Biomaterial Database

Evidence that nalorphine, butorphanol and oxilorphan are partial agonists at a kappa-opioid receptor. 1983

J D Leander

Nalorphine, butorphanol and oxilorphan were compared in their ability to increase urinary output in the normally hydrated rat and to antagonize the increased urinary output produced by the full kappa-agonist, bremazocine. Nalorphine, butorphanol and oxilorphan increased 5-h cumulative urine output compared to controls, but the maximal effect was less than half the amount excreted after injection with 0.08 mg/kg of bremazocine. The effects of bremazocine were antagonized by nalorphine, butorphanol and oxilorphan. These effects of nalorphine, butorphanol and oxilorphan satisfy the criteria for classifying these agents as partial agonists at the kappa-opioid receptor responsible for mediating the effect of increased urinary output.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D009019	Morphinans	Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.	Morphinan
D009269	Nalorphine	A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.	Allylnormorphine,Lethidrone,Nalorphine Hydrobromide,Nalorphine Hydrochloride,Nalorphine, (14 alpha)-Isomer,Nalorphine, L-tartrate (1:1),Hydrobromide, Nalorphine,Hydrochloride, Nalorphine
D009292	Narcotic Antagonists	Agents inhibiting the effect of narcotics on the central nervous system.	Competitive Opioid Antagonist,Narcotic Antagonist,Opioid Antagonist,Opioid Antagonists,Opioid Receptor Antagonist,Opioid Reversal Agent,Competitive Opioid Antagonists,Opioid Receptor Antagonists,Opioid Reversal Agents,Agent, Opioid Reversal,Agents, Opioid Reversal,Antagonist, Competitive Opioid,Antagonist, Narcotic,Antagonist, Opioid,Antagonist, Opioid Receptor,Antagonists, Competitive Opioid,Antagonists, Narcotic,Antagonists, Opioid,Antagonists, Opioid Receptor,Opioid Antagonist, Competitive,Opioid Antagonists, Competitive,Receptor Antagonist, Opioid,Receptor Antagonists, Opioid,Reversal Agent, Opioid,Reversal Agents, Opioid
D011957	Receptors, Opioid	Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.	Endorphin Receptors,Enkephalin Receptors,Narcotic Receptors,Opioid Receptors,Receptors, Endorphin,Receptors, Enkephalin,Receptors, Narcotic,Receptors, Opiate,Endorphin Receptor,Enkephalin Receptor,Normorphine Receptors,Opiate Receptor,Opiate Receptors,Opioid Receptor,Receptors, Normorphine,Receptors, beta-Endorphin,beta-Endorphin Receptor,Receptor, Endorphin,Receptor, Enkephalin,Receptor, Opiate,Receptor, Opioid,Receptor, beta-Endorphin,Receptors, beta Endorphin,beta Endorphin Receptor,beta-Endorphin Receptors
D002077	Butorphanol	A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.	17-(Cyclobutylmethyl)morphinan-3,14-diol,Apo-Butorphanol,BC-2627,Beforal,Butorphanol Tartrate,Dolorex,Moradol,Stadol,Stadol NS,Torbugesic,BC 2627,BC2627
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus