History and development of mixed opioid agonists, partial agonists and antagonists.

Opioid antagonists, partial agonists, and agonists/antagonists: the role of office-based detoxification.

BACKGROUND The opioid receptor antagonists naloxone and naltrexone are competitive antagonists at the mu, kappa, and sigma receptors with a higher affinity for the mu receptor and lacking any mu receptor efficacy. Buprenorphine is classified as a partial agonist. It has a high affinity, but low efficacy at the mu receptor where it yields a partial effect upon binding. It also, however, possesse...

Potency ratio between opioid agonists and partial agonists.

POTENCY RATIO BETWEEN OPIOID AGONISTS AND PARTIAL AGONISTS Sir,—The paper by Klepper and colleagues (1986) again seems to indicate the belief of this group of workers in a fixed potency ratio between opioid agonists and partial agonists, although such a concept is theoretically unlikely (Kay, 1985). Support for a variable potency ratio is apparent in their paper, however, in that nalbuphine in ...

Marketed New Drug Delivery Systems for Opioid Agonists/Antagonists ‎Administration: A Rapid Overview

Novel drug delivery systems for controlled-release of opioid agonists as a long time painkillers or opioid antagonists for opium, heroin, and alcohol addiction are under development or in clinical use today. In this article, the field of “new drug delivery systems” is momentarily reviewed from the viewpoint of the marketed opioid agonists/antagonists dosage forms today.

Behavioral interactions of opioid agonists and antagonists with serotonergic systems.

binding of agonists and antagonists

The effect of aldosterone and antimineralocorticoids on the intracellular localization of human mineralocorticosteroid receptor (hMR) was studied using a new monoclonal anti-peptide antibody FD4. This antibody was directed against the peptide hMR-(412-422). As demonstrated by ultracentrifugation analysis, immunoprecipitation assays and Western blot, FD4 recognized both the native and denatured ...