β-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia
Description
The potent opioid peptide β-endorphin is found in the brain and pituitary with two related fragments, β-endorphin-(1-27) and β-endorphin-(1-26). The fragments, retain substantial opioid-receptor binding activity but are virtually inactive analgesically. β-Endorphin-(1-27) inhibits β-endorphin-induced and etorphine-induced analgesia when coinjected intracerebroventricularly into mice. Antagonism by competition at the same site(s) is suggested from parallel shifts of the dose-response curves of etorphine or β-endorphin in the presence of β-endorphin-(1-27). Its potency is 4-5 times greater than that of the opiate antagonist naloxone. β-Endorphin-(1-26) does not antagonize the antinociceptive action of etorphine or β-endorphin in doses up to 500 pmol per animal
Additional details
Publishing Information
- Journal Title
- Proc. Natl. Acad. Sci. U.S.A
- Journal Volume
- 82
- Journal Issue
- 10
- Series
- Proc. Natl. Acad. Sci. U.S.A.
- Journal Page Range
- 3178-3181
- ISSN
- 0027-8424
- CODEN
- PNASA
INIS
- Country of Publication
- United States
- Country of Input or Organization
- United States
- INIS RN
- 17044155
- Subject category
- S62: RADIOLOGY AND NUCLEAR MEDICINE;
- Descriptors DEI
- ANALGESICS; BIOCHEMICAL REACTION KINETICS; BRAIN; DOSE-RESPONSE RELATIONSHIPS; ENDORPHINS; INHIBITION; MICE; RADIORECEPTOR ASSAY; TRITIUM COMPOUNDS
- Descriptors DEC
- ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENT; BODY; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; CENTRAL NERVOUS SYSTEM DEPRESS; DRUGS; HYDROGEN COMPOUNDS; ISOTOPE APPLICATIONS; KINETICS; MAMMALS; NERVOUS SYSTEM; NEUROREGULATORS; ORGANIC COMPOUNDS; ORGANS; PEPTIDES; POLYPEPTIDES; PROTEINS; REACTION KINETICS; RODENTS; TRACER TECHNIQUES; VERTEBRATES