US -endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia
The potent opioid peptide US -endorphin is found in the brain and pituitary with two related fragments, US -endorphin-(1-27) and US -endorphin-(1-26). The fragments, retain substantial opioid-receptor binding activity but are virtually inactive analgesically. US -Endorphin-(1-27) inhibits US -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 US -endorphin in the presence of US -endorphin-(1-27). Its potency is 4-5 times greater than that of the opiate antagonist naloxone. US -Endorphin-(1-26) does not antagonize the antinociceptive action of etorphine or US -endorphin in doses up to 500 pmol per animal.
- Research Organization:
- Univ. of California, San Francisco, CA (United States)
- OSTI ID:
- 6334305
- Journal Information:
- Proc. Natl. Acad. Sci. U.S.A.; (United States), Vol. 82:10
- Country of Publication:
- United States
- Language:
- English
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ANALGESICS
DOSE-RESPONSE RELATIONSHIPS
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MICE
TRITIUM COMPOUNDS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM DEPRESSANTS
DRUGS
ISOTOPE APPLICATIONS
KINETICS
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550601* - Medicine- Unsealed Radionuclides in Diagnostics