Opiate receptor binding-enhancement by opiate administration in vivo

Candace B. Pert, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

Administration of opiate agonists and antagonists to mice produces a dose-dependent 50-100 per cent enhancement of stereospecific [3H]dihydromorphine or [3H]naloxone binding to brain homogenates within 5 min. Three opiate antagonists are 10-1000 times more potent in eliciting this increase in binding than their structurally analogous agonists. Naloxone, the antagonist with the least agonist activity, is the most potent drug in producing receptor enhancement. Implantation of morphine pellets in mice increases receptor binding 30-100 per cent for 2 108 hr with no time-dependent trend. Drug-induced receptor binding enhancement appears to involve an increase in number of binding sites rather than a change in receptor affinity. Sodium, which increases binding of opiate antagonists in normal mouse brain homogenate, fails to increase binding of [3H]naloxone in homogenates derived from naloxone-injected mice.

Original languageEnglish (US)
Pages (from-to)847-853
Number of pages7
JournalBiochemical Pharmacology
Volume25
Issue number7
DOIs
StatePublished - Apr 1 1976

Fingerprint

Opiate Alkaloids
Opioid Receptors
Naloxone
Brain
Dihydromorphine
Drug Receptors
Pharmaceutical Preparations
Morphine
Sodium
Binding Sites

ASJC Scopus subject areas

  • Pharmacology

Cite this

Opiate receptor binding-enhancement by opiate administration in vivo. / Pert, Candace B.; Snyder, Solomon H.

In: Biochemical Pharmacology, Vol. 25, No. 7, 01.04.1976, p. 847-853.

Research output: Contribution to journalArticle

@article{0fb3a4f108324ce383186a134d2553a6,
title = "Opiate receptor binding-enhancement by opiate administration in vivo",
abstract = "Administration of opiate agonists and antagonists to mice produces a dose-dependent 50-100 per cent enhancement of stereospecific [3H]dihydromorphine or [3H]naloxone binding to brain homogenates within 5 min. Three opiate antagonists are 10-1000 times more potent in eliciting this increase in binding than their structurally analogous agonists. Naloxone, the antagonist with the least agonist activity, is the most potent drug in producing receptor enhancement. Implantation of morphine pellets in mice increases receptor binding 30-100 per cent for 2 108 hr with no time-dependent trend. Drug-induced receptor binding enhancement appears to involve an increase in number of binding sites rather than a change in receptor affinity. Sodium, which increases binding of opiate antagonists in normal mouse brain homogenate, fails to increase binding of [3H]naloxone in homogenates derived from naloxone-injected mice.",
author = "Pert, {Candace B.} and Snyder, {Solomon H}",
year = "1976",
month = "4",
day = "1",
doi = "10.1016/0006-2952(76)90157-X",
language = "English (US)",
volume = "25",
pages = "847--853",
journal = "Biochemical Pharmacology",
issn = "0006-2952",
publisher = "Elsevier Inc.",
number = "7",

}

TY - JOUR

T1 - Opiate receptor binding-enhancement by opiate administration in vivo

AU - Pert, Candace B.

AU - Snyder, Solomon H

PY - 1976/4/1

Y1 - 1976/4/1

N2 - Administration of opiate agonists and antagonists to mice produces a dose-dependent 50-100 per cent enhancement of stereospecific [3H]dihydromorphine or [3H]naloxone binding to brain homogenates within 5 min. Three opiate antagonists are 10-1000 times more potent in eliciting this increase in binding than their structurally analogous agonists. Naloxone, the antagonist with the least agonist activity, is the most potent drug in producing receptor enhancement. Implantation of morphine pellets in mice increases receptor binding 30-100 per cent for 2 108 hr with no time-dependent trend. Drug-induced receptor binding enhancement appears to involve an increase in number of binding sites rather than a change in receptor affinity. Sodium, which increases binding of opiate antagonists in normal mouse brain homogenate, fails to increase binding of [3H]naloxone in homogenates derived from naloxone-injected mice.

AB - Administration of opiate agonists and antagonists to mice produces a dose-dependent 50-100 per cent enhancement of stereospecific [3H]dihydromorphine or [3H]naloxone binding to brain homogenates within 5 min. Three opiate antagonists are 10-1000 times more potent in eliciting this increase in binding than their structurally analogous agonists. Naloxone, the antagonist with the least agonist activity, is the most potent drug in producing receptor enhancement. Implantation of morphine pellets in mice increases receptor binding 30-100 per cent for 2 108 hr with no time-dependent trend. Drug-induced receptor binding enhancement appears to involve an increase in number of binding sites rather than a change in receptor affinity. Sodium, which increases binding of opiate antagonists in normal mouse brain homogenate, fails to increase binding of [3H]naloxone in homogenates derived from naloxone-injected mice.

UR - http://www.scopus.com/inward/record.url?scp=0017275905&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0017275905&partnerID=8YFLogxK

U2 - 10.1016/0006-2952(76)90157-X

DO - 10.1016/0006-2952(76)90157-X

M3 - Article

C2 - 938584

AN - SCOPUS:0017275905

VL - 25

SP - 847

EP - 853

JO - Biochemical Pharmacology

JF - Biochemical Pharmacology

SN - 0006-2952

IS - 7

ER -