Analgesic activity of the naturally occurring heptapeptide [Met]enkephalin-Arg6-Phe7.
- 1 September 1980
- journal article
- research article
- Published by Proceedings of the National Academy of Sciences in Proceedings of the National Academy of Sciences
- Vol. 77 (9) , 5512-5514
- https://doi.org/10.1073/pnas.77.9.5512
Abstract
[Met]Enkephalin-Arg6-Phe7 is an opiate-like peptide normally found in the adrenal gland and brain that has analgesic (antinociceptive) activity when administered directly into the cerebral ventricles of mice. On a molar basis, [Met]enkephalin-Arg6-Phe7, with an ED50 of 38.5 nmol/mouse, is 8 times more potent than [Met]enkephalin. As with [Met]enkephalin, analgesic activity is blocked by naloxone and i.v. administration does not produce characteristic opiate effects in tests for analgesic, antidiuretic or antidiarrheal activity. [Met]Enkephalin-Arg6-Phe7 may be as important as the enkephalins in the postulated enkephalin system mediating pain and analgesia.This publication has 13 references indexed in Scilit:
- Enkephalin-Like Material Elevated in Ventricular Cerebrospinal Fluid of Pain Patients After Analgetic Focal StimulationScience, 1978
- The direct and specific opiate-like effect of Met5-enkephalin and analogues on the spinal cordNeuroscience, 1977
- A synthetic enkephalin analogue with prolonged parenteral and oral analgesic activityNature, 1977
- Immunohistochemical analysis of peptide pathways possibly related to pain and analgesia: enkephalin and substance P.Proceedings of the National Academy of Sciences, 1977
- β-Endorphin: Structure-activity relationships in the guinea pig ileum and opiate receptor binding assaysBiochemical and Biophysical Research Communications, 1977
- Analgesia induced in vivo by central administration of enkephalin in ratNature, 1976
- Identification of two related pentapeptides from the brain with potent opiate agonist activityNature, 1975
- Determination and characterization of the antinociceptive activity of intraventricularly administered acetylcholine in mice.1975
- The effect of various neurohumoral modulators on the activity of morphine and the narcotic antagonists in the tail-flick and phenylquinone tests.1970
- The antidiuretic effect of narcotic analgesics in the mouseToxicology and Applied Pharmacology, 1968