [doi] PST - ppublish SO - Neuropharmacology. 1984 Jan;23(1):7-12. doi: 10.1016/0028-3908(84)90209-0.