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Literature DB >> 6328494

beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin.

Abstract

Competitive antagonism of human beta-endorphin (beta h-EP)-induced analgesia by synthetic beta h-EP analogs with high in vitro opiate receptor binding to in vivo analgesic potency ratio has been demonstrated. A parallel shift of the dose-response curve for analgesia to the right was observed when either beta h-EP or [ Trp27 ] -beta h-EP was coinjected with various doses of [Gln8, Gly31 ]-beta h-EP-Gly-Gly-NH2, [Arg9,19,24,28,29]-beta h-EP, or [ Cys11 ,26, Phe27 , Gly31 ]-beta h-EP. It was estimated that the most potent antagonist, [Gln8, Gly31 ]-beta h-EP-Gly-NH2, is at least 200 times more potent than naloxone.

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Year: 1984 PMID： 6328494 PMCID： PMC345223 DOI： 10.1073/pnas.81.10.3074

Source DB: PubMed Journal: Proc Natl Acad Sci U S A ISSN： 0027-8424 Impact factor: 11.205

29 in total

beta-Endorphin-induced analgesia is inhibited by synthetic analogs of beta-endorphin.

1. Opioid activity of a peptide, beta-lipotropin-(61-91), derived from beta-lipotropin.

2. Isolation and structure of an untriakontapeptide with opiate activity from camel pituitary glands.

3. C fragment of lipotropin has a high affinity for brain opiate receptors.

4. The C-fragment of lipotropin - a potent analgesic [proceedings].

5. Beta-Endorphin as a potent analgesic by intravenous injection.

6. Comparative study on analgesic effect of Met5-enkephalin and related lipotropin fragments.

7. beta-endorphin is a potent analgesic agent.

8. Quantitative studies of the antagonism of morphine by nalorphine and naloxone.

9. Synthesis and analgesic activity of human beta-endorphin.

10. Some quantitative uses of drug antagonists.

1. Beta-endorphin-(1-27) is a naturally occurring antagonist of the reinforcing effects of opioids.

2. Beta-endorphin-(1-27) is a naturally occurring antagonist to etorphine-induced analgesia.

3. Opioid-receptor antagonism increases pain and decreases pleasure in obese and non-obese individuals.