Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 70 ·No. 7 ·1973-07-00 ·Pages 1947-9

Simon EJ, Hiller JM, Edelman I

Abstract

Etorphine, the most potent narcotic analgesic known, was labeled with tritium by catalytic exchange. This drug exhibits stereospecific, saturable binding to rat-brain homogenate. At saturation, the stereospecific binding is 0.1-0.15 pmol/mg of protein. Specific binding is inhibited high salt concentrations, sulfhydryl reagents, and proteolytic enzymes, but is unaffected by phospholipases A and C, sodium azide, sodium fluoride, and prostaglandins E(1) and E(2). Competition for binding of [(3)H]etorphine correlates with agonist and antagonist potencies. The stable, stereospecific binding of an active narcotic analgesic supports the existence of opiate receptors.

MeSH Terms

Acetamides/pharmacology Analgesics/metabolism Animals Azides/pharmacology Binding Sites Binding, Competitive Brain/metabolism Ethylmaleimide/pharmacology Fluorides/pharmacology In Vitro Techniques Levorphanol/metabolism Male Mercuribenzoates/pharmacology Methadone/metabolism Morphinans/metabolism Morphine/metabolism Nalorphine/metabolism Naloxone/metabolism Pentanols/metabolism Phospholipases/pharmacology Pronase/pharmacology Prostaglandins/pharmacology Rats Receptors, Drug/drug effects Tritium Trypsin/pharmacology

Chemicals

Acetamides Analgesics Azides Mercuribenzoates Morphinans Pentanols Prostaglandins Receptors, Drug Tritium Levorphanol Naloxone Morphine Phospholipases Trypsin Pronase Ethylmaleimide Fluorides Nalorphine Methadone

Authors & Affiliations

3 authors, click to expand affiliations / ORCID

Simon E J

Hiller J M

Edelman I

References (8)

8 references, click to expand

Studies on the intracellular distribution and tissue binding of dihydromorphine-7,8-H3 in the rat.
Proc Soc Exp Biol Med. 1966 May;122(1):6-11 PMID: 5944896
On the mechanism of action of phospholipase A and insulin on glucose entry into free adipose cells.
Biochem Biophys Res Commun. 1966 Apr 6;23(1):68-74 PMID: 5928896
Actions of etorphine hydrochloride, (M99): a potent morphine-like agent.
Br J Pharmacol Chemother. 1967 May;30(1):11-22 PMID: 4962749
Protein measurement with the Folin phenol reagent.
J Biol Chem. 1951 Nov;193(1):265-75 PMID: 14907713
Stereospecific and nonspecific interactions of the morphine congener levorphanol in subcellular fractions of mouse brain.
Proc Natl Acad Sci U S A. 1971 Aug;68(8):1742-7 PMID: 5288759
Coupling of a new, active morphine derivative to sepharose for affinity chromatography.
Proc Natl Acad Sci U S A. 1972 Jul;69(7):1835-7 PMID: 4505662
Opiate receptor: demonstration in nervous tissue.
Science. 1973 Mar 9;179(4077):1011-4 PMID: 4687585
Biochemistry of addiction.
Annu Rev Biochem. 1970;39:821-40 PMID: 4320263

Article Info

Journal

Proceedings of the National Academy of Sciences of the United States of America

Abbr.

Proc Natl Acad Sci U S A

ISSN

0027-8424

DOI

10.1073/pnas.70.7.1947

Published

1973-07-00

Pages

1947-9

Language

English

Region

United States

NLM ID

7505876

PMCID

PMC433639

Subset

External Links

PubMed source DOI: 10.1073/pnas.70.7.1947 PMC Full Text View journal details

Analysis Services

Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate.

Contact

WeChat Official Account